CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist

…, K Yoshimura, S Harada, T Tanaka, W Nomura…

Index: Narumi, Tetsuo; Ochiai, Chihiro; Yoshimura, Kazuhisa; Harada, Shigeyoshi; Tanaka, Tomohiro; Nomura, Wataru; Arai, Hiroshi; Ozaki, Taro; Ohashi, Nami; Matsushita, Shuzo; Tamamura, Hirokazu Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 19 p. 5853 - 5858

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Citation Number: 31

Abstract

Small molecules behaving as CD4 mimics were previously reported as HIV-1 entry inhibitors that block the gp120–CD4 interaction and induce a conformational change in gp120, exposing its co-receptor-binding site. A structure–activity relationship (SAR) study of a series of CD4 mimic analogs was conducted to investigate the contribution from the piperidine moiety of CD4 mimic 1 to anti-HIV activity, cytotoxicity, and CD4 mimicry effects on ...