Publications

(200) “Divergent, C-C Bond Forming Macrocyclizations Using Modular Sulfonylhydrazone and Derived Substrates,” Xu, W.; Brown, L.E.; Porco, J.A. Jr. J Org Chem, 2021, Nov 3.  DOI: 10.1021/acs.joc.1c01848. Online ahead of print.

(119) “A forward genetic screen identifies modifiers of rocaglate responsiveness.” Shen, L., Pugsley, L., Cencic, R., Wang, H., Robert, F., Naineni, S.K., Sahni, A., Morin, G., Zhang, W., Nijnik, A. and Porco, J.A., Jr, Langlais, D., Huang, S., & Pelletier, J., Scientific Reports 2021​, 11, 18156, pp. 1-13. DOI: 10.1038/s41598-021-97765-8

(118) “Eukaryotic Translation Initiation Factor 4AI: A Potential Novel Target in Neuroblastoma,” Skofler,C.; Kleinegger,F.; Krassnig, S.; Birkl-Toeglhofer, A.M.; Singer, G.; Till, H.; Benesc, M.; Cencic, R.; Porco, J. A., Jr.; Pelletier, J.; Castellani, C.; Raicht, A.; Izycka-Swieszewska, E.; Czapiewski, P.; Haybaeck, J. Cells, 2021, 10, 301. DOI: 10.3390/cells10020301

(117) “Fungal-Selective Resorcylate Aminopyrazole Hsp90 Inhibitors: Optimization of Whole-Cell Anticryptococcal Activity and Insights into the Structural Origins of Cryptococcal Selectivity,” Marcyk, P.T.; LeBlanc, E.V.; Kuntz, D.A.; Xue, A.;  Ortiz, F.; Trilles, R.; Bengtson,  B.; Kenney, T.M.G.;  Huang, D.S.; Robbins, N.; Williams, N.S.; Krysan, D.J.; Privé, G.G.; Whitesell, L.;  Cowen, L.E.;  Lauren E Brown, L.E.  J. Med. Chem., 2021, Jan 14. DOI: 10.1021/acs.jmedchem.0c01777

(116) “An oxindole efflux inhibitor potentiates azoles and impairs virulence in the fungal pathogen Candida auris,” Iyer ,K.R.; Camara, K.; Daniel-Ivad ,M.; Trilles, R.; Pimentel-Elardo, S.M.; Fossen, J.L.; Marchillo, K.; Liu, Z.; Singh, S.; Muñoz, J.F.; Kim ,S.H.; Porco, J.A. Jr.; Cuomo, C,A,; Williams, N.S.; Ibrahim, A.S.; Edwards, J.E. Jr.; Andes, D.R.; Nodwell, J.R.; Brown, L.E.; Whitesell, L.; Robbins, N.; Cowen, L.E. Nat. Commun., 2020, 11, 6429. DOI: 10.1038/s41467-020-20183-3

(115) “Heat Shock Factor 1-dependent extracellular matrix remodeling mediates the transition from chronic intestinal inflammation to colon cancer,” Levi-Galibov, O.: Lavon, H.; Wassermann-Dozorets, R.; Pevsner-Fischer, M.; Mayer, S.; Wershof,E,.; Stein, Y.; Brown, L.E.; Zhang, W.; Friedman, G.; Nevo, R.; Golani ,O.; Katz, L.H.;  Yaeger, R.; Laish, I.; Porco, J.A.; Sahai, E.; Shouval, D.S.; Kelsen, D.; Scherz-Shouval, R. Nat. Commun., 2020, 11, 6245. DOI: 10.1038/s41467-020-20054-x

(114) Synthesis and Multiplexed Activity Profiling of Synthetic Acylphloroglucinol Scaffolds. Boyce, J.H.; Reisman, B.; Bachmann, B.O.; Porco, J.A. Jr. ACS Central Science, 2020, Accepted. DOI: 10.1002/anie.202010338

(113) Translation Inhibition by Rocaglates Activates a Species-Specific Cell Death Program in the Emerging Fungal Pathogen Candida auris. Iyer, K. R.; Whitesell, L.; Porco, J.A., Jr.; Henkel, T; Brown, L.E.; Robbins, N.; Cowen, L.E. mBio, 2020, 11, e03329-19. DOI: 10.1128/mBio.03329-19

(112) Rocaglates Induce Gain-of-Function Alterations to eIF4A and eIF4F. Chu, J.; Zhang, W.; Cencic, R.; O’Connor, P.B.F.; Robert, F.; Devine, W.G.; Selznick, A.; Henkel, T.; Merrick, W.C.; Brown, L.E.; Baranov, P.V.; Porco, J.A., Jr.; Pelletier, J. J Cell Reports, 2020, 30, 2481-2488. DOI: 10.1016/j.celrep.2020.02.002

(111) eIF4A supports an oncogenic translation program in pancreatic ductal adenocarcinoma. Chan, K.; Robert, F.; Oertlin, C.; Kapeller-Libermann, D.; Avizonis, D.; Gutierrez, J.; Handly-Santana, A.; Doubrovin, M.; Park, J.; Schoepfer, C.; Da Silva, B.; Yao, M.; Gorton, F.; Shi, J.; Thomas, C.T.; Brown, L.E.; Porco, J.A.; Pollak, M.; Larsson, O.; Pelletier, J.; Chio, I.I.C.  Nat. Commun. 2019, 10, 5151. http://doi.org/10.1038/s41467-019-13086-5

