title: Synthesis and characterization of 2-substituted benzimidazoles and their evaluation as anticancer agent.
abstract: In this work, we report a series of benzimidazole derivatives synthesized from benzene-1,2-diamine and aryl-aldehydes at room temperature. The synthesized compounds have been characterized on the basis of elemental analysis and various spectroscopic studies viz., IR, (1)H- and (13)C-NMR, ESI-MS as well by X-ray single X-ray crystallographic study. Interaction of these compounds with CT-DNA has been examined with fluorescence experiments and showed significant binding ability. All the synthesized compounds have been screened for their antitumor activities against various human cancer cell lines viz., Human breast adenocarcinoma cell line (MCF-7), Human leukemia cell line (THP-1), Human prostate cancer cell lines (PC-3) and adenocarcinomic human alveolar basal epithelial cell lines (A-549). Interestingly, all the compounds showed significant anticancer activity.
authors.affiliation: Department of Chemistry, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia. Electronic address: azam_res@yahoo.com.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Azam
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
authors.forename: Azmat Ali
authors.initials: AA
authors.lastname: Khan
authors.affiliation: Department of Chemistry, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
authors.forename: Saud I
authors.initials: SI
authors.lastname: Al-Resayes
authors.affiliation: Department of Chemistry, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
authors.forename: Mohammad Shahidul
authors.initials: MS
authors.lastname: Islam
authors.affiliation: Cancer Pharmacology Division, Indian Institute of Integrative Medicine, CSIR, Canal Road, Jammu 180001, India.
authors.forename: Ajit Kumar
authors.initials: AK
authors.lastname: Saxena
authors.affiliation: Department of Ag. Microbiology, Faculty of Ag. Sciences, Aligarh Muslim University, Aligarh, India.
authors.forename: Sourabh
authors.initials: S
authors.lastname: Dwivedi
authors.affiliation: Department of Ag. Microbiology, Faculty of Ag. Sciences, Aligarh Muslim University, Aligarh, India.
authors.forename: Javed
authors.initials: J
authors.lastname: Musarrat
authors.affiliation: Institute of General and Ecological Chemistry, Technical University of Lodz, Zeromskiego 116, 90-924 Lodz, Poland.
authors.forename: Agata
authors.initials: A
authors.lastname: Trzesowska-Kruszynska
authors.affiliation: Institute of General and Ecological Chemistry, Technical University of Lodz, Zeromskiego 116, 90-924 Lodz, Poland.
authors.forename: Rafal
authors.initials: R
authors.lastname: Kruszynski
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D018360:Crystallography, X-Ray; D004247:DNA / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D013057:Spectrum Analysis
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; D004247:DNA; C427203:calf thymus DNA
keywords: Anti-proliferative studies; Benzimidazoles; Crystal structure; DNA interactive studies