title: Synthesis and in vitro antitumor evaluation of primary amine substituted quinazoline linked benzimidazole.
abstract: By combining the structural features of quinazoline and benzimidazole, new hybrid regioisomeric molecules with substituted primary amines have been synthesized. Evaluation of these molecules over 60 cancer cell line panel has identified three molecules as most potent anticancer agents. Compound 10 showed ten and eleven folds more activity than respective quinazoline and benzimidazole class of compounds with GI50 value of 1.64 μM. Compound 11 (GI50 value of 0.81 μM) showed almost twenty and twenty-two fold more activity than quinazoline and benzimidazole analogue, respectively while compound 12 (GI50 value of 4.52 μM) has four fold more activity than quinazoline and benzimidazole analogue. In vitro evaluation of compound 11 exhibited remarkable anticancer activity towards colon cancer cell lines and prostate cancer cell lines at five dose concentrations with GI50 values of 0.34 and 0.31 μM, respectively.
authors.affiliation: School of Chemistry and Biochemistry, Thapar University, Patiala 147004, India. Electronic address: kpaul@thapar.edu.
authors.forename: Kamaldeep
authors.initials: K
authors.lastname: Paul
authors.affiliation: School of Chemistry and Biochemistry, Thapar University, Patiala 147004, India.
authors.forename: Alka
authors.initials: A
authors.lastname: Sharma
authors.affiliation: School of Chemistry and Biochemistry, Thapar University, Patiala 147004, India.
authors.forename: Vijay
authors.initials: V
authors.lastname: Luxami
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006801:Humans; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; D011799:Quinazolines; C031000:benzimidazole
keywords: Antitumor activity; Benzimidazole; Primary amines; Quinazoline