(110) Design and synthesis of fungal-selective resorcylate aminopyrazole Hsp90 inhibitors. Huang, D.; LeBlanc, E.; Shekhar-Guturja, T.; Robbins, N.; Krysan, D.; Pizarro, J.C.; Whitesell, L.; Cowen, L.; Brown, L.E.  J. Med. Chem. 2020, 63, 2139. http://doi.org/10.1021/acs.jmedchem.9b00826

(109) Amidino-Rocaglates – A potent class of eIF4A inhibitors. Chu, J; Zhang, W.; Cencic, R.; Devine, W./G.; Beglov, D.; Henkel, T.; Brown, L.E.; Vadja, S.; Porco, J.A., Jr.; Pelletier, J.  Cell Chemical Biology, 2019, 26 16141-16146.  DOI:10.1016/j.chembiol.2019.08.008

(108) Intercepted Retro-Nazarov Reaction: Syntheses of Amidino-Rocaglate Derivatives and their Biological Evaluation as eIF4A Inhibitors. Zhang, W; Chu, J.; Cyr, A.M.; Yueh, H; Brown, L.E.; Wang, T.T.; Pelletier, J.; Porco, J.A., Jr. J. Am. Chem. Soc., 2019, 141, 12891-12900. DOI:10.1021/jacs.9b06446

(107) Targeting translation initiation by synthetic rocaglates for treating MYC-driven lymphomas. Zhang, X.; Bi, C.; Lu, T.; Zhang W.; Yue, T.; Wang, C.; Tian, T.; Zhang, X.; Huang, Y.; Lunning, M.; Hao, X.; Brown, L.E.; Devine, W.G.; Vose, J.; Porco, J.A., Jr.; Fu, K.  Leukemia, 2019, 34, 138-150. DOI:10.1038/s41375-019-0503-z

(106) Tracing MYC Expression for Small Molecule Discovery. Steinberger, J.; Robert, F.; Hall´e, M.; Williams, D.E.; Cencic, R.; Sawhney, N.; Pelletier, D.; Williams, P.; Igarashi, Y.; Porco, J.A, Jr.; Rodriguez, A.D.;  Kopp, B.; Bachmann, B.; Andersen, R.J.; Pelletier, J. Cell Chemical Biology, 2019, 26, 669-710e6.  DOI: 10.1016/j.chembiol.2019.02.007

(105) Small Molecule Amyloid-β Protein Precursor Processing Modulators Lower Amyloid-β Peptide Levels via cKit Signaling. Chen, C.D.; Zeldich, E.; Khodr, C.; Camara, K.; Tung, T.Y.; Lauder, E.C.; Mullen, P.; Polanco, T.J.; Liu, Y.Y.; Zeldich, D.; Xia, W.; Van Nostrand, W.E.; Brown, L.E.; Porco, J.A.; Abraham, C. J. Alzheimers Dis. 2019, 67, 1089-1106. DOI: 10.3233/JAD-180923

(104) Oxo-aglaiastatin-Mediated Inhibition of Translation Initiation. Maïga. R.I; Cencic, R.; Chu. J.; Waller, D.W.; Brown, L.E.; Devine, W.G.; Zhang, W.; Sebag, M.; Porco, J.A. Jr.; Pelletier, J. Sci. Rep., 2019, 9, 1-12. DOI: 10.1038/s41598-018-37666-5

(103) Structural basis for species-selective targeting of Hsp90 in a pathogenic fungus. Whitesell, L.; Robbins, N.; Huang, D.S.; McLellan, C.A.; Shekhar-Guturja, T.; LeBlanc, E.V.; Nation, C.S.; Hui, R.; Hutchinson, A.; Collins, C.; Chatterjee, S.; Trilles, R.; Xie, J.L.; Krysan, D.J.; Lindquist, S.; Porco, J.A. Jr.; Tatu, U.; Brown, L.E.; Pizarro, J.; Cowen, L.E. Nat. Commun. 2019, 10, 1-17.  DOI: 10.1038/s41467-018-08248-w

(102) Discovery of macrocyclic inhibitors of Apurinic/apyrimidinic endonuclease 1. Trilles, R.; Beglov, D.; Chen, Q.; He, H.; Wireman, R.; Reed, A.; Chennamadhavuni, S.; Panek, J.S.; Brown, L.E.; Vajda, S.; Porco, J.A., Jr.; Kelley, M.R.; Georgiadis, M.M. J. Med. Chem. 2019, 62, 1971-1988. DOI: 10.1021/acs.jmedchem.8b01529

(101) Chemical Synthesis Enables Structural Reengineering of Aglaroxin C Leading to Inhibition Bias for HCV Infection. Zhang, W.; Liu, S.; Maiga, R.I.; Pelletier, J.; Brown, L.E.; Wang, T.T.; Porco, J.A., Jr. J. Am. Chem. Soc., 2019, 141, 1312-1323. DOI: 10.1021/jacs.8b11477

(100) Sensitization of renal carcinoma cells to TRAIL-induced apoptosis by rocaglamide and analogs. Nalli, A. D.; Brown, L. E.; Thomas, C. L.; Sayers, T. J.; Porco, J. A., Jr.; Henrich, C. J. Sci. Rep. 2018, 8, 17519. DOI: 10.1038/s41598-018-35908-0

(99) Diastereodivergent synthesis of chiral tetrahydropyrrolodiazepinediones via a one-pot intramolecular aza-Michael/lactamization sequence. Chennamadhavuni, S.; Panek, J.S.;  Porco, J.A., Jr.; Brown, L.E. J. Org. Chem. 2018, 83, 15449-15462. DOI: 10.1021/acs.joc.8b02724

