Synthesis and anticancer activity of lavendustin A derivatives containing arylethenylchromone substituents.

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.

• Authors: Ki Yong Lee, Dong Hyuk Nam, Chang Sang Moon, Seon Hee Seo, Jae Yeol Lee, Yong Sup Lee
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 41 Issue 8 Pg. 991-6 (Aug 2006) ISSN: 0223-5234 [Print] France
• PMID: 16762460 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Chromones
• Phenols
• lavendustin A

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Chromones (chemical synthesis, chemistry, pharmacology)
• Drug Screening Assays, Antitumor
• Humans
• Magnetic Resonance Spectroscopy
• Phenols (chemical synthesis, chemistry, pharmacology)