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1-1,2,3-三唑连接的硝基咪唑-异吲哚酮共轭物：合成、对接及对乳腺癌的抗增殖评估

1-1,2,3-Triazole Tethered Nitroimidazole-Isatin Conjugates: Synthesis, Docking, and Anti-Proliferative Evaluation against Breast Cancer.

作者信息

Kumar Sumit, Saha Sourav Taru, Gu Liang, Palma Gabriella, Perumal Shanen, Singh-Pillay Ashona, Singh Parvesh, Anand Amit, Kaur Mandeep, Kumar Vipan

机构信息

Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.

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

出版信息

ACS Omega. 2018 Sep 30;3(9):12106-12113. doi: 10.1021/acsomega.8b01513. Epub 2018 Sep 27.

DOI:10.1021/acsomega.8b01513
PMID:30320289
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6175498/
Abstract

1-1,2,3-Triazole tethered imidazole-isatin and imidazole-isatin-thiosemicarbazone conjugates were synthesized and evaluated against MCF-7 and MDA-MB-231 cell lines. Antiproliferative activities of the synthesized conjugates revealed an optimum combination of longer alkyl chain length as spacer and a halogen-substituent on the isatin ring as a pre-requisite for good activity. The compound with an optimum combination of chloro-substituent at C-5 position of isatin ring and a butyl chain length proved to be most active and noncytotoxic with IC of 54.25 and 26.12 μM against MCF-7 and MDA-MB-231 cell lines, respectively.

摘要

合成了1,2,3-三唑连接的咪唑-异吲哚酮和咪唑-异吲哚酮-硫代半卡巴腙共轭物，并针对MCF-7和MDA-MB-231细胞系进行了评估。合成共轭物的抗增殖活性表明，较长的烷基链长度作为间隔基以及异吲哚酮环上的卤素取代基的最佳组合是良好活性的先决条件。异吲哚酮环C-5位氯取代基和丁基链长度的最佳组合的化合物被证明活性最高且无细胞毒性，对MCF-7和MDA-MB-231细胞系的IC分别为54.25和26.12 μM。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/6646184/625c163e0872/ao-2018-01513a_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/6646184/06d7d54f597f/ao-2018-01513a_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/6646184/40204dc43959/ao-2018-01513a_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/6646184/cf0b08226439/ao-2018-01513a_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/6646184/ed2385521042/ao-2018-01513a_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/6646184/13e8e3672b1a/ao-2018-01513a_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/6646184/625c163e0872/ao-2018-01513a_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/6646184/06d7d54f597f/ao-2018-01513a_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/6646184/40204dc43959/ao-2018-01513a_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/6646184/cf0b08226439/ao-2018-01513a_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/6646184/ed2385521042/ao-2018-01513a_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/6646184/13e8e3672b1a/ao-2018-01513a_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/6646184/625c163e0872/ao-2018-01513a_0004.jpg

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