(98) Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space. Kearney, S.E. et al. ACS Cent. Sci. 2018, 4, 1727-1741. DOI: 10.1021/acscentsci.8b00747

(97)  High Throughput Screening in Larval Zebrafish Identifies Novel Potent Sedative-Hypnotics. Yang, X.; Jounaidi, Y.; Dai, J.B.; Marte-Oquendo, F.; Halpin, E.S.; Brown, L.E.; Trilles, R.; Xu, W.; Daigle, R.; Yu, B.; Schaus, S. E.; Porco, J.A., Jr.; Forman, S.A. Anesthesiology, 2018, 129, 459-476. DOI: 10.1097/ALN.0000000000002281

(96) Rocaglates as dual-targeting agents for experimental cerebral malaria. Langlais, D.; Cencic, R.; Moradin, N.; Kennedy, J. M.; Ayi, K.; Brown, L. E.; Crandall, I.; Tarry, M. J.; Schmeing, M.; Kain, K. C.; Porco, J. A., Jr.; Pelletier, J.; Gros, P. Proc. Natl. Acad. Sci. U S A, 2018, 115, E2366-E2375.  DOI: 10.1073/pnas.1713000115

(95) Dihydropyrimidine-Thiones and Clioquinol Synergize To Target β-Amyloid Cellular Pathologies through a Metal-Dependent Mechanism. Tardiff, D. F.; Brown, L. E.; Yan, X.; Trilles, R.; Jui, N. T.; Barrasa, M. I.; Caldwell, K. A.; Caldwell, G. A.; Schaus, S. E.; Lindquist, S. ACS Chem. Neurosci. 2017, 8, 2039-2055. DOI: 10.1021/acschemneuro.7b00187

(94) A Photochemical Flow Reactor for Large Scale Syntheses of Aglain and Rocaglate Natural Product Analogues. Yueh, H.; Gao, Q., Porco, J. A., Jr.; Beeler, A. B. Bioorg. Med. Chem. 2017, 25, 6197-6202. DOI: 10.1016/j.bmc.2017.06.010

(93)  Inhibiting the oncogenic translation program is an effective therapeutic strategy in multiple myeloma. Manier, S.;Huynh,D.; Shen, Y. J.; Zhou, J.; Yusufzai, T.; Salem, K. Z.; Ebright, R. Y.; Shi, J.; Park, J.; Glavey, S. V.; Devine, W. G.; Liu, C.-J.; Leleu, X.; Quesnel, B.; Roche-Lestienne, C.; Snyder, J. K.; Brown, L. E.; Gray, N.; Bradner, J.; Whitesell, L.; Porco, J. A. Jr.; Ghobrial,I. M. Sci. Transl. Med., 2017, 9, eaal2668. DOI: 10.1126/scitranslmed.aal2668

(92) Development of a Potent and Selective HDAC8 Inhibitor. Ingham, O. J.; Paranal, R. M.; Smith, W. B.; Escobar, R. A.; Yueh, H.; Snyder, T.; Porco, J. A., Jr.; Bradner, J. E.; Beeler, A. B. ACS Med. Chem. Lett. 2016, 7, 929-932. DOI: 10.1021/acsmedchemlett.6b00239

(91) Asymmetric Dearomatization/Cyclization Enables Access to Novel Chemotypes. Hayashi, M.; Brown, L. E.; Porco, J. A., Jr. Eur. J. Org. Chem. 201628, 4800-4804. DOI: 10.1002/ejoc.201601003

(90) Fine-tuning of macrophage activation using synthetic rocaglate derivatives. Bhattacharya, B.; Chatterjee, S; Devine, W.G.; Kobzik, L.; Beeler, A.B.; Porco, J.A., Jr.; Kramnik, I. Sci. Rep. 20166, 24409. DOI: 10.1038/srep24409

(89) A Novel Class of Small Molecule Compounds that Inhibit Hepatitis C Virus Infection by Targeting the Prohibitin-CRaf Pathway. Liu, S.; Wang, W.; Brown, L. E.; Qiu, C.; Lajkiewicz, N.; Zhao, T.; Zhou, J.; Porco, J. A., Jr.; Wang, T. T. EBioMedicine, 2015, 2, 1600-1606. DOI: 10.1016/j.ebiom.2015.09.018

(88) Inhibition of Oncogenic Transcription Factor REL by the Natural Product Derivative Calafianin Monomer 101 Induces Proliferation Arrest and Apoptosis in Human B-Lymphoma Cell Lines. Yeo, A. T.; Chennamadhavuni, S.; Whitty, A.; Porco, J. A., Jr.; Gilmore, T. D. Molecules, 2015, 20, 7474-7494. DOI: 10.3390/molecules20057474

(87) Rapid Synthesis of Polyprenylated Acylphoroglucinol Analogs via Dearomative Conjunctive Allylic Annulation. Grenning, A. J.; Boyce, J. H.; Porco, J. A., Jr. J. Am. Chem. Soc., 2014, 136, 11799-11804. DOI: 10.1021/ja5060302

(86) How proteins bind macrocycles. Villar, E. A.; Beglov, D.; Chennamadhavuni, S.; Porco, J. A., Jr.; Kozakov, D.; Vajda, S.; Whitty, A. Nat. Chem. Bio., 2014, 10, 723-731. DOI: 10.1021/nchembio.1584

(85) Multidimensional Reaction Screening for Photochemical Transformations as a Tool for Discovering New Chemotypes. Martin, V. I.; Goodell, J. R.; Ingham, O. J.; Porco, J. A., Jr.; Beeler, A. B. J. Org. Chem., 2014, 79, 3838-3846. DOI: 10.1021/jo500190b

