Synthesis and anticancer activity of lavendustin A derivatives containing arylethenylchromone substituents |
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Authors: | Lee Ki Yong Nam Dong Hyuk Moon Chang Sang Seo Seon Hee Lee Jae Yeol Lee Yong Sup |
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Affiliation: | 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 |
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Abstract: | 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. |
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