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三芳基乙烯-吲哚啉-2,3-二酮分子共轭物：设计、合成、对接研究及抗增殖评估。

Triarylethylene-indolin-2,3-dione molecular conjugates: design, synthesis, docking studies and anti-proliferation evaluation.

作者信息

Kumar Sumit, Palma Gabriella, Perumal Shanen, Kaur Mandeep, Singh-Pillay Ashona, Raj Raghu, Singh Parvesh, Kumar Vipan

机构信息

Department of Chemistry, Guru Nanak Dev University Amritsar-143005 India +91 183 2258802-09 ext. 3320 +91 183 2258819-20

School of Molecular and Cell Biology, University of the Witswatersrand Private Bag 3, Wits-2050 Johannesburg South Africa.

出版信息

RSC Adv. 2019 Dec 20;9(72):42409-42414. doi: 10.1039/c9ra08776a. eCollection 2019 Dec 18.

DOI:10.1039/c9ra08776a
PMID:35542879
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9076587/
Abstract

A series of 1-1,2,3-triazole-linked ospemifene-isatin and -methylated ospemifene-isatin conjugates were synthesized and assayed for their anti-proliferative activities against estrogen-responsive as well as estrogen-non-responsive cells. The non-cytotoxic conjugate 14e, with an optimal combination of bromo substituents at the C-5/C-7 positions of isatin, proved to be a promising hit with an IC value of 31.62 μM against MCF-7 and 19.23 μM against MDA-MB-231. The observed anti-proliferative activities of active conjugates were further corroborated docking studies carried out on estrogen receptor subtypes α and β.

摘要

合成了一系列1,2,3-三唑连接的奥司米芬-异吲哚酮和甲基化奥司米芬-异吲哚酮共轭物，并测定了它们对雌激素反应性细胞和雌激素非反应性细胞的抗增殖活性。非细胞毒性共轭物14e在异吲哚酮的C-5/C-7位具有最佳的溴取代基组合，被证明是一个有前景的命中物，对MCF-7的IC值为31.62 μM，对MDA-MB-231的IC值为19.23 μM。对雌激素受体亚型α和β进行的对接研究进一步证实了活性共轭物观察到的抗增殖活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/dc8bd7bb01c1/c9ra08776a-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/afa85f6cdd70/c9ra08776a-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/13e682a901b4/c9ra08776a-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/50a552d592cf/c9ra08776a-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/f4a3de31c207/c9ra08776a-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/b3de9bbc5ff6/c9ra08776a-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/edef267e44ec/c9ra08776a-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/dc8bd7bb01c1/c9ra08776a-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/afa85f6cdd70/c9ra08776a-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/13e682a901b4/c9ra08776a-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/50a552d592cf/c9ra08776a-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/f4a3de31c207/c9ra08776a-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/b3de9bbc5ff6/c9ra08776a-s3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/edef267e44ec/c9ra08776a-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78f7/9076587/dc8bd7bb01c1/c9ra08776a-f4.jpg

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