Synthesis and in vitro anti-proliferative evaluation of naphthalimide-chalcone/pyrazoline conjugates as potential SERMs with computational validation.

ABSTRACT: A series of naphthalimide-chalcone/pyrazoline conjugates was prepared and evaluated for their anti-breast cancer potential against estrogen responsive, i.e. MCF-7 (ER+), and triple-negative, i.e. MDA-MB-231 (ER-), cell lines. The structure-activity-relationship (SAR) was deduced based on the influence of linker length, substituents on the phenyl ring and the generated functionalities, on anti-proliferative activities. Docking simulations further delineate the type of interactions of the designed molecules with the selected targets. This report discloses the scope of triazole tethered naphthalimide-chalcone/pyrazoline conjugates as anti breast cancer agents.

SUBMITTER: Shalini 

PROVIDER: S-EPMC9052575 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature