Prodrug design, synthesis and pharmacokinetic evaluation of (3'R, 4'R)-3-hydroxymethyl-4-methyl-3', 4'-di-O-(S)-camphanoyl-(+)-cis-khellactone

• Main Authors: Huanfang Guo (Author), Xiaomei Zhuang (Author), Keduo Qian (Author), Lianqi Sun (Author), Xiaofeng Wang (Author), Hua Li (Author), Kuohsiung Lee (Author), Lan Xie (Author)
• Format: Book
• Published: Elsevier, 2012-04-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

3-Hydroxymethyl-4-methyl-DCK (3, HMDCK) was discovered previously as a potent HIV non-nucleoside reverse transcriptase inhibitor (NNRTIs) (EC50: 0.004 μM, TI: 6225) with a novel mechanism of action. It exerts anti-HIV activity by inhibiting the production of HIV-1 double-stranded viral DNA from a si...