(84) Total Syntheses of Secalonic Acids A and D. Qin, T.; Porco, J. A., Jr. Angew. Chemie Int. Ed., 2014, 53, 3107-3110. DOI: 10.1002/anie.201311260

(83) Remodeling of Fumagillol: Discovery of an Oxygen-Directed Oxidative Mannich Reaction. Grenning, A. J.; Snyder, J. K.; Porco, J. A., Jr. Org. Lett., 2014, 16, 792-795. DOI: 10.1021/ol4035269

(82) Rhodium(II)-Catalyzed Alkyne Amination of Homopropargylic Sulfamate Esters: Stereoselective Synthesis of Functionalized Norcaradienes by Arene Cyclopropanation. Brawn, R. A.; Zhu, K.; Panek, J. S. Org. Lett., 2014, 16, 74-77. DOI: 10.1021/ol403035g

(81) Tandem Dienone Photorearrangement-Cycloaddition for the Rapid Generation of Molecular Complexity. Bos, P. H.; Antalek, M. T.; Porco, J. A.; Stephenson, C. R. J. J. Am. Chem. Soc., 2013, 135, 17978-17982. DOI: 10.1021/ja409992m

(80) Identification of a broad-spectrum inhibitor of viral RNA synthesis: validation of a prototype virus-based approach.. Filone C. M.; Hodges E. N.; Honeyman B.; Bushkin G. G.; Boyd K.; Platt A.; Ni F.; Strom K.; Hensley L.; Snyder J. K.; Connor J. H. Chem. Biol., 2013, 20, 424-433. DOI: 10.1016/j.chembiol.2013.02.011

(79) Metal-Catalyzed Cascade Rearrangements of 3-Alkynyl Flavone Ethers. Xiong, Y.; Schaus, S. E.; Porco, J. A. Jr., Org. Lett., 2013, 15, 1962-1965. DOI: 10.1021/ol400631b

(78) Enantioselective Addition of Boronates to o-Quinone Methides Catalyzed by Chiral Biphenols. Luan, Y.; Schaus, S.E. J. Am. Chem. Soc., 2012, 134, 19965-19968. DOI: 10.1021/ja309076g

(77) Divergent Synthesis of Functionalized Carbocycles through Organosilane-Directed Asymmetric Alkyne-Alkene Reductive Coupling and Annulation Sequence. Wu, J.; Pu, Y.; Panek, J. S. J. Am. Chem. Soc., 2012, 134, 18440-18446. DOI: 10.1021/ja3083945

(76) Synthesis of Chamaecypanone C Analogues from in Situ-Generated Cyclopentadienones and Their Biological Evaluation. Dong, S.; Qin, T.; Hamel, E.; Beutler, J. A.; Porco, J. A. Jr. J. Am. Chem. Soc., 2012, 134, 19782-19787. DOI: 10.1021/ja3084708

(75) Bifunctional homoallylic carbamates from chiral silane additions to in situ generated N-acyl iminium ions. Wu, J.; Zhu, K.-C.; Yuan, P.-W.; Panek, J. S. Org. Lett., 2012, 14, 3624-3627. DOI: 10.1021/ol301428y

(74) An intramolecular inverse electron demand Diels-Alder approach to annulated a-carbolines. Ma, Z.; Ni, F.; Woo, G.H.C.; Lo, S.-M.; Roveto, P.M.; Schaus, S. E.; Snyder, J.K. Beilstein J. Org. Chem., 2012, 8, 829-840. DOI: 10.3762/bjoc.8.93

(73) Synthesis of a novel chemotype via sequential metal-catalyzed cycloisomerizations. Leng, B.; Chichetti, S.; Su, S.; Beeler, A. B.; Porco, J. A., Jr.; Beilstein J. Org. Chem., 2012, 8, 1338-1343. DOI: 10.3762/bjoc.8.153

(72) Identification of a pyridopyrimidinone inhibitor of orthopoxviruses from a diversity-oriented synthesis library. Dower, K.; Filone, C. M.; Hodges, E. N.; Bjornson, Z. B.; Rubins, K. H.; Brown, L. E.; Schaus, S.; Hensley, L. E.; Connor, J. H. J.Virol., 2012, 86, 2632-2640. DOI: 10.1128/JVI.05416-11

(71) Direct Binding of a Hepatitis C Virus Inhibitor to the Viral Capsid Protein. Kota, S.; Takahashi, V.; Ni, F.; Snyder, J. K.; Strosberg, A. D. PLoS ONE, 2012, 7, e32207. DOI: 10.1371/journal.pone.0032207

(70) Synthesis of Azaphilone-Based Chemical Libraries. Achard, M.; Beeler, A. B.; Porco, J. A., Jr. ACS Comb. Sci., 2012, 14, 236-244. DOI:10.1021/co300002x

(69) Development of a Photochemical Microfluidics Platform. Pimparkar, K.; Yen, B.; Goodell, J. R.; Martin, V. I.; Lee, W.-H.; Porco, J. A., Jr., Beeler, A. B.; Jensen, K. F. Journal of Flow Chemistry, 2011, 1, 53-55. DOI: 10.1556/jfchem.2011.00006

(68) Iron-Catalyzed Rearrangements and Cycloaddition Reactions of 2H-Chromenes. Luan, Y.; Sun, H.; Schaus, S. E. Org. Lett., 2011, 13, 6480-6483. DOI: 10.1021/ol202772k

