title: Inhibition of T24 and RT4 Human Bladder Cancer Cell Lines by Heterocyclic Molecules.
abstract: BACKGROUND Bladder cancer is a major widespread tumor of the genitourinary tract. Around 30% of patients with superficial cancers develop invasive and metastatic pathology. MATERIAL AND METHODS Some new heterocyclic 4-methyl coumarin derivatives were designed using molecular modeling studies to evaluate their potential against bladder cancer lines T24 and RT-4. The designed compounds that showed good binding affinity to T24 and RT4 were synthesized, with excellent yield. The synthesized compounds after structural evaluation were further evaluated for their antiproliferative activity by cell viability assay, cell cycle analysis, and apoptosis assay. RESULTS The compound BC-14 exhibited the best cytotoxicity against T24 cells, but were not highly active against RT4 cells. CONCLUSIONS The results of the present study may suggest the selectivity pattern of the synthesized compounds. These results should be explored further with chemical modification for other cancer types.
authors.affiliation: Department of Urinary Surgery, Linyi People's Hospital, Linyi, Shandong, China (mainland).
authors.forename: Zhi-Feng
authors.initials: ZF
authors.lastname: Zhao
authors.affiliation: Department of Urinary Surgery, Linyi People's Hospital, Linyi, Shandong, China (mainland).
authors.forename: Kai
authors.initials: K
authors.lastname: Wang
authors.affiliation: Department of Urinary Surgery, Linyi People's Hospital, Linyi, Shandong, China (mainland).
authors.forename: Feng-Fu
authors.initials: FF
authors.lastname: Guo
authors.affiliation: Department of Urinary Surgery, Linyi People's Hospital, Linyi, Shandong, China (mainland).
authors.forename: Hua
authors.initials: H
authors.lastname: Lu
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D018360:Crystallography, X-Ray; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D062105:Molecular Docking Simulation; D001749:Urinary Bladder Neoplasms / Q000473:pathology*
chemical_list: D000970:Antineoplastic Agents; D006571:Heterocyclic Compounds