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Page 1
Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor.
Cho YS, Levell JR, Liu G, Caferro T, Sutton J, Shafer CM, Costales A, Manning JR, Zhao Q, Sendzik M, Shultz M, Chenail G, Dooley J, Villalba B, Farsidjani A, Chen J, Kulathila R, Xie X, Dodd S, Gould T, Liang G, Heimbach T, Slocum K, Firestone B, Pu M, Pagliarini R, Growney JD. Cho YS, et al. Among authors: costales a. ACS Med Chem Lett. 2017 Sep 18;8(10):1116-1121. doi: 10.1021/acsmedchemlett.7b00342. eCollection 2017 Oct 12. ACS Med Chem Lett. 2017. PMID: 29057061 Free PMC article.
Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors.
Zhao Q, Manning JR, Sutton J, Costales A, Sendzik M, Shafer CM, Levell JR, Liu G, Caferro T, Cho YS, Palermo M, Chenail G, Dooley J, Villalba B, Farsidjani A, Chen J, Dodd S, Gould T, Liang G, Slocum K, Pu M, Firestone B, Growney J, Heimbach T, Pagliarini R. Zhao Q, et al. Among authors: costales a. ACS Med Chem Lett. 2018 Jun 11;9(7):746-751. doi: 10.1021/acsmedchemlett.8b00182. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034612 Free PMC article.
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.
Williams TE, Subramanian S, Verhagen J, McBride CM, Costales A, Sung L, Antonios-McCrea W, McKenna M, Louie AK, Ramurthy S, Levine B, Shafer CM, Machajewski T, Renhowe PA, Appleton BA, Amiri P, Chou J, Stuart D, Aardalen K, Poon D. Williams TE, et al. Among authors: costales a. ACS Med Chem Lett. 2015 Aug 3;6(9):961-5. doi: 10.1021/ml500526p. eCollection 2015 Sep 10. ACS Med Chem Lett. 2015. PMID: 26396681 Free PMC article.
Discovery of Potent and Selective RSK Inhibitors as Biological Probes.
Jain R, Mathur M, Lan J, Costales A, Atallah G, Ramurthy S, Subramanian S, Setti L, Feucht P, Warne B, Doyle L, Basham S, Jefferson AB, Lindvall M, Appleton BA, Shafer CM. Jain R, et al. Among authors: costales a. J Med Chem. 2015 Sep 10;58(17):6766-83. doi: 10.1021/acs.jmedchem.5b00450. Epub 2015 Aug 13. J Med Chem. 2015. PMID: 26270416
Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990.
McBride CM, Levine B, Xia Y, Bellamacina C, Machajewski T, Gao Z, Renhowe P, Antonios-McCrea W, Barsanti P, Brinner K, Costales A, Doughan B, Lin X, Louie A, McKenna M, Mendenhall K, Poon D, Rico A, Wang M, Williams TE, Abrams T, Fong S, Hendrickson T, Lei D, Lin J, Menezes D, Pryer N, Taverna P, Xu Y, Zhou Y, Shafer CM. McBride CM, et al. Among authors: costales a. J Med Chem. 2014 Nov 13;57(21):9124-9. doi: 10.1021/jm501107q. Epub 2014 Nov 4. J Med Chem. 2014. PMID: 25368984
Design and synthesis of potent RSK inhibitors.
Jain R, Mathur M, Lan J, Costales A, Atallah G, Ramurthy S, Subramanian S, Setti L, Feucht P, Warne B, Doyle L, Basham S, Jefferson AB, Appleton BA, Lindvall M, Shafer CM. Jain R, et al. Among authors: costales a. Bioorg Med Chem Lett. 2018 Oct 15;28(19):3197-3201. doi: 10.1016/j.bmcl.2018.08.020. Epub 2018 Aug 21. Bioorg Med Chem Lett. 2018. PMID: 30170943
Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors.
Ramurthy S, Subramanian S, Aikawa M, Amiri P, Costales A, Dove J, Fong S, Jansen JM, Levine B, Ma S, McBride CM, Michaelian J, Pick T, Poon DJ, Girish S, Shafer CM, Stuart D, Sung L, Renhowe PA. Ramurthy S, et al. Among authors: costales a. J Med Chem. 2008 Nov 27;51(22):7049-52. doi: 10.1021/jm801050k. J Med Chem. 2008. PMID: 18942827
79 results