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Page 1
Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.
Gavai AV, Fink BE, Fairfax DJ, Martin GS, Rossiter LM, Holst CL, Kim SH, Leavitt KJ, Mastalerz H, Han WC, Norris D, Goyal B, Swaminathan S, Patel B, Mathur A, Vyas DM, Tokarski JS, Yu C, Oppenheimer S, Zhang H, Marathe P, Fargnoli J, Lee FY, Wong TW, Vite GD. Gavai AV, et al. Among authors: holst cl. J Med Chem. 2009 Nov 12;52(21):6527-30. doi: 10.1021/jm9010065. J Med Chem. 2009. PMID: 19821562
Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.
Xiao HY, Balog A, Attar RM, Fairfax D, Fleming LB, Holst CL, Martin GS, Rossiter LM, Chen J, Cvjic ME, Dell-John J, Geng J, Gottardis MM, Han WC, Nation A, Obermeier M, Rizzo CA, Schweizer L, Spires T Jr, Shan W, Gavai A, Salvati ME, Vite G. Xiao HY, et al. Among authors: holst cl. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4491-5. doi: 10.1016/j.bmcl.2010.06.034. Epub 2010 Jun 10. Bioorg Med Chem Lett. 2010. PMID: 20584610
Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
Balog A, Rampulla R, Martin GS, Krystek SR, Attar R, Dell-John J, DiMarco JD, Fairfax D, Gougoutas J, Holst CL, Nation A, Rizzo C, Rossiter LM, Schweizer L, Shan W, Spergel S, Spires T, Cornelius G, Gottardis M, Trainor G, Vite GD, Salvati ME. Balog A, et al. Among authors: holst cl. ACS Med Chem Lett. 2015 Jun 19;6(8):908-12. doi: 10.1021/acsmedchemlett.5b00173. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288692 Free PMC article.
Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development.
Nair AG, Zeng Q, Selyutin O, Rosenblum SB, Jiang Y, Yang DY, Keertikar K, Zhou G, Dwyer MP, Kim SH, Shankar B, Yu W, Tong L, Chen L, Mazzola R, Caldwell J, Tang H, Allard ML, Buckle RN, Gauuan PJ, Holst CL, Martin GS, Naicker KP, Vellekoop S, Agrawal S, Liu R, Kong R, Ingravallo P, Xia E, Zhai Y, Nomeir A, Kozlowski JA. Nair AG, et al. Among authors: holst cl. Bioorg Med Chem Lett. 2016 Mar 1;26(5):1475-9. doi: 10.1016/j.bmcl.2016.01.050. Epub 2016 Jan 19. Bioorg Med Chem Lett. 2016. PMID: 26850003
Discovery of potent macrocyclic HCV NS5A inhibitors.
Yu W, Vibulbhan B, Rosenblum SB, Martin GS, Vellekoop AS, Holst CL, Coburn CA, Wong M, Selyutin O, Ji T, Zhong B, Hu B, Chen L, Dwyer MP, Jiang Y, Nair AG, Tong L, Zeng Q, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Fells J, Kozlowski JA. Yu W, et al. Among authors: holst cl. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3793-9. doi: 10.1016/j.bmcl.2016.05.042. Epub 2016 May 17. Bioorg Med Chem Lett. 2016. PMID: 27282743
Total synthesis of gibbilimbols A-D.
Vyvyan JR, Holst CL, Johnson AJ, Schwenk CM. Vyvyan JR, et al. Among authors: holst cl. J Org Chem. 2002 Apr 5;67(7):2263-5. doi: 10.1021/jo0162991. J Org Chem. 2002. PMID: 11925238