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Design, synthesis, antitumor activity and mode of action of novel oxiranyl and thiiranyl phenol derivatives

Title: Design, synthesis, antitumor activity and mode of action of novel oxiranyl and thiiranyl phenol derivatives

Authors: Yang Z.; Kang J.-A.; Kim W.H.; Park A.-Y.; Kim H.S.; Kim J.; Kim J.-A.; Gong P.; Jeong L.S.; Moon H.R.

Citation: Bulletin of the Korean Chemical Society vol. 30, no. 7, pp. 1463 - 1469

Abstract: Eleven novel oxiranyl and thiiranyl phenolic compounds were synthesized as potential antitumor agents using epichlorohydrin and epithiohydrin in the presence of K 2CO 3. Cytotoxicities were found in range of IC 50 values of 2.5-14.8 μM, which was partially attributed to topoisomerase II inhibition. Bis-thiiranyl anthraquinone analog, 19 showed more cytotoxicity against MDA-MB-231 (breast cancer cell) and PC3 (prostate cancer cell) after 24 and/or 48 h and more potent topoisomerase II inhibitory activity than etoposide.