Synthesis and Structure–Activity Relationship Correlations of Gnidimacrin Derivatives as Potent HIV‑1 Inhibitors and HIV Latency Reversing Agents

• Published in: Journal of medicinal chemistry Vol. 62; no. 15; pp. 6958 - 6971
• Main Authors: Liu, Qingbo, Cheng, Yung-Yi, Li, Wei, Huang, Li, Asada, Yoshihisa, Hsieh, Min-Tsang, Morris-Natschke, Susan L, Chen, Chin-Ho, Koike, Kazuo, Lee, Kuo-Hsiung
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 08.08.2019; Amer Chemical Soc
• Subjects: Animals; Anti-HIV Agents - chemical synthesis; Anti-HIV Agents - pharmacology; Chemistry, Medicinal; Diterpenes - chemical synthesis; Diterpenes - pharmacology; HIV-1 - drug effects; HIV-1 - physiology; Humans; Life Sciences & Biomedicine; Pharmacology & Pharmacy; Plant Extracts - chemical synthesis; Plant Extracts - isolation & purification; Plant Extracts - pharmacology; Plant Roots; Rats; Rats, Sprague-Dawley; Reactive Oxygen Species - chemical synthesis; Reactive Oxygen Species - pharmacology; Science & Technology; Structure-Activity Relationship; Virus Latency - drug effects; Virus Latency - physiology; ANTI-AIDS AGENTS; ELIMINATION; REPLICATION; DITERPENOIDS

Currently, due to the HIV latency mechanism, the search continues for effective drugs to combat this issue and provide a cure for AIDS. Gnidimacrin activates latent HIV-1 replication and inhibits HIV-1 infection at picomolar concentrations. This natural diterpene was able to markedly reduce the late...