title: Novel benzimidazole analogs as inhibitors of EGFR tyrosine kinase.
abstract: 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.
authors.forename: Soni
authors.initials: S
authors.lastname: Yadav
authors.forename: Deepa
authors.initials: D
authors.lastname: Sinha
authors.forename: Sanjay K
authors.initials: SK
authors.lastname: Singh
authors.forename: Vinay K
authors.initials: VK
authors.lastname: Singh
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D001562:Benzimidazoles / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D001940:Breast / Q000187:drug effects; D001943:Breast Neoplasms / Q000188:drug therapy / Q000201:enzymology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000378:metabolism; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011817:Rabbits
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; D066246:ErbB Receptors