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萘酰亚胺-查尔酮/吡唑啉共轭物作为潜在选择性雌激素受体调节剂的合成、抗增殖评估及计算验证

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

作者信息

Saha Sourav Taru, Kaur Mandeep, Oluwakemi Ebenezer, Awolade Paul, Singh Parvesh, Kumar Vipan

机构信息

Department of Chemistry, Guru Nanak Dev University Amritsar 143005 India

School of Molecular and Cell Biology, University of Witwatersrand Private Bag 3, Wits-2050 Johannesberg South Africa

出版信息

RSC Adv. 2020 Apr 21;10(27):15836-15845. doi: 10.1039/d0ra01822h.

DOI:10.1039/d0ra01822h
PMID:35493668
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9052575/
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.

摘要

制备了一系列萘二甲酰亚胺-查尔酮/吡唑啉共轭物，并评估了它们对雌激素反应性MCF-7（ER+）和三阴性MDA-MB-231（ER-）细胞系的抗乳腺癌潜力。基于连接子长度、苯环上的取代基和生成的官能团对抗增殖活性的影响，推导了构效关系（SAR）。对接模拟进一步描绘了设计分子与所选靶点的相互作用类型。本报告揭示了三唑连接的萘二甲酰亚胺-查尔酮/吡唑啉共轭物作为抗乳腺癌药物的应用范围。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/442e8f3b2a53/d0ra01822h-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/8a8cfca4ea6f/d0ra01822h-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/0df502ecefd1/d0ra01822h-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/f1b7d930556a/d0ra01822h-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/3b7f0cf11fe5/d0ra01822h-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/6345675012f8/d0ra01822h-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/db50b5b898ff/d0ra01822h-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/42b86cc5e67b/d0ra01822h-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/7193f02d8447/d0ra01822h-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/442e8f3b2a53/d0ra01822h-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/8a8cfca4ea6f/d0ra01822h-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/0df502ecefd1/d0ra01822h-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/f1b7d930556a/d0ra01822h-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/3b7f0cf11fe5/d0ra01822h-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/6345675012f8/d0ra01822h-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/db50b5b898ff/d0ra01822h-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/42b86cc5e67b/d0ra01822h-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/7193f02d8447/d0ra01822h-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0d7d/9052575/442e8f3b2a53/d0ra01822h-f6.jpg

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