title: Design, synthesis and molecular modeling studies of few chalcone analogues of benzimidazole for epidermal growth factor receptor inhibitor in search of useful anticancer agent.
abstract: In the present investigation, few 3-(substitutedphenyl)-1-[2-(1-hydroxy-ethyl)]-1H-benzimidazol-1-yl)prop-2-en-1-ones are EGFR antagonist are designed, by molecular docking analysis. The synthesized compounds were tested for their in vitro anticancer activity by propidium iodide fluorescent assay and Trypan blue viability assay against colorectal cancer cell lines (HCT116) and non-small cell lung cancer cell lines (H460). Human Epithelial Kidney cell lines (HEK) are used as normal cell lines for studying effect of drug on non-cancerous cells within human body. Evaluation of cytotoxic studies of synthesized compounds CHL(1-8) reveal that compound CHL1 [IC50=7.31 and 10.16 μM against HCT116 and H460 cell lines respectively, by PI assay] and CHL8 [IC50=12.52 and 6.83 against HCT116 and H460μM cell lines respectively] possess promising cytotoxic activity.
authors.affiliation: Department of Pharmaceutical Chemistry, Bhujbal Knowledge City, MET's Institute of Pharmacy Adgaon, Nashik, MS, India. Electronic address: santosh_chhajed@rediffmail.com.
authors.forename: Santosh S
authors.initials: SS
authors.lastname: Chhajed
authors.affiliation: Department of Pharmaceutical Chemistry, Bhujbal Knowledge City, MET's Institute of Pharmacy Adgaon, Nashik, MS, India.
authors.forename: Sandeep S
authors.initials: SS
authors.lastname: Sonawane
authors.affiliation: Department of Pharmacology, SNJB's Shriman Sureshdada Jain College of Pharmacy, Neminagar, Chandwad, Nashik, MS, India.
authors.forename: Chandrashekhar D
authors.initials: CD
authors.lastname: Upasani
authors.affiliation: Department of Pharmaceutics, MET's Institute of Pharmacy Adgaon, Nashik, MS, India.
authors.forename: Sanjay J
authors.initials: SJ
authors.lastname: Kshirsagar
authors.affiliation: School of biotechnology and bioinformatics, D.Y. Patil University, Navi Mumbai-15, MS, India.
authors.forename: Pramodkumar P
authors.initials: PP
authors.lastname: Gupta
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000737:chemistry*; D002460:Cell Line; D045744:Cell Line, Tumor; D047188:Chalcones / Q000737:chemistry*; D015195:Drug Design; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D006801:Humans; D008958:Models, Molecular; D062105:Molecular Docking Simulation
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; D047188:Chalcones; D066246:ErbB Receptors
keywords: Anticancer activity; EGFR; Flow cytometry; Molecular docking