(67) Remodelling of the Natural Product Fumagillol Employing a Reaction Discovery Approach. Balthaser, B. R.; Maloney, M. C.; Beeler, A. B.; Porco, J. A., Jr; Snyder J. K. Nature Chemistry, 2011, 3, 969-973. DOI: 10.1038/nchem.1178

(66) Synthesis and Reactivity of Bicyclo[3.2.1]octanoid-Derived Cyclopropanes. Goodell, J. R.; Poole, J. L.; Beeler, A. B.; Aube, J.; Porco, J. A. Jr. J. Org. Chem., 2011, 76, 9792-9800. DOI: 10.1021/jo2018922

(65) Microwave-Based Reaction Screening: Tandem Retro-Diels-Alder/Diels-Alder Cycloadditions of o-Quinol Dimers. Dong, S.; Cahill, K. J.; Kang, M.-I.; Colburn, N. H.; Henrich, C. J.; Wilson, J. A.; Beutler, J. A.; Johnson, R. P.; Porco, J. A., Jr. J. Org. Chem., 2011, 76, 8944-8954. DOI: 10.1021/jo201658y

(64) Tandem Visible Light-Mediated Radical Cyclization-Divinylcyclopropane Rearrangement to Tricyclic Pyrrolidinones. Tucker, J. W.; Stephenson, C. R. J. Org. Lett., 2011, 13, 5468-5471. DOI: 10.1021/ol202178t

(63) Truncated Aspidosperma Alkaloid-Like Scaffolds: Unique Structures for the Discovery of New, Bioactive Compounds. Gibeau, A. L.; Snyder, J. K. Heterocycles, 2011, 84, 135-155. DOI: 10.3987/REV-11-SR(P)4

(62) Indium(III)-Catalyzed Hydrative Cyclization of 1,7-Diynyl Ethers. Gibeau, A. L.; Snyder, J. K. Org. Lett., 2011, 13, 4280-4283. DOI: 10.1021/ol201624b

(61) Gold Catalyzed Cyclization of Alkyne-Tethered Dihydropyrimidones. Brown, L. E.; Dai, P.; Porco, J. A., Jr.; Schaus, S. E. Org. Lett., 2011, 13, 4228-4231. DOI: 10.1021/ol2015658

(60) A Cycloisomerization/Friedel-Crafts Alkylation Strategy for the Synthesis of Pyrano[3,4-b]indoles. Medeiros, M. R.; Schaus, S. E.; Porco, J. A., Jr. Org. Lett., 2011, 13, 4012-4015. DOI: 10.1021/ol201532k

(59) Catalytic Diastereoselective Petasis Reactions. Muncipinto, G.; Moquist, P. N.; Schreiber, S. L.; Schaus, S. E. Angew. Chem. Int. Ed., 2011, 50, 8172-8175. DOI: 10.1002/anie.201103271

(58) Sequential Transformations to Access Polycyclic Chemotypes: Asymmetric Crotylation and Metal Carbenoid Reactions. Wu, J.; Becerril, J.; Lian, Y.; Davies, H. M. L.; Porco, J. A., Jr.,; Panek, J. S. Angew. Chem. Int. Ed., 2011, 50, 5938-5942. DOI: 10.1002/anie.201101366

(57) Discovery of New Antimalarial Chemotypes Through Chemical Methodology & Library Development. Brown, L. E.; Cheng, K. C.-C.; Wei, W.-G.; Yuan, P.; Dai, P.; Trilles, R.; Ni, F.; Yuan, J.; MacArthur, R.; Guha, R.; Johnson, R. L.; Su, X.-z.; Dominguez, M. M.; Snyder, J. K.; Beeler, A. B.; Schaus, S. E.; Inglese, J.; Porco, J. A. Jr. Proc. Natl. Acad. Sci. USA, 2011, 108, 6775-6780. DOI: 10.1073/pnas.1017666108

(56) Multicomponent Mannich Reactions with Boron Enolates Derived from Diazo Esters and 9-BBN. Luan, Y.; Schaus, S. E. Org. Lett., 2011, 13, 2510-2513. DOI: 10.1021/ol200766t

(55) Potent Inhibitors of Hepatitis C Core Dimerization as New Leads for Anti-hepatitis C Agents.. Ni, F.; Kota, S.; Takahashi, V.; Strosberg, A.D.; Snyder, J.K. Bioorg. Med. Chem. Lett., 2011, 21, 2198-2202. DOI: 10.1016/j.bmcl.2011.03.014

(54) Core as a Novel Viral Target for Hepatitis C Drugs. Strosberg, A. D.; Kota, S.; Takahashi, V. Snyder, J. K. Viruses, 2010, 2, 1734-1751. DOI: 10.3390/v2081734

(53) Synthesis of Unique Scaffolds via Diels-Alder Cycloadditions of Tetrasubstituted Cyclohexadienes. Jones, A. L.; Snyder, J. K. Org. Lett., 2010, 12, 1592-1595. DOI: 10.1021/ol100318f

(52) A Time-Resolved Fluorescence-Resonance Energy Transfer Assay for Identifying Inhibitors of Hepatitis C Virus Core Dimerization. Kota, S.; Scampavia, L.; Spicer, T.; Beeler, A. B; Takahashi, V.; Snyder, J. K.; Porco, J. A., Jr; Hodder, P.; Strosberg, A. D. Assay Drug Dev. Technol.2010, 8, 96-105. DOI: 10.1089/adt.2009.0217

(51) Skeletal Diversity via Cationic Rearrangements of Substituted Dihydropyrans. Medeiros, M. R.; Narayan, R. S.; McDougal, N. T.; Schaus, S. E.; Porco, J. A., Jr. Org. Lett., 2010, 12, 3222-3225. DOI: 10.1021/ol101144k

