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

Tetsuo Narumi, Chihiro Ochiai, Kazuhisa Yoshimura, Shigeyoshi Harada, Tomohiro Tanaka, Wataru Nomura, Hiroshi Arai, Taro Ozaki, Nami Ohashi, Shuzo Matsushita, Hirokazu Tamamura

研究成果: Article査読

41 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)5853-5858
ページ数6
ジャーナルBioorganic and Medicinal Chemistry Letters
20
19
DOI
出版ステータスPublished - 1 10月 2010

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