Synthesis and Anti-proliferative Evaluation of Naphthalimide-chalcone/pyrazoline Conjugates As Potential SERMs with Computational Validation

Overview

Journal RSC Adv

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2022 May 2

PMID 35493668

Authors

Shalini

Pankaj

Sourav Taru Saha

Mandeep Kaur

Ebenezer Oluwakemi

Paul Awolade

Parvesh Singh

Vipan Kumar

Affiliations

Soon will be listed here.

Abstract

A series of naphthalimide-chalcone/pyrazoline conjugates was prepared and evaluated for their anti-breast cancer potential against estrogen responsive, MCF-7 (ER+), and triple-negative, 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.

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