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The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer.
Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA, Friedman LS, Hayes A, Hancox TC, Kugendradas A, Lensun L, Moore P, Olivero AG, Pang J, Patel S, Pergl-Wilson GH, Raynaud FI, Robson A, Saghir N, Salphati L, Sohal S, Ultsch MH, Valenti M, Wallweber HJ, Wan NC, Wiesmann C, Workman P, Zhyvoloup A, Zvelebil MJ, Shuttleworth SJ. Folkes AJ, et al. Among authors: zvelebil mj. J Med Chem. 2008 Sep 25;51(18):5522-32. doi: 10.1021/jm800295d. J Med Chem. 2008. PMID: 18754654
Exploring the specificity of the PI3K family inhibitor LY294002.
Gharbi SI, Zvelebil MJ, Shuttleworth SJ, Hancox T, Saghir N, Timms JF, Waterfield MD. Gharbi SI, et al. Among authors: zvelebil mj. Biochem J. 2007 May 15;404(1):15-21. doi: 10.1042/BJ20061489. Biochem J. 2007. PMID: 17302559 Free PMC article.
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.
Beaufils F, Cmiljanovic N, Cmiljanovic V, Bohnacker T, Melone A, Marone R, Jackson E, Zhang X, Sele A, Borsari C, Mestan J, Hebeisen P, Hillmann P, Giese B, Zvelebil M, Fabbro D, Williams RL, Rageot D, Wymann MP. Beaufils F, et al. J Med Chem. 2017 Sep 14;60(17):7524-7538. doi: 10.1021/acs.jmedchem.7b00930. Epub 2017 Sep 1. J Med Chem. 2017. PMID: 28829592 Free PMC article.
Gene and protein expression profiling of human ovarian cancer cells treated with the heat shock protein 90 inhibitor 17-allylamino-17-demethoxygeldanamycin.
Maloney A, Clarke PA, Naaby-Hansen S, Stein R, Koopman JO, Akpan A, Yang A, Zvelebil M, Cramer R, Stimson L, Aherne W, Banerji U, Judson I, Sharp S, Powers M, deBilly E, Salmons J, Walton M, Burlingame A, Waterfield M, Workman P. Maloney A, et al. Cancer Res. 2007 Apr 1;67(7):3239-53. doi: 10.1158/0008-5472.CAN-06-2968. Cancer Res. 2007. PMID: 17409432
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.
Rageot D, Bohnacker T, Melone A, Langlois JB, Borsari C, Hillmann P, Sele AM, Beaufils F, Zvelebil M, Hebeisen P, Löscher W, Burke J, Fabbro D, Wymann MP. Rageot D, et al. J Med Chem. 2018 Nov 21;61(22):10084-10105. doi: 10.1021/acs.jmedchem.8b01262. Epub 2018 Nov 14. J Med Chem. 2018. PMID: 30359003 Free article.
Novel inhibitors of Trypanosoma cruzi dihydrofolate reductase.
Zuccotto F, Zvelebil M, Brun R, Chowdhury SF, Di Lucrezia R, Leal I, Maes L, Ruiz-Perez LM, Gonzalez Pacanowska D, Gilbert IH. Zuccotto F, et al. Eur J Med Chem. 2001 May;36(5):395-405. doi: 10.1016/s0223-5234(01)01235-1. Eur J Med Chem. 2001. PMID: 11451529
99 results