Synthesis and anticancer evaluation of bis(benzimidazoles), bis(benzoxazoles), and benzothiazoles

Four classes of UK-1 analogues were synthesized and their cytotoxicity testing against human A-549, BFTC-905, RD, MES-SA, and HeLa carcinoma cell lines was determined. The results revealed that UK-1 and four of these analogues (15–18) are potent against the cancer cell lines. In particular, compound 16 is more potent than UK-1 against A-549 and HeLa cell lines, and compounds 15, 17, and 18 selectively exhibit potent cytotoxic activity against the BFTV-905 cells (IC50 9.6 μM), A-549 cells (IC50 6.6 μM), and MES-SA cells (IC50 9.2 μM), respectively.

The syntheses of nineteen bis(benzimidazoles), bis(benzoxazoles), benzothiazoles, and their derivatives are described, and their in vitro antitumor activities (Against A-549, BFTC-905, RD, MES-SA, and HeLa cell lines) are evaluated.Figure optionsDownload as PowerPoint slide