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5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors.
Albright JD, Reich MF, Delos Santos EG, Dusza JP, Sum FW, Venkatesan AM, Coupet J, Chan PS, Ru X, Mazandarani H, Bailey T. Albright JD, et al. Among authors: delos santos eg. J Med Chem. 1998 Jul 2;41(14):2442-4. doi: 10.1021/jm980179c. J Med Chem. 1998. PMID: 9651149 Clinical Trial. No abstract available.
5-fluoro-2-methyl-N-[5-(5H-pyrrolo[2,1-c][1,4]benzodiazepine-10(11H)-yl carbonyl)-2-pyridinyl]benzamide (CL-385004) and analogs as orally active arginine vasopressin receptor antagonists.
Aranapakam V, Albright JD, Grosu GT, Delos Santos EG, Chan PS, Coupet J, Ru X, Saunders T, Mazandarani H. Aranapakam V, et al. Among authors: delos santos eg. Bioorg Med Chem Lett. 1999 Jul 5;9(13):1737-40. doi: 10.1016/s0960-894x(99)00279-6. Bioorg Med Chem Lett. 1999. PMID: 10406633
Benzodiazepine inhibitors of the MMPs and TACE.
Nelson FC, Delos Santos E, Levin JI, Chen JM, Skotnicki JS, DiJoseph JF, Sharr MA, Sung A, Killar LM, Cowling R, Jin G, Roth CE, Albright JD. Nelson FC, et al. Bioorg Med Chem Lett. 2002 Oct 21;12(20):2867-70. doi: 10.1016/s0960-894x(02)00633-9. Bioorg Med Chem Lett. 2002. PMID: 12270165
Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.
Venkatesan AM, Dehnhardt CM, Delos Santos E, Chen Z, Dos Santos O, Ayral-Kaloustian S, Khafizova G, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Gibbons J, Abraham RT, Chaudhary I, Mansour TS. Venkatesan AM, et al. J Med Chem. 2010 Mar 25;53(6):2636-45. doi: 10.1021/jm901830p. J Med Chem. 2010. PMID: 20166697
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.
Dehnhardt CM, Venkatesan AM, Chen Z, Delos-Santos E, Ayral-Kaloustian S, Brooijmans N, Yu K, Hollander I, Feldberg L, Lucas J, Mallon R. Dehnhardt CM, et al. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4773-8. doi: 10.1016/j.bmcl.2011.06.063. Epub 2011 Jun 21. Bioorg Med Chem Lett. 2011. PMID: 21763134
Design and synthesis of novel diaminoquinazolines with in vivo efficacy for beta-catenin/T-cell transcriptional factor 4 pathway inhibition.
Dehnhardt CM, Venkatesan AM, Chen Z, Ayral-Kaloustian S, Dos Santos O, Delos Santos E, Curran K, Follettie MT, Diesl V, Lucas J, Geng Y, Dejoy SQ, Petersen R, Chaudhary I, Brooijmans N, Mansour TS, Arndt K, Chen L. Dehnhardt CM, et al. J Med Chem. 2010 Jan 28;53(2):897-910. doi: 10.1021/jm901370m. J Med Chem. 2010. PMID: 20025292
Benzodiazepine inhibitors of the MMPs and TACE. Part 2.
Levin JI, Nelson FC, Delos Santos E, Du MT, MacEwan G, Chen JM, Ayral-Kaloustian S, Xu J, Jin G, Cummons T, Barone D. Levin JI, et al. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4147-51. doi: 10.1016/j.bmcl.2004.06.031. Bioorg Med Chem Lett. 2004. PMID: 15261259
Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.
Dehnhardt CM, Venkatesan AM, Delos Santos E, Chen Z, Santos O, Ayral-Kaloustian S, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J, Chaudhary I, Yu K, Gibbons J, Abraham R, Mansour TS. Dehnhardt CM, et al. J Med Chem. 2010 Jan 28;53(2):798-810. doi: 10.1021/jm9014982. J Med Chem. 2010. PMID: 19968288
12 results