title: Benzothiazole derivatives bearing amide moiety: potential cytotoxic and apoptosis-inducing agents against cervical cancer.
abstract: Cervical cancer is a major cause of morbidity and mortality in women worldwide. In recent years, benzothiazole analogues have attracted considerable attention in anticancer research. Therefore, in this study, the earlier reported amide series of benzothiazole derivatives were investigated for their antiproliferative activity. The activity of amide derivatives was evaluated using the 3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, flow cytometric analysis, apoptosis assay, and DNA fragmentation on two human cervical cancer cell lines: SiHa and C33-A. The data reported from this investigation indicated that benzothiazole derivatives show pronounced cytotoxicity in the HPV16-positive SiHa cells compared with HPV-negative C-33A cells. The in-vitro cytotoxicity of the compounds on the HEK-293 noncancer cell line was evaluated to establish selectivity. Cells treated with benzothiazole derivatives showed prominent morphological features as evidenced by cell shrinkage, membrane blebbing, apoptotic nuclei, and DNA fragmentation. The benzothiazole derivatives show accumulation of cells in the sub-G1 and S-phase of the cell cycle in SiHa and C33-A, respectively. In addition, these derivatives exert their beneficial effect by inducing apoptosis, in the chemoprevention of cervical cancer cells, and were further ascertained using a DNA fragmentation assay. The compounds studied showed potent cytotoxic and apoptotic properties against SiHa and C33-A cancer cell lines and thus represent an excellent starting point for further optimization of therapeutically effective anticancer drugs.
authors.affiliation: aDepartment of Pharmaceutics, Indian Institute of Technology (BHU) bCancer Genetics Laboratory, Department of Molecular and Human Genetics, Banaras Hindu University, Varanasi, Uttar Pradesh, India.
authors.forename: Meenakshi
authors.initials: M
authors.lastname: Singh
authors.forename: Arusha
authors.initials: A
authors.lastname: Modi
authors.forename: Gopeshwar
authors.initials: G
authors.lastname: Narayan
authors.forename: Sushil K
authors.initials: SK
authors.lastname: Singh
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D052160:Benzothiazoles / Q000737:chemistry / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D053938:DNA Fragmentation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D005260:Female; D052162:Human papillomavirus 16 / Q000472:pathogenicity; D006801:Humans; D002583:Uterine Cervical Neoplasms / Q000188:drug therapy* / Q000821:virology
chemical_list: D000970:Antineoplastic Agents; D052160:Benzothiazoles