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Page 1
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: hollander i. 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
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.
Venkatesan AM, Chen Z, dos Santos O, Dehnhardt C, Santos ED, Ayral-Kaloustian S, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Chaudhary I, Mansour TS. Venkatesan AM, et al. Among authors: hollander i. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5869-73. doi: 10.1016/j.bmcl.2010.07.104. Epub 2010 Jul 30. Bioorg Med Chem Lett. 2010. PMID: 20797855
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: hollander i. 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
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: hollander i. 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
Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).
Kaplan J, Verheijen JC, Brooijmans N, Toral-Barza L, Hollander I, Yu K, Zask A. Kaplan J, et al. Among authors: hollander i. Bioorg Med Chem Lett. 2010 Jan 15;20(2):640-3. doi: 10.1016/j.bmcl.2009.11.050. Epub 2009 Dec 4. Bioorg Med Chem Lett. 2010. PMID: 19963384
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: hollander i. J Med Chem. 2010 Jan 28;53(2):798-810. doi: 10.1021/jm9014982. J Med Chem. 2010. PMID: 19968288
74 results