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Page 1
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.
Cheng H, Nair SK, Murray BW, Almaden C, Bailey S, Baxi S, Behenna D, Cho-Schultz S, Dalvie D, Dinh DM, Edwards MP, Feng JL, Ferre RA, Gajiwala KS, Hemkens MD, Jackson-Fisher A, Jalaie M, Johnson TO, Kania RS, Kephart S, Lafontaine J, Lunney B, Liu KK, Liu Z, Matthews J, Nagata A, Niessen S, Ornelas MA, Orr ST, Pairish M, Planken S, Ren S, Richter D, Ryan K, Sach N, Shen H, Smeal T, Solowiej J, Sutton S, Tran K, Tseng E, Vernier W, Walls M, Wang S, Weinrich SL, Xin S, Xu H, Yin MJ, Zientek M, Zhou R, Kath JC. Cheng H, et al. Among authors: yin mj. J Med Chem. 2016 Mar 10;59(5):2005-24. doi: 10.1021/acs.jmedchem.5b01633. Epub 2016 Jan 28. J Med Chem. 2016. PMID: 26756222
Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).
Murphy ST, Alton G, Bailey S, Baxi SM, Burke BJ, Chappie TA, Ermolieff J, Ferre R, Greasley S, Hickey M, Humphrey J, Kablaoui N, Kath J, Kazmirski S, Kraus M, Kupchinsky S, Li J, Lingardo L, Marx MA, Richter D, Tanis SP, Tran K, Vernier W, Xie Z, Yin MJ, Yu XH. Murphy ST, et al. Among authors: yin mj. J Med Chem. 2011 Dec 22;54(24):8490-500. doi: 10.1021/jm201019k. Epub 2011 Nov 23. J Med Chem. 2011. PMID: 22040023
Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design.
Cheng H, Li C, Bailey S, Baxi SM, Goulet L, Guo L, Hoffman J, Jiang Y, Johnson TO, Johnson TW, Knighton DR, Li J, Liu KK, Liu Z, Marx MA, Walls M, Wells PA, Yin MJ, Zhu J, Zientek M. Cheng H, et al. Among authors: yin mj. ACS Med Chem Lett. 2012 Nov 7;4(1):91-7. doi: 10.1021/ml300309h. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900568 Free PMC article.
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide.
Zehnder L, Bennett M, Meng J, Huang B, Ninkovic S, Wang F, Braganza J, Tatlock J, Jewell T, Zhou JZ, Burke B, Wang J, Maegley K, Mehta PP, Yin MJ, Gajiwala KS, Hickey MJ, Yamazaki S, Smith E, Kang P, Sistla A, Dovalsantos E, Gehring MR, Kania R, Wythes M, Kung PP. Zehnder L, et al. Among authors: yin mj. J Med Chem. 2011 May 12;54(9):3368-85. doi: 10.1021/jm200128m. Epub 2011 Apr 20. J Med Chem. 2011. PMID: 21438541
Targeting 3-phosphoinoside-dependent kinase-1 to inhibit insulin-like growth factor-I induced AKT and p70 S6 kinase activation in breast cancer cells.
Baxi SM, Tan W, Murphy ST, Smeal T, Yin MJ. Baxi SM, et al. Among authors: yin mj. PLoS One. 2012;7(10):e48402. doi: 10.1371/journal.pone.0048402. Epub 2012 Oct 31. PLoS One. 2012. Retraction in: PLoS One. 2017 Apr 10;12(4):e0175772. doi: 10.1371/journal.pone.0175772 PMID: 23119004 Free PMC article. Retracted.
Targeting the mTOR pathway in tumor malignancy.
Cheng H, Walls M, Baxi SM, Yin MJ. Cheng H, et al. Among authors: yin mj. Curr Cancer Drug Targets. 2013 Mar;13(3):267-77. doi: 10.2174/1568009611313030005. Curr Cancer Drug Targets. 2013. PMID: 23297825 Review.
Targeting small cell lung cancer harboring PIK3CA mutation with a selective oral PI3K inhibitor PF-4989216.
Walls M, Baxi SM, Mehta PP, Liu KK, Zhu J, Estrella H, Li C, Zientek M, Zong Q, Smeal T, Yin MJ. Walls M, et al. Among authors: yin mj. Clin Cancer Res. 2014 Feb 1;20(3):631-43. doi: 10.1158/1078-0432.CCR-13-1663. Epub 2013 Nov 15. Clin Cancer Res. 2014. Retraction in: Clin Cancer Res. 2017 Aug 1;23(15):4523. doi: 10.1158/1078-0432.CCR-17-1502 PMID: 24240111 Retracted.
Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity.
Liu KK, Zhu J, Smith GL, Yin MJ, Bailey S, Chen JH, Hu Q, Huang Q, Li C, Li QJ, Marx MA, Paderes G, Richardson PF, Sach NW, Walls M, Wells PA, Baxi S, Zou A. Liu KK, et al. Among authors: yin mj. ACS Med Chem Lett. 2011 Sep 19;2(11):809-13. doi: 10.1021/ml200126j. eCollection 2011 Nov 10. ACS Med Chem Lett. 2011. PMID: 24900269 Free PMC article.
97 results