title: Benzimidazole clubbed with triazolo-thiadiazoles and triazolo-thiadiazines: new anticancer agents.
abstract: Two series of Benzimidazole clubbed with triazolo-thiadiazoles (5a-q, 5r, 5s and 5x-a(1)) and triazolo-thiadiazines (5t-w) were synthesized with an aim to produce promising anticancer agents. In vitro anticancer activities of synthesized compounds were investigated at the National Cancer Institute (NCI) against NCI 60 cell line panel; results showed good to remarkable broad-spectrum anticancer activity. Among them, the compound 5h (NCS: 760452, 1-(1H-benzo [d] imidazol-2-yl)-3-(6-(2,4-dichlorophenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl) propan-1-one) exhibited significant growth inhibition with GI50 values ranging from 0.20 to 2.58 μM and found superior selectivity for the leukemia cell lines and further screened at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 μM). The 5h may possibly be used as lead compound for developing new anticancer agents.
authors: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi 110062, India. drasifhusain@yahoo.com
authors: Asif
authors: A
authors: Husain
authors: Mohd
authors: M
authors: Rashid
authors: M
authors: M
authors: Shaharyar
authors: Anees A
authors: AA
authors: Siddiqui
authors: Ravinesh
authors: R
authors: Mishra
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000737:chemistry*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013829:Thiadiazines / Q000737:chemistry*; D013830:Thiadiazoles / Q000737:chemistry*; D014230:Triazoles / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; D013829:Thiadiazines; D013830:Thiadiazoles; D014230:Triazoles; C031000:benzimidazole