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Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.
Verheijen JC, Richard DJ, Curran K, Kaplan J, Lefever M, Nowak P, Malwitz DJ, Brooijmans N, Toral-Barza L, Zhang WG, Lucas J, Hollander I, Ayral-Kaloustian S, Mansour TS, Yu K, Zask A. Verheijen JC, et al. Among authors: yu k. J Med Chem. 2009 Dec 24;52(24):8010-24. doi: 10.1021/jm9013828. J Med Chem. 2009. PMID: 19894727
Pyranonaphthoquinone lactones: a new class of AKT selective kinase inhibitors alkylate a regulatory loop cysteine.
Salaski EJ, Krishnamurthy G, Ding WD, Yu K, Insaf SS, Eid C, Shim J, Levin JI, Tabei K, Toral-Barza L, Zhang WG, McDonald LA, Honores E, Hanna C, Yamashita A, Johnson B, Li Z, Laakso L, Powell D, Mansour TS. Salaski EJ, et al. Among authors: yu k. J Med Chem. 2009 Apr 23;52(8):2181-4. doi: 10.1021/jm900075g. J Med Chem. 2009. PMID: 19309081
Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.
Yu K, Toral-Barza L, Shi C, Zhang WG, Lucas J, Shor B, Kim J, Verheijen J, Curran K, Malwitz DJ, Cole DC, Ellingboe J, Ayral-Kaloustian S, Mansour TS, Gibbons JJ, Abraham RT, Nowak P, Zask A. Yu K, et al. Cancer Res. 2009 Aug 1;69(15):6232-40. doi: 10.1158/0008-5472.CAN-09-0299. Epub 2009 Jul 7. Cancer Res. 2009. PMID: 19584280
ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines.
Zask A, Verheijen JC, Curran K, Kaplan J, Richard DJ, Nowak P, Malwitz DJ, Brooijmans N, Bard J, Svenson K, Lucas J, Toral-Barza L, Zhang WG, Hollander I, Gibbons JJ, Abraham RT, Ayral-Kaloustian S, Mansour TS, Yu K. Zask A, et al. Among authors: yu k. J Med Chem. 2009 Aug 27;52(16):5013-6. doi: 10.1021/jm900851f. J Med Chem. 2009. PMID: 19645448
Hybrid inhibitors of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR): design, synthesis, and superior antitumor activity of novel wortmannin-rapamycin conjugates.
Ayral-Kaloustian S, Gu J, Lucas J, Cinque M, Gaydos C, Zask A, Chaudhary I, Wang J, Di L, Young M, Ruppen M, Mansour TS, Gibbons JJ, Yu K. Ayral-Kaloustian S, et al. Among authors: yu k. J Med Chem. 2010 Jan 14;53(1):452-9. doi: 10.1021/jm901427g. J Med Chem. 2010. PMID: 19928864
9,377 results