Abstract
A series ofN-1,3-benzothiazol-2-ylbenzamide derivatives were studied for their antiproliferative activity on human liver hepatocellular carcinoma (HepG2) and human breast cancer (MCF-7) cell lines. Most of them were found to show a prominent inhibitory effect on cell growth. Among the most active compounds,1kemerged for its proapoptotic effect that is particularly evident towards MCF-7 cancer cell lines.
Highlights
Cancer, a group of diseases characterized by uncontrolled growth of abnormal cells, is one of the major worldwide health problems
The tumor-specific action of most anticancer drugs has been attributed to their debilitating effects on actively proliferating cells, several studies suggest that anticancer agents induce apoptosis, a physiological mode of cell death in higher eukaryotes [1,2,3]
Anticancer activity on human carcinoma cell lines has been reported for a benzothiazole linked to a phthalimide moiety [15]; benzothiazole-2-thiol derivatives have been proposed as novel apoptosis inducers [16]
Summary
A group of diseases characterized by uncontrolled growth of abnormal cells, is one of the major worldwide health problems. Apoptosis has been recognized as a basic component in the pathogenesis of cancer It may be considered a defense mechanism to remove potentially dangerous cells, such as tumor cells. Our research group was interested in the design, synthesis, and biological evaluation of novel benzothiazole derivatives as antimicrobial agents [8, 10, 18]. Based on the results obtained by Wang et al [16] on a series of benzothiazole derivatives that exhibited antiproliferative activity against the human hepatocellular carcinoma cell line, HepG2, and the human mammary carcinoma cell line, MCF-7, we selected a small series of compounds among the previously synthesized benzothiazoles [18] for biological evaluation as potential apoptosis inducers. In order to improve structure-activity relationship (SAR) studies on this class of compounds, three additional analogues (1m,n and 2a) were synthesized and evaluated, too
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