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Page 1
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: collins mr. J Med Chem. 2014 Jun 12;57(11):4720-44. doi: 10.1021/jm500261q. Epub 2014 Jun 3. J Med Chem. 2014. PMID: 24819116
Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.
Kung PP, Funk L, Meng J, Collins M, Zhou JZ, Johnson MC, Ekker A, Wang J, Mehta P, Yin MJ, Rodgers C, Davies JF 2nd, Bayman E, Smeal T, Maegley KA, Gehring MR. Kung PP, et al. Among authors: collins m. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6273-8. doi: 10.1016/j.bmcl.2008.09.081. Epub 2008 Sep 26. Bioorg Med Chem Lett. 2008. PMID: 18929486
Practical and innate carbon-hydrogen functionalization of heterocycles.
Fujiwara Y, Dixon JA, O'Hara F, Funder ED, Dixon DD, Rodriguez RA, Baxter RD, Herlé B, Sach N, Collins MR, Ishihara Y, Baran PS. Fujiwara Y, et al. Among authors: collins mr. Nature. 2012 Dec 6;492(7427):95-9. doi: 10.1038/nature11680. Epub 2012 Nov 28. Nature. 2012. PMID: 23201691 Free PMC article.
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: collins mr. 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.
A simple litmus test for aldehyde oxidase metabolism of heteroarenes.
O'Hara F, Burns AC, Collins MR, Dalvie D, Ornelas MA, Vaz AD, Fujiwara Y, Baran PS. O'Hara F, et al. Among authors: collins mr. J Med Chem. 2014 Feb 27;57(4):1616-20. doi: 10.1021/jm4017976. Epub 2014 Feb 5. J Med Chem. 2014. PMID: 24472070 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: collins mr. Science. 2016 Jan 15;351(6270):241-6. doi: 10.1126/science.aad6252. Science. 2016. PMID: 26816372 Free PMC article.
Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.
Kung PP, Rui E, Bergqvist S, Bingham P, Braganza J, Collins M, Cui M, Diehl W, Dinh D, Fan C, Fantin VR, Gukasyan HJ, Hu W, Huang B, Kephart S, Krivacic C, Kumpf RA, Li G, Maegley KA, McAlpine I, Nguyen L, Ninkovic S, Ornelas M, Ryskin M, Scales S, Sutton S, Tatlock J, Verhelle D, Wang F, Wells P, Wythes M, Yamazaki S, Yip B, Yu X, Zehnder L, Zhang WG, Rollins RA, Edwards M. Kung PP, et al. J Med Chem. 2016 Sep 22;59(18):8306-25. doi: 10.1021/acs.jmedchem.6b00515. Epub 2016 Sep 6. J Med Chem. 2016. PMID: 27512831
Correction to Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.
Kung PP, Rui E, Bergqvist S, Bingham P, Braganza J, Collins M, Cui M, Diehl W, Dinh D, Fan C, Fantin VR, Gukasyan HJ, Hu W, Huang B, Kephart S, Krivacic C, Kumpf RA, Li G, Maegley KA, McAlpine I, Nguyen L, Ninkovic S, Ornelas M, Ryskin M, Scales S, Sutton S, Tatlock J, Verhelle D, Wang F, Wells P, Wythes M, Yamazaki S, Yip B, Yu X, Zehnder L, Zhang WG, Rollins RA, Edwards M. Kung PP, et al. J Med Chem. 2016 Dec 22;59(24):11196. doi: 10.1021/acs.jmedchem.6b01747. Epub 2016 Dec 12. J Med Chem. 2016. PMID: 27936698 No abstract available.
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: collins mr. 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.
61 results