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Design and synthesis of 3-substituedmethylenethiochroman-4-ones as anticancer agents

Zheng-Yue Ma, Xing-Hua Zhang, Ya-Jun Zheng, Geng-Liang Yang

A series of 3-substituedmethylenethiochroman-4-ones were designed and synthesized, and their structures were confirmed by1H NMR, MS, IR, UV and elemental analysis. The evaluation result of their anticancer activity showed that almost all 3-chloromethylenethiochroman-4-ones exhibited high anticancer activity and their activitieswere all better than reference cisplatin, the IC50 of them against cancer cells was at the range of 0.80-9.17 ìg/mL. Thus they could be promising candidates for novel anticancer drugs. However, other 3-substituedmethyl- enethiochroman-4-ones had no activity against cancer cells, thus chloromethylene at the 3 position of thiochroman- 4-ones was the required active functional group.