Analogues of 4-[(7-Bromo-2-methyl-4-oxo-3 H-quinazolin-6-yl) methylprop-2-ynylamino]-N-(3-pyridylmethyl) benzamide (CB-30865) as Potent Inhibitors of …

…, J Green, R McKinnon, RT Terry-Lorenzo…

Index: Lockman, Jeffrey W.; Murphy, Brett R.; Zigar, Daniel F.; Judd, Weston R.; Slattum, Paul M.; Gao, Zhong-Hua; Ostanin, Kirill; Green, Jeremy; McKinnon, Rena; Terry-Lorenzo, Ryan T.; Fleischer, Tracey C.; Boniface, J. Jay; Shenderovich, Mark; Willardsen, J. Adam Journal of Medicinal Chemistry, 2010 , vol. 53, # 24 p. 8734 - 8746

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Citation Number: 22

Abstract

We have shown previously that the target of the potent cytotoxic agent 4-[(7-bromo-2-methyl- 4-oxo-3 H-quinazolin-6-yl) methyl-prop-2-ynylamino]-N-(3-pyridylmethyl) benzamide (CB38065, 1) is nicotinamide phosphoribosyltransferase (Nampt). With its cellular target known we sought to optimize the biochemical and cellular Nampt activity of 1 as well as its cytotoxicity. It was found that a 3-pyridylmethylamide substituent in the A region was ...