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204 results

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Page 1
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.
Cai J, Bennett DJ, Rankovic Z, Dempster M, Fradera X, Gillespie J, Cumming I, Finlay W, Baugh M, Boucharens S, Bruin J, Cameron KS, Hamilton W, Kerr J, Kinghorn E, McGarry G, Robinson J, Scullion P, Uitdehaag JC, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E. Cai J, et al. Among authors: bennett dj. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4447-50. doi: 10.1016/j.bmcl.2010.06.049. Epub 2010 Jun 15. Bioorg Med Chem Lett. 2010. PMID: 20594841
4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important.
Cai J, Fradera X, van Zeeland M, Dempster M, Cameron KS, Bennett DJ, Robinson J, Popplestone L, Baugh M, Westwood P, Bruin J, Hamilton W, Kinghorn E, Long C, Uitdehaag JC. Cai J, et al. Among authors: bennett dj. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4507-10. doi: 10.1016/j.bmcl.2010.06.043. Epub 2010 Jun 10. Bioorg Med Chem Lett. 2010. PMID: 20580231
Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.
Cai J, Robinson J, Belshaw S, Everett K, Fradera X, van Zeeland M, van Berkom L, van Rijnsbergen P, Popplestone L, Baugh M, Dempster M, Bruin J, Hamilton W, Kinghorn E, Westwood P, Kerr J, Rankovic Z, Arbuckle W, Bennett DJ, Jones PS, Long C, Martin I, Uitdehaag JC, Meulemans T. Cai J, et al. Among authors: bennett dj. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6890-4. doi: 10.1016/j.bmcl.2010.10.012. Epub 2010 Oct 26. Bioorg Med Chem Lett. 2010. PMID: 21030256
1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka.
Arbuckle W, Baugh M, Belshaw S, Bennett DJ, Bruin J, Cai J, Cameron KS, Claxton C, Dempster M, Everett K, Fradera X, Hamilton W, Jones PS, Kinghorn E, Long C, Martin I, Robinson J, Westwood P. Arbuckle W, et al. Among authors: bennett dj. Bioorg Med Chem Lett. 2011 Feb 1;21(3):932-5. doi: 10.1016/j.bmcl.2010.12.065. Epub 2010 Dec 19. Bioorg Med Chem Lett. 2011. PMID: 21227690
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Hoyt SB, Park MK, London C, Xiong Y, Tata J, Bennett DJ, Cooke A, Cai J, Carswell E, Robinson J, MacLean J, Brown L, Belshaw S, Clarkson TR, Liu K, Liang GB, Struthers M, Cully D, Wisniewski T, Ren N, Bopp C, Sok A, Cai TQ, Stribling S, Pai LY, Ma X, Metzger J, Verras A, McMasters D, Chen Q, Tung E, Tang W, Salituro G, Buist N, Kuethe J, Rivera N, Clemas J, Zhou G, Gibson J, Maxwell CA, Lassman M, McLaughlin T, Castro-Perez J, Szeto D, Forrest G, Hajdu R, Rosenbach M, Ali A. Hoyt SB, et al. Among authors: bennett dj. ACS Med Chem Lett. 2015 Apr 7;6(5):573-8. doi: 10.1021/acsmedchemlett.5b00054. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005536 Free PMC article.
Imidazopyridyl compounds as aldosterone synthase inhibitors.
Whitehead BR, Lo MM, Ali A, Park MK, Hoyt SB, Xiong Y, Cai J, Carswell E, Cooke A, MacLean J, Ratcliffe P, Robinson J, Bennett DJ, Clemas JA, Wisniewski T, Struthers M, Cully D, MacNeil DJ. Whitehead BR, et al. Among authors: bennett dj. Bioorg Med Chem Lett. 2017 Jan 15;27(2):143-146. doi: 10.1016/j.bmcl.2016.12.003. Epub 2016 Dec 2. Bioorg Med Chem Lett. 2017. PMID: 27979595
Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.
Zhang H, Liu K, Pu Q, Achab A, Ardolino MJ, Cheng M, Deng Y, Doty AC, Ferguson H, Fradera X, Knemeyer I, Kurukulasuriya R, Lam YH, Lesburg CA, Martinot TA, McGowan MA, Miller JR, Otte K, Biju PJ, Sciammetta N, Solban N, Yu W, Zhou H, Wang X, Bennett DJ, Han Y. Zhang H, et al. Among authors: bennett dj. ACS Med Chem Lett. 2019 Sep 18;10(11):1530-1536. doi: 10.1021/acsmedchemlett.9b00344. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749906 Free PMC article.
Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors.
Pu Q, Zhang H, Guo L, Cheng M, Doty AC, Ferguson H, Fradera X, Lesburg CA, McGowan MA, Miller JR, Geda P, Song X, Otte K, Sciammetta N, Solban N, Yu W, Sloman DL, Zhou H, Lammens A, Neumann L, Bennett DJ, Pasternak A, Han Y. Pu Q, et al. Among authors: bennett dj. ACS Med Chem Lett. 2020 Jul 15;11(8):1548-1554. doi: 10.1021/acsmedchemlett.0c00195. eCollection 2020 Aug 13. ACS Med Chem Lett. 2020. PMID: 32832022 Free PMC article.
204 results