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新型Baylis-Hillman加合物衍生的β-肉桂基取代异吲哚酮衍生物的合成、抗结核和抗癌活性

Synthesis, antitubercular and anticancer activity of new Baylis-Hillman adduct-derived -cinnamyl-substituted isatin derivatives.

作者信息

Kumar Sriramoju Bharath, Ravinder Mettu, Kishore Golla, Jayathirtha Rao Vaidya, Yogeeswari Perumal, Sriram Darmarajan

机构信息

1Crop Protection Chemicals Division, Indian Institute of Chemical Technology, Uppal Road, Hyderabad, 500607 India.

2Department of Biochemistry, School of Life Sciences, University of Hyderabad, Hyderabad, 500046 India.

出版信息

Med Chem Res. 2014;23(4):1934-1940. doi: 10.1007/s00044-013-0787-x. Epub 2013 Sep 26.

DOI:10.1007/s00044-013-0787-x
PMID:32214765
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7080103/
Abstract

Baylis-Hillman adduct-derived -cinnamyl-substituted isatin derivatives were synthesized and evaluated for their antitubercular activity on HRv strain ATCC 27294 by agar dilution method. Anticancer activity for the same compounds was also screened on four different cell lines: Chinese hamster ovary (CHO cells), Colo 205 (human colon cancer), Sup-T1 (human lymphoma) and C6 glioma (rat glioma) by MTT assay method. The compounds (-) have shown significant activity against strain and the compound has shown specific cytotoxic activity.

摘要

合成了来源于Baylis-Hillman加合物的 -肉桂基取代异吲哚酮衍生物，并通过琼脂稀释法对其抗结核活性进行了评估，测试对象为结核分枝杆菌H37Rv菌株ATCC 27294。还通过MTT分析法在四种不同细胞系上筛选了这些化合物的抗癌活性：中国仓鼠卵巢细胞（CHO细胞）、结肠癌细胞系Colo 205、人淋巴瘤细胞系Sup-T1和大鼠胶质瘤细胞系C6。这些化合物（-）已显示出对该菌株的显著活性，且化合物 已显示出特定的细胞毒性活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c242/7080103/3db3aea17655/44_2013_787_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c242/7080103/76962b048b3e/44_2013_787_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c242/7080103/23452f145645/44_2013_787_Sch2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c242/7080103/3db3aea17655/44_2013_787_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c242/7080103/76962b048b3e/44_2013_787_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c242/7080103/23452f145645/44_2013_787_Sch2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c242/7080103/3db3aea17655/44_2013_787_Fig1_HTML.jpg

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