1253393-98-4Relevant articles and documents
CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist
Narumi, Tetsuo,Ochiai, Chihiro,Yoshimura, Kazuhisa,Harada, Shigeyoshi,Tanaka, Tomohiro,Nomura, Wataru,Arai, Hiroshi,Ozaki, Taro,Ohashi, Nami,Matsushita, Shuzo,Tamamura, Hirokazu
scheme or table, p. 5853 - 5858 (2010/11/18)
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.