Preparation and anti-HIV activities of retrojusticidin B analogs and azalignans.
Ten lignans (2-11) and a series of azalignans including 1-aryl-pyrronaphthalenes 20-24 and 3-N-alkylaminomethyl-1-arylnaphthalenes 25-28, structurally related to two HIV reverse transcriptase inhibitors, retrojusticidin B and phyllamyricin A, were prepared from phyllanthin (1) for evaluation of anti-HIV activities. Anti-HIV activity of these compounds on a R5 pseudotype virus, ConB/pNL43E-L+, in the U87-CD4-CCR5 cells has been measured. Compounds 5, 22, 23, and 28 showed good anti-HIV activity with IC(50) value of 0.25, 1.07, 0.01, 0.32 microg/mL, respectively.
Sagar
Kadali S
KS
School of Pharmacy, College of Medicine, National Taiwan University, Taipei 100, Taiwan, ROC.
Chang
Chia-Chuan
CC
Wang
Wei-Kung
WK
Lin
Jung-Yaw
JY
Lee
Shoei-Sheng
SS
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001681:Biological Assay; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D017705:Lignans / Q000138:chemical synthesis* / Q000494:pharmacology*; D015394:Molecular Structure; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology*
D019380:Anti-HIV Agents; D017705:Lignans; D009281:Naphthalenes; C496007:phyllamyricin A; C496008:retrojusticidin B