ACS National Meeting - San Francisco 2017

253rd American Chemical Society National Meeting & Expo

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288-TECH TECHNICAL PROGRAM ‡ Cooperative Cosponsorship MEDI 9:30 MEDI 350. Discovery of a novel class of potent, selective, and orally bioavail- able histone methyltransferase Enhancer of Zeste Homolog 2 (EZH2) inhibitors and the identification of development candidate PF-06821497. P. Kung, S. Bergqvist, P. Bingham, J.F. Braganza, A. Brooun, M.R. Collins, W. Diehl, Y. Deng, D. Dinh, C. Fan, V.R. Fantin, H.J. Gukasyan, W. Hu, B. Huang, R. Kania, W. Liu, S. Kephart, M. Kraus, C. Krivacic, R.A. Kumpf, G. Li, K. Maegley, I.J. McAlpine, L. Nguyen, S. Ninkovic, M.A. Ornelas, D. Richter, E. Rui, M. Ryskin, S.A. Scales, J. Spangler, A. Stewart, S.C. Sutton, J. Tatlock, C. Tsao, D. Verhelle, F. Wang, H. Wang, P. Wells, M. Wythes, S. Yamazaki, B. Yip, X. Yu, L. Zehnder, W. Zhang, P. Zhu, J. Zhu, R.A. Rollins, S. Sharma, M.P. Edwards 10:00 MEDI 351. Discovery and devel- opment of BLU-554: A potent, highly selective covalent inhibitor of Fibroblast Growth Factor Receptor 4 (FGFR4) in development for the targeted treatment of advanced Hepatocellular Carcinoma (HCC) patients with amplified and overexpressed FGF19. C.V. Miduturu, M. Hagel, M. Sheets, N. Rubin, W. Weng, N. Bifulco, L.V. Dipietro, J. Kim, N. Brooijmans, B.L. Hodous, N. Stransky, K. Hoeflich, V.J. Kadambi, N. Kohl, C. Lengauer, T. Guzi 10:30 MEDI 352. Discovery of PRN1371: A highly selective, irreversible inhibitor of FGFR1-4 in clinical development for the treatment of solid tumors. K.A. Brameld 11:00 MEDI 353. FGF401: A revers- ible-covalent inhibitor of FGFR4 for the treatment of hepatocellular carcinoma. R.A. Fairhurst, T. Knoepfel, P. Furet, N. Buschmann, C. Leblanc, R. Mah, M. Kiffe, D. Graus-Porta, A. Weiss, J. Kinyamu-Akunda, M. Wartmann, J. Trappe, T. Gabriel, F. Hofmann, W. Sellers 11:30 MEDI 354. Interdiction at a protein-protein interface: Structure- based design of the Mcl-1 inhib- itor AMG 176. S.P. Brown Section B Moscone Center 3006/3008 Targeting Epigenetic Writers & Erasers J. Jin, Organizer, Presiding 8:30 Introductory Remarks. 8:35 MEDI 355. Probing the epigenome for therapeutic targets. C.H. Arrowsmith 9:05 MEDI 356. Tazemetostat, a first-in- class inhibitor of EZH2: From bench to bedside to bench. R. Copeland 9:35 MEDI 357. Sirtuin inhibitors as promising anticancer agents. H. Lin 10:05 Intermission. 10:20 MEDI 358. Targeting histone lysine methylation regulatory pathways in cancer. P. Trojer 10:50 MEDI 359. Exploring novel models of interaction to inhibit protein methyltransferases. M. Luo 11:20 MEDI 360. Chemical probes targeting the protein arginine deiminases. P.R. Thompson 11:50 Concluding Remarks. WEDNESDAY AFTERNOON Section A Moscone Center Gateway Ballroom 103/104 First Time Disclosures J. B. Schwarz, Organizer, Presiding 1:30 MEDI 361. Discovery of clinical candidate PF-06648671: A potent, highly brain penetrant gamma secretase mod- ulator for the treatment of Alzheimer's disease. M. Pettersson, C. am Ende, T.W. Butler, P.H. Dorff, I.V. Efremov, E. Evrard, S.A. Eisenbeis, C.J. Helal, M.E. Green, J.M. Humphrey, G.W. Kauffman, P.B. Mullins, C.J. O'Donnell, D.A. Rankic, A.F. Stepan, C.M. Stiff, N. Patel, C. Subramanyam, T.P. Tran, E.X. Yang, L. Xie, K.R. Bales, E. Hajos- Korcsok, B.A. Pettersen, L.R. Pustilnik, S.J. Steyn, K.M. Wood, R. Qiu, P.R. Verhoest 2:00 MEDI 362. Discovery of a small molecule αvβ6 inhibitor for idiopathic pulmonary fibrosis. S.J. MacDonald, J. Pritchard, N. Anderson 