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.

Keywords: Cell Cycle - drug effects, Cell Survival - drug effects, Crystallography, X-Ray, Heterocyclic Compounds - pharmacology, Molecular Docking Simulation, Urinary Bladder Neoplasms - pathology