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2-Arylethenylchromone Derivatives : Synthesis and Anticancer Activity  

문창상 (한국과학기술연구원 생체과학연구부 의약화학센터)
이경원 (경희대학교 약학대학)
이지용 (한국과학기술연구원 생체과학연구부 의약화학센터)
이재열 (한국과학기술연구원 생체과학연구부 의약화학센터)
정봉영 (고려대학교 화학과)
이경태 (경희대학교 약학대학)
이용섭 (한국과학기술연구원 생체과학연구부 의약화학센터)
Publication Information
YAKHAK HOEJI / v.47, no.6, 2003 , pp. 376-381 More about this Journal
Abstract
2-Arylchromones, also known as flavones, are among the most ubiquitous classes of natural products occurring in the plant kingdom. On the other hand, 2-styrylchromones are relatively scarce in nature and only a few compounds has been isolated from the blue-green algae species. Therefore, new 2-arylethenylchromone derivatives ( 4a∼n, 5a∼f) were synthesized by the aldol condensation of 2-methylchromone ( 3) with several aromatic aldehydes in order to evaluate their cytotoxicities using a MTT assay on three tumor cells. 2-Arylethenylchromone derivative 4a showed the significant cytotoxic activities on KB, HL-60 and P-388 cell lines with $IC_{50}$/ values of 25.2, 63.59 and 49.51 $\mu$M, respectively, indicating that 2-arylethenylchromone skeleton has a potential anti-tumor application.
Keywords
styrylchromone; arylethenylchromone; flavonoid; aldol condensation; cytotoxicity; KB cell;
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