2:30 MEDI 363. Identification of AZD9567, an anti-inflammatory glucocorticoid receptor modu- lator with improved side effect profile. L. Ripa, M. Dearman, G. Edenro, K. Edman, R. Hendrickx, M. Lepistö, L. Öberg 3:00 MEDI 364. Discovery and early clinical profile of a non-catchol dopamine 1 receptor agonist. D.L. Gray, R. Kozak, S. Mente, J.E. Davoren, D. Nason, S. ONeil, I.V. Efremov, A. Harris, R. O'Connor, M. Salafia 3:30 MEDI 365. Discovery and devel- opment of BLU-285: A potent, highly selective inhibitor of KIT and PDGFRα activation loop mutants. B.L. Hodous, E. Evans, A. Gardino, A. Davis, J. Zhu, D.P. Wilson, K. Wilson, L.V. Dipietro, J. Kim, N. Brooijmans, V.J. Kadambi, A. Shutes, Y. Zhang, N. Kohl, C. Lengauer, T. Guzi 4:00 MEDI 366. NVP-LXS196, a novel PKC inhibitor for the treatment of uveal melanoma. M. Visser, J.P. Papillon, J. Fan, M. Luzzio, W. Michael, R. Wang, A. Zhang, C. Straub, S. Mathieu, M. Kato, M.G. Palermo, C. Chen, M.J. LaMarche, T.M. Ramsey, A. Vattay, R. Guo, V. Cooke, A. Bric, F. Chung, G. Liang, M. Romanowski, A. Wylie 4:30 MEDI 367. Discovery of selonsertib (GS-4997): A first in class, selective inhibitor of apoptosis signal-regu- lating kinase 1. G.T. Notte, B. Corkey, E. Lansdon, D. Breckenridge, O.L. Saunders, M. Graupe, B. Murray, C. Venkataramani, J. Guerrero, J. Farand, J.A. Zablocki, K. Babaoglu, J. Liles, G. Budas, S. Wise, K. Koch, L. Castonguay, M.C. Desai 5:00 MEDI 368. Discovery of a selective inhibitor of indoleamine-2,3-dioxygenase for use in the therapy of cancer. A. Balog Section B Moscone Center 3006/3008 General Orals A. W. Stamford, Organizer J. Ramanjulu, Presiding 1:30 MEDI 369. Teaching old drugs new tricks: Reprogramming ethionamide's bioactivation to fight multidrug resistant Mycobacterium tuberculosis. N. Willand, M. Gitzinger, B. Deprez, A. Baulard 1:50 MEDI 370. Preclinical development and characterization of MYC inhib- itors. N. Jacob, P. Miranda, P. Serrano Navarro, J. Hart, P.K. Vogt, K.D. Janda 2:10 MEDI 371. Discovery of PF-06748962: A potent and selective lactam-based EP3 antagonist. K. Futatsugi 2:30 MEDI 372. Novel pyrrolomy- cins as potent antibacterial agents against ESKAPE pathogens and biofilms. R. Li, Z. Yang, J. Ahn, Y. Liu, Y. Chhonker, D. Murry, H.A. Zhong, K. Bayles 2:50 MEDI 373. Development and appli- cation of an NMR-based activity and inhibition assay for mycobacterial isoci- trate lyase. R.P. Bhusal, K. Patel, B. Kwai, G. Bashiri, J. Reynisson, J. Sperry, I.K. Leung 3:10 MEDI 374. LEGO ® -inspired drug design: Discovery of novel fungal Plasma membrane H + -ATPase (Pma1) inhibitors from small molecule libraries: An introduction of HFSA-SBS_DOS-RD strategy in drug discovery. T. Tung, T. Dao, M.B. Palmgren, A.T. Fuglsang, S.B. Christensen, J. Nielsen 3:30 MEDI 375. Reducing cycle time in medicinal chemistry drug dis- covery. J.S. Wai, T. Wang 3:50 MEDI 376. Enzymatic tandem carboxylation-amidation as a bio- activity-potentiating strategy in the production of natural and unnatural thiolactomycin antibiotics. J. Li, X. Tang, S. Mckinnie, T. Awakawa, B.S. Moore 4:10 MEDI 377. Structure-based design of highly potent small-molecule inhibi- tors of DCN1-UBC12 protein-protein interaction. H. Zhou, J. Lu, L. Liu, D. Bernard, J. Stuckey, Y. Sun, S. Wang 4:30 MEDI 378. CDK8 inhibitors with long residence time emerging from a retro-design approach: New opportunities for cancer treatment. J.C. Benningshof, B. Aerts, G. Müller, J. Veerman, E. Damen, M. Kubbutat, J. Ehlert, H. Holger, F. Totzke 4:50 MEDI 379. Structure-based