Synthesis and anticancer activity of lavendustin A derivatives containing arylethenylchromone substituents.
2-Styrylchromones, which are relatively scarce in nature, have been reported to possess potent cytotoxicities on KB cell line. Lavendustin A, a metabolite of Streptomyces griseolavendus, has been shown to inhibit a growth of A431 cell line. Accordingly, a series of compounds 3a-g having structural features of styrylchromones and lavendustin A were synthesized and evaluated for cytotoxicity using SRB assay on four tumor cell lines. Compounds 3a-g were synthesized by the condensation of 2-methylchromone derivative 7 with several aromatic aldehydes. Among synthesized, compound 3e showed the significant cytotoxic activity on HCT-15 cell line with IC(50) values of 7.17 microg/ml indicating that lavendustin A derivatives containing 2-arylethenylchromone ring have a potential in anti-tumor application.
Lee
Ki Yong
KY
Kyung Hee East-West Pharmaceutical Research Institute and Department of Pharmaceutical Science, College of Pharmacy, Kyung Hee University, 1 Hoegi-Dong, Seoul 130-701, South-Korea. kyslee@khu.ac.kr
Nam
Dong Hyuk
DH
Moon
Chang Sang
CS
Seo
Seon Hee
SH
Lee
Jae Yeol
JY
Lee
Yong Sup
YS
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002867:Chromones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D010636:Phenols / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000970:Antineoplastic Agents; D002867:Chromones; D010636:Phenols; C062898:lavendustin A