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Page 1
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
Acetylenic TACE inhibitors. Part 1. SAR of the acyclic sulfonamide hydroxamates.
Levin JI, Chen JM, Cheung K, Cole D, Crago C, Santos ED, Du X, Khafizova G, MacEwan G, Niu C, Salaski EJ, Zask A, Cummons T, Sung A, Xu J, Zhang Y, Xu W, Ayral-Kaloustian S, Jin G, Cowling R, Barone D, Mohler KM, Black RA, Skotnicki JS. Levin JI, et al. Bioorg Med Chem Lett. 2003 Aug 18;13(16):2799-803. doi: 10.1016/s0960-894x(03)00514-6. Bioorg Med Chem Lett. 2003. PMID: 12873518
Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors.
Zask A, Kaplan J, Du X, MacEwan G, Sandanayaka V, Eudy N, Levin J, Jin G, Xu J, Cummons T, Barone D, Ayral-Kaloustian S, Skotnicki J. Zask A, et al. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1641-5. doi: 10.1016/j.bmcl.2005.01.053. Bioorg Med Chem Lett. 2005. PMID: 15745814
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
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. Among authors: ayral kaloustian s. J Med Chem. 2010 Mar 25;53(6):2636-45. doi: 10.1021/jm901830p. J Med Chem. 2010. PMID: 20166697
4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).
Tsou HR, MacEwan G, Birnberg G, Zhang N, Brooijmans N, Toral-Barza L, Hollander I, Ayral-Kaloustian S, Yu K. Tsou HR, et al. Among authors: ayral kaloustian s. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2259-63. doi: 10.1016/j.bmcl.2010.02.012. Epub 2010 Feb 6. Bioorg Med Chem Lett. 2010. PMID: 20188551
Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).
Tsou HR, MacEwan G, Birnberg G, Grosu G, Bursavich MG, Bard J, Brooijmans N, Toral-Barza L, Hollander I, Mansour TS, Ayral-Kaloustian S, Yu K. Tsou HR, et al. Among authors: ayral kaloustian s. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2321-5. doi: 10.1016/j.bmcl.2010.01.135. Epub 2010 Feb 2. Bioorg Med Chem Lett. 2010. PMID: 20188552
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. Among authors: ayral kaloustian s. 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
44 results