A series of benzo[d]imidazo[2,1-b]thiazole[BIT] derivatives were designed, synthesized and rectified for their cytotoxicity against cell line of HepG2 human liver carcinoma. Preliminary results showed that two of three examined [BIT] compounds a6 and b1b showed an importantant antiproliferation toward human cancer cell line (HepG2), where the IC50 values were 104.9 and 160.7 µg.ml−1 respectively. The derivative a6 could be considered as the probability leads up to developing them as a novel anti-cancer effective agent, while compound b1b appears to be active at a certain level of concentrations of HepG2 human cancer cell line. The studies suggested that derivative a6 has the potency to be employed up for further, especially against hepatocaricinoma.

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