design, synthesis, biological eval- uation, and x-ray crystallographic analysis of novel, highly potent HIV-1 protease inhibitors to address multi-drug resistant HIV. A.K. Ghosh, H.L. Osswald, J. Agniswamy, Y. Wang, I. Weber, M. Amano, H. Mitsuya WEDNESDAY EVENING Section A Moscone Center West Hall General Posters A. W. Stamford, Organizer 7:00 - 9:00 MEDI 380. Inhibition of Aβ-40 and Aβ-42 aggregation by piceatannol and cis-piceatan- nol. J.M. Chapman, M. Moss, Y. Wang MEDI 381. Photoelectrocatalytic inhibition of Alzheimer's β-amyloid aggrega- tion in vitro by hole-derived radi- cals. K. Kim, B. Lee, Y. Chung, W. Choi MEDI 382. Synthesis of Yakuchinone- derived compounds that inhibit β-amyloid aggregation. L. Chen, C. Yen, H. Tseng, Y. Huang, Y. Lu, W. Hou, K. Hsu, I. Pan, K. Huang, W. Huang MEDI 383. Photoexcited ruthenium complex for highly sensitive inhibi- tion of β-amyloidogenesis. G. Son, C. Park, B. Lee, Y. Chung MEDI 384. New hydroxyquinoline-based derivatives as potent modulators of amyloid-b aggregations. M. Hu MEDI 385. Potential multimechanistic therapeutic effects of dihydropyridine calcium channel blockers: Mechanistic study of effects on amyloid-beta aggregation associated with Alzheimer's disease. J.M. Chapman, M. Moss, J. Tseng MEDI 386. Withdrawn. MEDI 387. Development of MBRI-001, a deuterium-substituted plinabulin, as a potent anti-microtubule agent for anticancer. Z. Ding, H. Cheng, S. Wang, Y. Hou, J. Zhao, H. Guan, W. Li MEDI 388. β-Sheet propensity of com- petitive peptide inhibitor's residue is crucial in binding to proteases: PACE4 inhibitors as a case study. V. Dianati, A. Shamloo, A. Kwiatkowska, R. Desjardins, A. Soldera, R. Day, Y. Dory MEDI 389. Hepsin-targeted ligands for prostate cancer imaging and therapy. Y. Byun, S. Son, H. Kwon MEDI 390. X-ray crystallographic structures of teixobactin analogues. H. Yang, D.R. Du Bois, J.W. Ziller, J.S. Nowick MEDI 391. Withdrawn. MEDI 392. Long wavelength, orthogonal release of internalized anti-inflammatory compounds from cellular vehi- cles. R.M. Hughes, C. Marvin, Z. Rodgers, S. Ding, N. Oien, W.J. Smith, D.S. Lawrence MEDI 393. Amino acid and peptide conjugates are potential drug candidates. S.S. Panda MEDI 394. Withdrawn. MEDI 395. Directed immune responses via covalently linked TLR agonist combina- tions for a Q-fever vaccine. T.J. Albin, J. Tom, S. Manna, A. Gilkes, A. Jain, M. Supnet, H. Davies, A. Nalca, A. Burkhardt, P. Felgner, A.P. Esser-Kahn MEDI 396. Development of anti- dotes against nerve agent inhibited acetylcholinesterase – the transfor- mation of an inhibitor into a reactiva- tor. C. Lindgren, N. Forsgren, C. Akfur, L. Berg, D. Andersson, M. Hillgren, W. Qian, F. Worek, F. Ekström, A. Linusson MEDI 397. Generating site-specific antibody-drug conjugates with high drug to antibody ratios using a tandem Knoevenagel dondensation-Mi- chael addition. R. Kudirka, R. Barfield, J. McFarland, P. Drake, A. Carlson, S. Banas, W. Zmolek, A. Garofalo, D. Rabuka MEDI 398. Synthesis of truncated tirandamycin A-D derivatives as new antihelminthic agents. T. Jimenez, M. Grotli, C. Wallentin MEDI 399. Beyond IC50 and simple PK models – considerations for dis- covery chemists. R. Fraczkiewicz, M.B. Bolger, W. Woltosz MEDI 400. Synthesis and evaluation of anti- tubercular agents 2-aminothiophenes and benzo-1,2-selenazol-3(2H)-ones targeting Pks13 and Ag85C respectively. S. Thanna, S.E. Knudson, C.M. Goins, F. Salem, S. Kapil, A. Grzegorzewicz, M. Jackson, D.R. Ronning, R.A. Slayden, S.J. Sucheck

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