Recent advances in the discovery and development of flavonoids and their analogues as antitumor and anti-HIV agents.
Antitumor and anti-HIV flavonoids and their analogues will be reviewed with emphasis on those discovered in our laboratory. The active antitumor compounds include the antileukemic tricin (1) and kaempferol-3-O-beta-D-glucopyranoside (2) from Wikstroemia indica, the cytotoxic hinokiflavone (3) from Rhus succedanea, the cytotoxic isoflavone (8) from Amorpha fruticosa, two dihydroxypentamethoxyflavones (9, 10) from Polanisia dodencandra. The development of synthetic 2-phenyl-4-quinolones as potent cytotoxic antimitotic flavonoid analogues and 2-phenylthiochromen-4-ones as potent antitumor flavonoid analogues will be presented. Selected results from other laboratories and antitumor-related biological studies also will be discussed. Flavonoids have also been investigated as potential anti-HIV agents. In our laboratory, acacetin-7-O-beta-D-galactopyranoside (131) from Chrysanthemum morifolium and chrysin (102), as well as apigenin-7-O-beta-D-glucopyranoside (130), from Kummerowia striata, have been found to exhibit anti-HIV activity. In other studies, some flavonoids and related compounds have been investigated as inhibitors of HIV-1 reverse transcriptase, protease, and integrase. The isolation and structural modification of such plant-derived active principles provide a continuing source of potential antitumor and anti-HIV agents.
Natural Products Laboratory, School of Pharmacy University of North Carolina, Chapel Hill 27599, USA.
H K
HK
Wang
Y
Y
Xia
Z Y
ZY
Yang
S L
SL
Natschke
K H
KH
Lee
D000818:Animals; D019380:Anti-HIV Agents / Q000494:pharmacology* / Q000627:therapeutic use*; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use*; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D015658:HIV Infections / Q000188:drug therapy*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*
D019380:Anti-HIV Agents; D000970:Antineoplastic Agents; D005419:Flavonoids