(50) Enantioselective Synthesis of 3,4-Chromanediones via Asymmetric Rearrangement of 3-Allyloxyflavones. Marie, J.-C.; Xiong, Y.; Min, G. K.; Yeager, A. R.; Taniguchi, T.; Berova, N.; Schaus, S. E.; Porco, J. A., Jr. J. Org. Chem., 2010, 75, 4584-4590. DOI: 10.1021/jo100889c

(49) Multidimensional Screening and Methodology Development for Condensations Involving Complex 1,2-Diketones. Goodell, J. R.; Leng, B.; Snyder, T. K.; Beeler, A. B; Porco, J. A., Jr. Synthesis, 2010, 13, 2254-2270. DOI: 10.1055/s-0029-1218813

(48) Tandem Processes Identified from Reaction Screening: Nucleophilic Addition to Aryl N-Phosphinylimines Employing La(III)-TFAA Activation. Kinoshita, H.; Ingham, O.J.; Ong, W. W.; Porco, J. A., Jr.; Beeler, A. B; J. Org. Chem., 2010, 132, 6412-6418. DOI: 10.1021/ja100346w

(47) Reaction Discovery Using Microfluidic-Based Multidimensional Screening of Polycyclic Iminium Ethers. Treece, J.L.; Goodell, J.R.; Vander Velde, D. ; Porco, J. A., Jr.; Aube, J. J. Org. Chem., 2010, 75, 2028-2038. DOI: 10.1021/jo100087h

(46) Enantioselective syntheses of candenatenins B and C using a chiral anthracene auxiliary. Jones, A. L.; Liu, X; Snyder, J.K. Tetrahedron Lett., 2010, 51, 1091-1094. DOI: 10.1016/j.tetlet.2009.12.108

(45) Multicomponent Reaction Discovery: Three-Component Synthesis of Spirooxindoles. Liang, B.; Kalidindi, S.; Porco, J. A., Jr.; Stephenson, C. R. J. J. Org. Chem., 2010, 12, 572-575. DOI: 10.1021/ol902764k

(44) New Small Molecule Inhibitors of Hepatitis C Virus. Wei, W.; Cai, C.; Kota, S.; Takahashi, V.; Ni, F.; Strosberg, A. D.; Snyder J. K. Bioorg. Med. Chem. Lett., 2009, 19, 6926-6930. DOI: 10.1016/j.bmcl.2009.10.070

(43) Development of an Automated Microfluidic Reaction Platform for Multidimensional Screening: Reaction Discovery Employing Bicyclo[3.2.1]octanoid Scaffolds. Goodell, J. R.; McMullen, J. P.; Zaborenko, N.; Maloney, J. R.; Ho, C.-X.; Jensen, K. F.; Porco, J. A., Jr.; Beeler, A. B . J. Org. Chem., 2009, 74, 6169-6180. DOI: 10.1021/jo901073v

(42) Stereoselective Synthesis of Spirocyclic Oxindoles via Prins Cyclizations. Castaldi, M. P.; Troast, D.M.; Porco, J. A., Jr. Org. Lett., 2009, 11, 3362-3365. DOI: 10.1021/ol901201k

(41) Stereocontrolled Synthesis of Spirooxindoles through Lewis Acid-Promoted [5 + 2]-Annulation of Chiral Silyl Alcohols. Zhang, Y.; Panek, J. S. Org. Lett., 2009, 11, 3366-3369. DOI: 10.1021/ol901202t

(40) Enantioselective Addition of Boronates to Acyl Imines Catalyzed by Chiral Biphenols. Bishop, J. A.; Lou, S.; Schaus, S. E. Angew. Chem. Int. Ed., 2009, 48, 4337-4340. DOI: 10.1002/anie.200901023

(39) Reaction Discovery Employing Macrocycles: Transannular cyclizations of macrocyclic bis-lactams. Han, C.; Rangarajan, S.; Voukides, A. C.; Beeler, A. B.; Johnson, R.; Porco, J. A., Jr. Jr. Org. Lett., 2009, 11, 413-416. DOI: 10.1021/ol802729f

(38) Intramolecular Rhodium-Catalyzed [2 + 2 + 2] Cyclizations of Diynes with Enones. Jones, A.; Snyder, J. K. J. Org. Chem., 2009, 74, 2907-2910. DOI: 10.1021/jo9001678

(37) Enantioselective Synthesis of (+)-Chamaecypanone C: A Novel Microtubule Inhibitor. Dong, S.; Hamel, E.; Bai, R.; Covell, D. G.; Beutler, J. A.; Porco, J. A., Jr. Angew. Chem. Int. Ed., 2009, 48, 1494-1497. DOI: 10.1002/anie.200805486

(36) Asymmetric Petasis Reactions Catalyzed by Chiral Biphenols. Lou, S.; Schaus, S. E. J. Am. Chem. Soc., 2008, 130, 6922-6923. DOI: 10.1021/ja8018934

(35) Library Synthesis Using 5,6,7,8-Tetrahydro-1,6-naphthyridines as Scaffolds. Zhou, Y.; Beeler, A. B.; Cho, S.; Wang, Y.; Franzblau, S. G.; Snyder, J. K. J. Comb. Chem., 2008, 10, 534-540. DOI: 10.1021/cc800038r

(34) Enantioselective Synthesis of Bicyclo[2.2.2]octenones Using a Copper-Mediated Oxidated Dearomatization/[4+2] Dimerization Cascade. Dong, S.; Zhu, J.; Porco, J. A., Jr. J. Am. Chem. Soc., 2008, 130, 2738-2739. DOI: 10.1021/ja711018z

