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 f...

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Veröffentlicht in:European journal of medicinal chemistry 2006-08, Vol.41 (8), p.991-996
Hauptverfasser: Lee, Ki Yong, Nam, Dong Hyuk, Moon, Chang Sang, Seo, Seon Hee, Lee, Jae Yeol, Lee, Yong Sup
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container_end_page 996
container_issue 8
container_start_page 991
container_title European journal of medicinal chemistry
container_volume 41
creator Lee, Ki Yong
Nam, Dong Hyuk
Moon, Chang Sang
Seo, Seon Hee
Lee, Jae Yeol
Lee, Yong Sup
description 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 μg/ml indicating that lavendustin A derivatives containing 2-arylethenylchromone ring have a potential in anti-tumor application.
doi_str_mv 10.1016/j.ejmech.2006.04.008
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subjects Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Arylethenylchromone
Biological and medical sciences
Cell Line, Tumor
Chromones - chemical synthesis
Chromones - chemistry
Chromones - pharmacology
Cytotoxicity
Drug Screening Assays, Antitumor
General aspects
HCT-15
Humans
Lavendustin A
Magnetic Resonance Spectroscopy
Medical sciences
Pharmacology. Drug treatments
Phenols - chemical synthesis
Phenols - chemistry
Phenols - pharmacology
Styrylchromone
title Synthesis and anticancer activity of lavendustin A derivatives containing arylethenylchromone substituents
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