1253393-96-2Relevant academic research and scientific papers
Small molecular CD4 mimics as HIV entry inhibitors
Narumi, Tetsuo,Arai, Hiroshi,Yoshimura, Kazuhisa,Harada, Shigeyoshi,Nomura, Wataru,Matsushita, Shuzo,Tamamura, Hirokazu
, p. 6735 - 6742 (2011/12/04)
Derivatives of CD4 mimics were designed and synthesized to interact with the conserved residues of the Phe43 cavity in gp120 to investigate their anti-HIV activity, cytotoxicity, and CD4 mimicry effects on conformational changes of gp120. Significant potency gains were made by installation of bulky hydrophobic groups into the piperidine moiety, resulting in discovery of a potent compound with a higher selective index and CD4 mimicry. The current study identified a novel lead compound 11 with significant anti-HIV activity and lower cytotoxicity than those of known CD4 mimics.
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
experimental part, 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.
