Synthesis and antiviral activities of novel acylhydrazone derivatives targeting HIV-1 capsid protein.
HIV-1 capsid protein (CA) plays important roles in the viral replication cycle. A number of acylhydrazone derivatives that act as inhibitors of HIV-1 CA assembly, were designed and synthesized. The synthesized compounds were tested for their antiviral activities and cytotoxicities using CEM cells. Some derivatives also were assayed for their ability to inhibit HIV-1 CA assembly in vitro. Among them, compounds 14f and 14i display the most promising potency with EC(50) values of 0.21 and 0.17 microM respectively.
Tian
Baohe
B
State Key Laboratory of Natural and Biomimetic Drugs, Peking University, PO Box 261, Beijing 100191, China.
He
Meizi
M
Tang
Shixing
S
Hewlett
Indira
I
Tan
Zhiwu
Z
Li
Jiebo
J
Jin
Yinxue
Y
Yang
Ming
M
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001665:Binding Sites / Q000187:drug effects / Q000502:physiology; D036022:Capsid Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism* / Q000502:physiology; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems / Q000379:methods*; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D006835:Hydrazones / Q000138:chemical synthesis* / Q000494:pharmacology
D019380:Anti-HIV Agents; D000998:Antiviral Agents; D036022:Capsid Proteins; D006835:Hydrazones