Novel benzimidazole analogs as inhibitors of EGFR tyrosine kinase.

A series of new benzimidazole congeners were synthesized, and their structures were elucidated on the basis of elemental analyses and spectral studies (¹H NMR, FT-IR and EI-MS). Preliminary pharmacokinetic studies showed a promising outlook for further in vivo evaluation. The newly synthesized compounds were tested in vitro on human breast carcinoma cell line (MCF-7) in which EGFR is highly expressed. Most of the tested compounds exhibited antitumor activity with IC₅₀ values in the micro to nano molar range.