Design, synthesis and X-ray crystallographic study of NAmPRTase inhibitors as anti-cancer agents

H You, HS Youn, I Im, MH Bae, SK Lee, H Ko…

Index: You, Hyun; Youn, Hyung-Seop; Im, Isak; Bae, Man-Ho; Lee, Sang-Kook; Ko, Hyojin; Eom, Soo Hyun; Kim, Yong-Chul European Journal of Medicinal Chemistry, 2011 , vol. 46, # 4 p. 1153 - 1164

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Citation Number: 13

Abstract

NAmPRTase (PBEF/Visfatin) plays a pivotal role in the salvage pathway of NAD+ biosynthesis. NAmPRTase has been an attractive target for anti-cancer agents that induce apoptosis of tumor cells via a declining plasma NAD+ level. In this report, a series of structural analogs of FK866 (1), a known NAmPRTase inhibitor, was synthesized and tested for inhibitory activities against the proliferation of cancer cells and human NAmPRTase. ...