Anti-AIDS agents 54. A potent anti-HIV chalcone and flavonoids from genus Desmos.
Sixteen flavonoids and their derivatives isolated from Desmos spp. were evaluated for inhibition of HIV replication in H9 lymphocyte cells. 2-Methoxy-3-methyl-4,6-dihydroxy-5-(3'-hydroxy)cinnamoylbenzaldehyde (12) and lawinal (6) demonstrated potent anti-HIV activity with EC(50) values of 0.022 and 2.30 microg/mL and therapeutic indexes of 489 and 45.2, respectively. Compound 12 appears to be an excellent lead for further anti-HIV drug development.
Department of Pharmacy, 306 Hospital of PLA, Beijing 100101, China.
Jiu-Hong
JH
Wu
Xi-Hong
XH
Wang
Yang-Hua
YH
Yi
Kuo-Hsiung
KH
Lee
D029061:Annonaceae / Q000737:chemistry*; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D002599:Chalcone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D004365:Drugs, Chinese Herbal; D005419:Flavonoids / Q000138:chemical synthesis / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D010946:Plants, Medicinal; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
D019380:Anti-HIV Agents; D004365:Drugs, Chinese Herbal; D005419:Flavonoids; D002599:Chalcone