Synthesis of novel chromene derivatives of expected antitumor activity

Inhibition of tubulin polymerization is one of the important tactics in cancer therapy. Since 4-aryl-4H-chromene derivatives are found to be microtubule-binding agents via interfering with tubulin polymerization so we decide to concentrate our exploration efforts on the combination of this nucleus with 5-, 6-, and/or 7-memebered heterocyclic moieties in a novel series of compounds to explore the effect that might result from this combination. Ten novel compounds were selected for anticancer screening assay against MCF-7 breast cancer cell line in comparison to colchicine as positive control and most of them showed excellent activity.

Graphical abstractThese triazolochromenopyrimidines were prepared for their promising anticancer activity since they have common features with the naturally occurring anticancer drugs – colchicine, podophyllotoxin and combretastatin A-4 – most of them showed excellent anticancer activity.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► This work highlights synthesis of a series of novel chromenopyrimidines as anticancer agents. ► Screening the target compounds against human breast tumor cell line (MCF-7) was carried out. ► Five out of the goal compounds showed excellent activity than colchicine.