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Background and the purpose of the study  There has been increscent interest in the field of cancer chemotherapy by discovery and development of novel agents with high efficacy, low toxicity, and minimum side effects. In order to find new anticancer agents, we replaced the pyrazolone part of well-known cytotoxic agent SJ-172550 with 7-methoxychroman-4-one. Thus, a novel series of 3-benzylidene-4-chromanones were synthesized and tested in vitro against human cancer cell lines.    Methods  The title compounds were prepared by condensation of 7-methoxychroman-4-one with suitable aldehydes in appropriate alcohol in the presence of gaseous HCl. The antiproliferative activity of target compounds were evaluated against MDA-MB-231 (breast cancer), KB (nasopharyngeal epidermoid carcinoma) and SK-N-MC (human neuroblastoma) cell lines using MTT assay.    Results  Although the direct analog of SJ-172550 (compound  5d ) did not show any cytotoxic activity against tested cell lines, but 2-(2-chloro-6-methoxyphenoxy)acetic acid methyl ester analog  5c  showed some activity against MDA-MB-231 and SK-N-MC cells. Further modification of compound  5c  resulted in the 3-chloro-4,5-dimethoxybenzylidene derivative  5b  which demonstrated better cytotoxic profile against all tested cell lines (IC 50  values = 7.56–25.04 μg/ml).    Conclusion  The results demonstrated that the cytotoxic activity of compound  5b  against MDA-MB-231 and SK-N-MC cells is more than etoposide. Therefore, compound  5b  prototype could be considered as novel cytotoxic agent for further developing new anticancer chemotherapeutics.

Synthesis and cytotoxic properties of novel (E)-3-benzylidene-7-methoxychroman-4-one derivatives