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Synthesis & Anticancer Evaluation of New Substituted 2-(3,4-Dimethoxyphenyl)benzazoles.

Medicinal Chemistry 2018 July 12
A series of new 2-(3,4-dimethoxyphenyl)-1H-benz(or pyrido)imidazoles 2, 4-25 were synthesized and evaluated for their anticancer and antimicrobial activities. The NMR assignments of the dimethoxy groups were established by the NOESY spectra. Compound 12 bearing two chlorine atoms at the 5(4) and 7(6) positions of the benzene moiety of benzimidazole was found the most potent analogue, against A549 cells with the GI50 value of 1.5 µg/mL. Moreover, compound 24 showed remarkable cell growth inhibition against MCF-7 and HeLa cells with the GI50 values of 7 and 5.5 µg/mL, respectively. The synthesized compounds have no important antibacterial and antifungal activities.

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