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Page 1
Sulfonylated Benzothiazoles as Inhibitors of Endothelial Lipase.
Johnson JA, Tora G, Pi Z, Phillips M, Yin X, Yang R, Zhao L, Chen AY, Taylor DS, Basso M, Rose A, Behnia K, Onorato J, Chen XQ, Abell LM, Lu H, Locke G, Caporuscio C, Galella M, Adam LP, Gordon D, Wexler RR, Finlay HJ. Johnson JA, et al. Among authors: galella m. ACS Med Chem Lett. 2018 Nov 21;9(12):1263-1268. doi: 10.1021/acsmedchemlett.8b00424. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613337 Free PMC article.
Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).
Watterson SH, Langevine CM, Van Kirk K, Kempson J, Guo J, Spergel SH, Das J, Moquin RV, Dyckman AJ, Nirschl D, Gregor K, Pattoli MA, Yang X, McIntyre KW, Yang G, Galella MA, Booth-Lute H, Chen L, Yang Z, Wang-Iverson D, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ. Watterson SH, et al. Among authors: galella ma. Bioorg Med Chem Lett. 2011 Dec 1;21(23):7006-12. doi: 10.1016/j.bmcl.2011.09.111. Epub 2011 Oct 5. Bioorg Med Chem Lett. 2011. PMID: 22018461
Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors.
Harikrishnan LS, Finlay HJ, Qiao JX, Kamau MG, Jiang J, Wang TC, Li J, Cooper CB, Poss MA, Adam LP, Taylor DS, Chen AY, Yin X, Sleph PG, Yang RZ, Sitkoff DF, Galella MA, Nirschl DS, Van Kirk K, Miller AV, Huang CS, Chang M, Chen XQ, Salvati ME, Wexler RR, Lawrence RM. Harikrishnan LS, et al. Among authors: galella ma. J Med Chem. 2012 Jul 12;55(13):6162-75. doi: 10.1021/jm300611v. Epub 2012 Jun 22. J Med Chem. 2012. PMID: 22650305
Improving the pharmacokinetic and CYP inhibition profiles of azaxanthene-based glucocorticoid receptor modulators-identification of (S)-5-(2-(9-fluoro-2-(4-(2-hydroxypropan-2-yl)phenyl)-5H-chromeno[2,3-b]pyridin-5-yl)-2-methylpropanamido)-N-(tetrahydro-2H-pyran-4-yl)-1,3,4-thiadiazole-2-carboxamide (BMS-341).
Yang MG, Dhar TG, Xiao Z, Xiao HY, Duan JJ, Jiang B, Galella MA, Cunningham M, Wang J, Habte S, Shuster D, McIntyre KW, Carman J, Holloway DA, Somerville JE, Nadler SG, Salter-Cid L, Barrish JC, Weinstein DS. Yang MG, et al. Among authors: galella ma. J Med Chem. 2015 May 28;58(10):4278-90. doi: 10.1021/acs.jmedchem.5b00257. Epub 2015 May 7. J Med Chem. 2015. PMID: 25905990
Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).
Gilmore JL, Sheppeck JE 2nd, Watterson SH, Haque L, Mukhopadhyay P, Tebben AJ, Galella MA, Shen DR, Yarde M, Cvijic ME, Borowski V, Gillooly K, Taylor T, McIntyre KW, Warrack B, Levesque PC, Li JP, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, Barrish JC, Pitts WJ, Carter PH, Xie J, Dyckman AJ. Gilmore JL, et al. Among authors: galella ma. J Med Chem. 2016 Jul 14;59(13):6248-64. doi: 10.1021/acs.jmedchem.6b00373. Epub 2016 Jul 1. J Med Chem. 2016. PMID: 27309907
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.
Watterson SH, De Lucca GV, Shi Q, Langevine CM, Liu Q, Batt DG, Beaudoin Bertrand M, Gong H, Dai J, Yip S, Li P, Sun D, Wu DR, Wang C, Zhang Y, Traeger SC, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Zhang Y, Heimrich E, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Galella MA, Tebben AJ, Muckelbauer JK, Chang C, Rampulla R, Mathur A, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA. Watterson SH, et al. Among authors: galella ma. J Med Chem. 2016 Oct 13;59(19):9173-9200. doi: 10.1021/acs.jmedchem.6b01088. Epub 2016 Sep 19. J Med Chem. 2016. PMID: 27583770
[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.
Shan W, Balog A, Nation A, Zhu X, Chen J, Cvijic ME, Geng J, Rizzo CA, Spires T Jr, Attar RM, Obermeier M, Traeger S, Dai J, Zhang Y, Galella M, Trainor G, Vite GD, Gavai AV. Shan W, et al. Among authors: galella m. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5707-5711. doi: 10.1016/j.bmcl.2016.10.059. Epub 2016 Oct 21. Bioorg Med Chem Lett. 2016. PMID: 27836399
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Gong H, Weinstein DS, Lu Z, Duan JJ, Stachura S, Haque L, Karmakar A, Hemagiri H, Raut DK, Gupta AK, Khan J, Camac D, Sack JS, Pudzianowski A, Wu DR, Yarde M, Shen DR, Borowski V, Xie JH, Sun H, D'Arienzo C, Dabros M, Galella MA, Wang F, Weigelt CA, Zhao Q, Foster W, Somerville JE, Salter-Cid LM, Barrish JC, Carter PH, Dhar TGM. Gong H, et al. Among authors: galella ma. Bioorg Med Chem Lett. 2018 Jan 15;28(2):85-93. doi: 10.1016/j.bmcl.2017.12.006. Epub 2017 Dec 5. Bioorg Med Chem Lett. 2018. PMID: 29233651
Discovery and synthesis of tetrahydropyrimidinedione-4-carboxamides as endothelial lipase inhibitors.
Hu CH, Wang TC, Qiao JX, Haque L, Chen AYA, Taylor DS, Ying X, Onorato JM, Galella M, Shen H, Huang CS, Toussaint N, Li YX, Abell L, Adam LP, Gordon D, Wexler RR, Finlay HJ. Hu CH, et al. Among authors: galella m. Bioorg Med Chem Lett. 2018 Dec 15;28(23-24):3721-3725. doi: 10.1016/j.bmcl.2018.10.022. Epub 2018 Oct 15. Bioorg Med Chem Lett. 2018. PMID: 30348490
33 results