CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist |
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Authors: | Tetsuo Narumi Chihiro Ochiai Kazuhisa Yoshimura Shigeyoshi Harada Tomohiro Tanaka Wataru Nomura Hiroshi Arai Taro Ozaki Nami Ohashi Shuzo Matsushita Hirokazu Tamamura |
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Affiliation: | 1. Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan;2. Center for AIDS Research, Kumamoto University, Kumamoto 860-0811, Japan |
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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 conformational changes of gp120. In addition, several hybrid molecules based on conjugation of a CD4 mimic analog with a selective CXCR4 antagonist were also synthesized and their utility evaluated. |
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