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Page 1
Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.
Venkatesan AM, Dehnhardt CM, Chen Z, Santos ED, Dos Santos O, Bursavich M, Gilbert AM, Ellingboe JW, Ayral-Kaloustian S, Khafizova G, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Gibbons J, Abraham R, Mansour TS. Venkatesan AM, et al. Among authors: feldberg l. Bioorg Med Chem Lett. 2010 Jan 15;20(2):653-6. doi: 10.1016/j.bmcl.2009.11.057. Epub 2009 Dec 1. Bioorg Med Chem Lett. 2010. PMID: 19954970
Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.
Berger DM, Torres N, Dutia M, Powell D, Ciszewski G, Gopalsamy A, Levin JI, Kim KH, Xu W, Wilhelm J, Hu Y, Collins K, Feldberg L, Kim S, Frommer E, Wojciechowicz D, Mallon R. Berger DM, et al. Among authors: feldberg l. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6519-23. doi: 10.1016/j.bmcl.2009.10.049. Epub 2009 Oct 26. Bioorg Med Chem Lett. 2009. PMID: 19864136
Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.
Gopalsamy A, Ciszewski G, Shi M, Berger D, Hu Y, Lee F, Feldberg L, Frommer E, Kim S, Collins K, Wojciechowicz D, Mallon R. Gopalsamy A, et al. Among authors: feldberg l. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6890-2. doi: 10.1016/j.bmcl.2009.10.074. Epub 2009 Oct 22. Bioorg Med Chem Lett. 2009. PMID: 19884006
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. Among authors: feldberg l. 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: feldberg l. J Med Chem. 2010 Mar 25;53(6):2636-45. doi: 10.1021/jm901830p. J Med Chem. 2010. PMID: 20166697
B-Raf kinase inhibitors: hit enrichment through scaffold hopping.
Gopalsamy A, Shi M, Hu Y, Lee F, Feldberg L, Frommer E, Kim S, Collins K, Wojciechowicz D, Mallon R. Gopalsamy A, et al. Among authors: feldberg l. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2431-4. doi: 10.1016/j.bmcl.2010.03.030. Epub 2010 Mar 9. Bioorg Med Chem Lett. 2010. PMID: 20307980
64 results