(33) Organocatalytic asymmetric Mannich reactions. New Methodology, Catalyst Design, and Synthetic Applications. Ting, A.; Schaus, S. E. Eur. J. Org. Chem., 2007, 35, 5797-5815. DOI: 10.1002/ejoc.200700409

(32) Asymmetric Mannich Reaction of Dicarbonyl Compounds with a-Amido Sulfones Catalyzed by Cinchona Alkaloids and Synthesis of Chiral Dihydropyrimidones. Lou, S.; Dai, P.; Schaus, S. E. J. Org. Chem., 200772, 9998-10008. DOI: 10.1021/jo701777g

(31) Preparation of Alkylidene Indane and Related Scaffolds and Their Further Elaboration to Novel Chemotypes. Kesavan, S.; Panek, J. S.; Porco, J. A., Jr. Org. Lett., 2007, 9, 5203-5206. DOI: 10.1021/ol7023778

(30) 1,2-Dihydroisoquinolines as Templates for Cascade Reactions to Access Isoquinoline Alkaloid Frameworks. Su, S.; Porco, J. A., Jr. Org. Lett., 2007, 9, 4983-4986. DOI: 10.1021/ol702176h

(29) Identification of Novel Epoxide Inhibitors of Hepatitis C Virus Replication Using a High-Throughput Screen. Peng, L. F.; Kim, S. S.; Matchacheep, S.; Lei, X.; Su, S.; Lin, W.; Runguphan, W.; Choe, W. H.; Sakamoto, N.; Ikeda, M.; Kato, N.; Beeler, A. B.; Porco, J. A., Jr.; Schreiber, S. L.; Chung, R. T. Antimicrob. Agents Chemother., 2007, 51, 3756-3759. DOI: 10.1128/AAC.00233-07

(28) Nucleophilic Addition to N-Phosphinylimines Via Rare Earth Metal Triflate/Trifluoroacetic Anhydride Activation. Ong, W.W.; Beeler, A.B.; Kesavan, S.; Panek, J. S.; Porco, J. A., Jr. Angew. Chem. Int. Ed., 2007, 46, 7470-7472. DOI: 10.1002/anie.200700694

(27) Skeletal Diversity through Radical Cyclization of Tetrahydropyridine Scaffolds. Dandapani, S.; Duduta, M.; Panek, J. S.; Porco, J. A., Jr. Org. Lett., 2007, 9, 3849-3852. DOI: 10.1021/ol701722z

(26) Synthesis of Pyrrolo-isoquinolines Related to the Lamellarins Using Silver-Catalyzed Cycloisomerizaton/Dipolar Cycloaddition. Su, S.; Porco, J. A., Jr. J. Am. Chem. Soc., 2007, 129, 7744-7745. DOI: 10.1021/ja072737v

(25) 1,2,3,4-Tetrahydro-1,5-naphthyridines and related heterocyclic scaffolds: Exploration of suitable chemistry for library development. Woo, G.H.C.; Beeler, A.B.; Snyder, J.K. Tetrahedron, 2007, 63, 5649-5655. DOI: 10.1016/j.tet.2007.04.003

(24) An Approach to Skeletal Diversity Using Functional Group Pairing of Multifunctional Scaffolds. Comer, E.; Rohan, E.; Deng, L.; Porco, J. A., Jr. Org. Lett., 2007, 9, 2123-2126. DOI: 10.1021/ol070606t

(23) Stereochemical and Skeletal Diversity Employing Pipecolate Ester Scaffolds. Chen, Y.; Porco, J. A., Jr.; Panek, J. S. Org. Lett., 2007, 9, 1529-1532. DOI: 10.1021/ol070321g

(22) Synthesis of Carbamates and Ureas Using Zr(IV)-Catalyzed Exchange Processes. Han, C.; Porco, J. A., Jr. Org. Lett., 2007, 9, 1517-1520. DOI: 10.1021/ol0702728

(21) Synthesis of 5,6,7,8-Tetrahydro-1,6-naphthyridines and Related Heterocycles by Cobalt-Catalyzed [2 + 2 + 2] Cyclizations. Zhou, Y.; Porco, J. A., Jr.; Snyder, J. K. Org. Lett., 2007, 9, 393-396. DOI: 10.1021/ol0625280

(20) Discovery of Chemical Reactions through Multidimensional Screening. Beeler, A. B.; Su, S.; Singleton, C. A.; Porco, J. A., Jr. J. Am. Chem. Soc., 2007, 129, 1413-1419. DOI: 10.1021/ja0674744

(19) Convergent Synthesis of Complex Diketopiperazines Derived from Pipecolic Acid Scaffolds and Parallel Screening against GPCR Targets. Dandapani, S.; Lan, P.; Beeler, A. B.; Beischel, S.; Abbas, A.; Roth, B. L., Porco, J. A., Jr.; Panek, J. S. J. Org. Chem., 2006, 71, 8934-8945. DOI: 10.1021/jo061758p

(18) Asymmetric Allylboration of Ketones Catalyzed by Chiral Diols. Lou, S.; Moquist, P. N.; Schaus, S. E. J. Am. Chem. Soc., 2006, 128, 12660-12661. DOI: 10.1021/ja0651308

(17) Exploring Skeletal Diversity via Ring Contraction of Glycal-Derived Scaffolds. Yeager, A. R.; Min, G. K.; Porco, J. A., Jr.; Schaus, S. E. Org. Lett., 2006, 8, 5065-5068. DOI: 10.1021/ol0618252

