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Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties.
Gunzner-Toste J, Zhao G, Bauer P, Baumeister T, Buckmelter AJ, Caligiuri M, Clodfelter KH, Fu B, Han B, Ho YC, Kley N, Liang X, Liederer BM, Lin J, Mukadam S, O'Brien T, Oh A, Reynolds DJ, Sharma G, Skelton N, Smith CC, Sodhi J, Wang W, Wang Z, Xiao Y, Yuen PW, Zak M, Zhang L, Zheng X, Bair KW, Dragovich PS. Gunzner-Toste J, et al. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3531-8. doi: 10.1016/j.bmcl.2013.04.040. Epub 2013 Apr 25. Bioorg Med Chem Lett. 2013. PMID: 23668988
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.
Zheng X, Bauer P, Baumeister T, Buckmelter AJ, Caligiuri M, Clodfelter KH, Han B, Ho YC, Kley N, Lin J, Reynolds DJ, Sharma G, Smith CC, Wang Z, Dragovich PS, Gunzner-Toste J, Liederer BM, Ly J, O'Brien T, Oh A, Wang L, Wang W, Xiao Y, Zak M, Zhao G, Yuen PW, Bair KW. Zheng X, et al. J Med Chem. 2013 Aug 22;56(16):6413-33. doi: 10.1021/jm4008664. Epub 2013 Jul 31. J Med Chem. 2013. PMID: 23859118
Combination drug scheduling defines a "window of opportunity" for chemopotentiation of gemcitabine by an orally bioavailable, selective ChK1 inhibitor, GNE-900.
Blackwood E, Epler J, Yen I, Flagella M, O'Brien T, Evangelista M, Schmidt S, Xiao Y, Choi J, Kowanetz K, Ramiscal J, Wong K, Jakubiak D, Yee S, Cain G, Gazzard L, Williams K, Halladay J, Jackson PK, Malek S. Blackwood E, et al. Mol Cancer Ther. 2013 Oct;12(10):1968-80. doi: 10.1158/1535-7163.MCT-12-1218. Epub 2013 Jul 19. Mol Cancer Ther. 2013. PMID: 23873850
Identification of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Dragovich PS, Bair KW, Baumeister T, Ho YC, Liederer BM, Liu X, Liu Y, O'Brien T, Oeh J, Sampath D, Skelton N, Wang L, Wang W, Wu H, Xiao Y, Yuen PW, Zak M, Zhang L, Zheng X. Dragovich PS, et al. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4875-85. doi: 10.1016/j.bmcl.2013.06.090. Epub 2013 Jul 6. Bioorg Med Chem Lett. 2013. PMID: 23899614
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Zheng X, Bair KW, Bauer P, Baumeister T, Bowman KK, Buckmelter AJ, Caligiuri M, Clodfelter KH, Feng Y, Han B, Ho YC, Kley N, Li H, Liang X, Liederer BM, Lin J, Ly J, O'Brien T, Oeh J, Oh A, Reynolds DJ, Sampath D, Sharma G, Skelton N, Smith CC, Tremayne J, Wang L, Wang W, Wang Z, Wu H, Wu J, Xiao Y, Yang G, Yuen PW, Zak M, Dragovich PS. Zheng X, et al. Bioorg Med Chem Lett. 2013 Oct 15;23(20):5488-97. doi: 10.1016/j.bmcl.2013.08.074. Epub 2013 Aug 22. Bioorg Med Chem Lett. 2013. PMID: 24021463
3,531 results