Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1, 6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties

…, YT Zheng, J Ding, N Neamati, YQ Long

Index: Zeng, Li-Fan; Wang, Yong; Kazemi, Roza; Xu, Shili; Xu, Zhong-Liang; Sanchez, Tino W.; Yang, Liu-Meng; Debnath, Bikash; Odde, Srinivas; Xie, Hua; Zheng, Yong-Tang; Ding, Jian; Neamati, Nouri; Long, Ya-Qiu Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9492 - 9509

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Citation Number: 20

Abstract

Among a large number of HIV-1 integrase (IN) inhibitors, the 8-hydroxy-[1, 6] naphthyridines (ie, L-870,810) were one of the promising class of antiretroviral drugs developed by Merck Laboratories. In spite of its remarkable potency and efficacy, unfortunately upon completion of phase I clinical studies, development of L-870,810 was halted. Because of its desirable pharmacological and pharmaceutical properties we were intrigued to design novel ...