(16) Enantioselective Synthesis of Linear Polypropionate Arrays Using Anthracene-Tagged Organosilanes. Kesavan, S.; Su, Q.; Shao, J.; Porco, J. A., Jr.; Panek, J. S. Org. Lett., 2005, 7, 4435-4438. DOI: 10.1021/ol0516723

(15) A new, chiral anthracene for the Diels-Alder/retro-Diels-Alder sequence in lactam and butenolide synthesis. Sanyal, A.; Yuan, Q.; Snyder, J. K. Tetrahedron Lett., 2005, 46, 2475-2478. DOI: 10.1016/j.tetlet.2005.02.046

(14) Chiral Anthracene and Anthrone templates as Stereocontrolling Elements in Diels-Alder/Retro Diels-Alder Sequences. Burgess, K. l.; Corbett, M. S.; Eugenio, P.; Lajkiewicz; N. J.; Liu, X.; Sanyal, A.; Yan, W.; Yuan, Q.; Snyder, J. K. Bioorg, Med. Chem., 2005, 13, 5299-5309. DOI: 10.1016/j.bmc.2005.06.025

(13) Asymmetric Mannich Reactions of beta- Keto Esters with Acyl Imines Catalyzed by Cinchona Alkaloids. Lou, S.; Taoka, M. B.; Ting, A.; Schaus, S. E. J. Am. Chem. Soc., 2005, 127, 11256-11257. DOI: 10.1021/ja0537373

(12) Chemical Library Synthesis Using Convergent Approaches. Beeler, A. B.; Schaus, S. E.; Porco, J. A., Jr. Curr. Opin. Chem. Bio., 2005, 9, 277-284. DOI: 10.1016/j.cbpa.2005.04.005

(11) Synthesis of a Library of Complex Macrodiolides Employing Cyclodimerization of Hydroxy Esters. Beeler, A. B.; Acquilano, D. E.; Su, Q.; Yan, F.; Roth, B. L.; Panek, J. S.; Porco, J. A., Jr. J. Comb. Chem., 2005, 7, 673-681. DOI: 10.1021/cc050064b

(10) Stereocontrolled Synthesis of a Complex Library via Elaboration of Angular Epoxyquinol Scaffolds. Lei, X.; Zaarur, N.; Sherman, M. Y.; Porco, J. A., Jr. J. Org. Chem., 2005, 70, 6474-6483. DOI: 10.1021/jo050956y

(9) Convergent Synthesis of a Complex Oxime Library Using Chemical Domain Shuffling. Su, S.; Acquilano, D. E.; Arumugasamy, J.; Beeler, A. B.; Eastwood, E. L.; Giguere, J. R.; Lan, P.; Lei, X.; Min, G. K.; Yeager, A. R.; Zhou, Y.; Panek, J. S.; Snyder, J. K.; Schaus, S. E.; Porco, J. A., Jr. Org. Lett., 2005, 7, 2751-2754. DOI: 10.1021/ol051023r

(8) Synthesis of a Polymer-Supported Anthracene and Its Application as a Dienophile Scavenger. Lei, X.; Porco, J. A., Jr.; Org. Lett., 2004, 6, 795-798. DOI: 10.1021/ol036502+

(7) Intramolecular Inverse-Electron-Demand Diels-Alder Reactions of Imidazoles with 1,2,4-Triazines : A New Route to 1,2,3,4-Tetrahydro-1,5-naphthyridines and Related Heterocycles. Lahue, R. B.; Lo, S.-M.; Woo, G. H. C.; Snyder, J. K. J. Org. Chem., 2004, 69, 7171- 7182. DOI: 10.1021/jo040193z

(6) Synthesis of Complex Alkoxyamines Using a Polymer-Supported N-Hydroxyphthalimide. Su, S.; Giguere, J. R.; Schaus, S. E.; Porco, J. A., Jr. Tetrahedron, 2004, 60, 8645-8657. DOI: 10.1016/j.tet.2004.05.109

(5) Stereochemical Diversity through Cyclodimerization : Synthesis of Polyketide-like Macrodiolides. Su, Q.; Beeler, A. B.; Lobkovsky, E.; Porco, J. A., Jr.; Panek, J. S. Org. Lett., 2003, 5, 2149-2152. DOI: 10.1021/ol034608z

(4) The Development of a Chromatography-Free Mitsunobu Reaction : Synthesis and Applications of an Anthracene-Tagged Phosphine Reagent. Lan, P.; Porco, J. A., Jr.; South, M. S.; Parlow, J. J. J. Comb. Chem., 2003, 5, 660-669. DOI: 10.1021/cc030028h

(3) Polymer-Assisted Solution-Phase (PASP) Suzuki Couplings Employing an Anthracene-Tagged Palladium Catalyst. Lan, P.; Berta, D.; Porco, J. A., Jr.; South, M. S.; Parlow, J. J. J. Org. Chem., 2003, 68, 9678-9686. DOI: 10.1021/jo035129g

(2) Combinatorial Synthesis of Natural Product-like Molecules Using a First Generation Spiroketal Scaffold. Kulkarni, B. A.; Roth, G. P.; Lobkovsky, E.; Porco, J. A., Jr. J. Comb. Chem., 2002, 4, 56-72. DOI: 10.1021/cc010047w

(1) Parallel Synthesis and Purification using Anthracene-Tagged Substrates. Wang, X.; Parlow, J. J.; Porco, J. A., Jr. Org. Lett., 2000, 2, 3509-3512. DOI: 10.1021/ol202772k