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Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.
Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Huang Q, Kania RS, Kath JC, Lam H, Lam JL, Le PT, Lingardo L, Liu W, McTigue M, Palmer CL, Sach NW, Smeal T, Smith GL, Stewart AE, Timofeevski S, Zhu H, Zhu J, Zou HY, Edwards MP. Johnson TW, et al. Among authors: zhu h, zhu j. J Med Chem. 2014 Jun 12;57(11):4720-44. doi: 10.1021/jm500261q. Epub 2014 Jun 3. J Med Chem. 2014. PMID: 24819116
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: zhu j. 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.
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
Huang Q, Johnson TW, Bailey S, Brooun A, Bunker KD, Burke BJ, Collins MR, Cook AS, Cui JJ, Dack KN, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Johnson PS, Kania RS, Lam H, Lam JL, Le PT, Li Q, Lingardo L, Liu W, Lu MW, McTigue M, Palmer CL, Richardson PF, Sach NW, Shen H, Smeal T, Smith GL, Stewart AE, Timofeevski S, Tsaparikos K, Wang H, Zhu H, Zhu J, Zou HY, Edwards MP. Huang Q, et al. Among authors: zhu h, zhu j. J Med Chem. 2014 Feb 27;57(4):1170-87. doi: 10.1021/jm401805h. Epub 2014 Feb 6. J Med Chem. 2014. PMID: 24432909 Free article.
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: zhu j. 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.
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: zhu j. 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.
Organic chemistry. Strain-release amination.
Gianatassio R, Lopchuk JM, Wang J, Pan CM, Malins LR, Prieto L, Brandt TA, Collins MR, Gallego GM, Sach NW, Spangler JE, Zhu H, Zhu J, Baran PS. Gianatassio R, et al. Among authors: zhu h, zhu j. Science. 2016 Jan 15;351(6270):241-6. doi: 10.1126/science.aad6252. Science. 2016. PMID: 26816372 Free PMC article.
Strain-Release Heteroatom Functionalization: Development, Scope, and Stereospecificity.
Lopchuk JM, Fjelbye K, Kawamata Y, Malins LR, Pan CM, Gianatassio R, Wang J, Prieto L, Bradow J, Brandt TA, Collins MR, Elleraas J, Ewanicki J, Farrell W, Fadeyi OO, Gallego GM, Mousseau JJ, Oliver R, Sach NW, Smith JK, Spangler JE, Zhu H, Zhu J, Baran PS. Lopchuk JM, et al. Among authors: zhu h, zhu j. J Am Chem Soc. 2017 Mar 1;139(8):3209-3226. doi: 10.1021/jacs.6b13229. Epub 2017 Feb 20. J Am Chem Soc. 2017. PMID: 28140573 Free PMC article.
Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497).
Kung PP, Bingham P, Brooun A, Collins M, Deng YL, Dinh D, Fan C, Gajiwala KS, Grantner R, Gukasyan HJ, Hu W, Huang B, Kania R, Kephart SE, Krivacic C, Kumpf RA, Khamphavong P, Kraus M, Liu W, Maegley KA, Nguyen L, Ren S, Richter D, Rollins RA, Sach N, Sharma S, Sherrill J, Spangler J, Stewart AE, Sutton S, Uryu S, Verhelle D, Wang H, Wang S, Wythes M, Xin S, Yamazaki S, Zhu H, Zhu J, Zehnder L, Edwards M. Kung PP, et al. Among authors: zhu h, zhu j. J Med Chem. 2018 Feb 8;61(3):650-665. doi: 10.1021/acs.jmedchem.7b01375. Epub 2017 Dec 27. J Med Chem. 2018. PMID: 29211475
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