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作为潜在抗癌剂的吡唑连接的芦荟大黄素衍生物的设计、合成及生物学评价

Design, synthesis, and biological evaluation of pyrazole-linked aloe emodin derivatives as potential anticancer agents.

作者信息

Kumar Guddeti Dileep, Siva Bandi, Vadlamudi Sravanthi, Bathula Surendar Reddy, Dutta Hashnu, Suresh Babu K

机构信息

Centre for Natural Products & Traditional Knowledge, CSIR-Indian Institute of Chemical Technology Hyderabad 500007 India

Academy of Scientific and Innovative Research (AcSIR) Ghaziabad - 201002 India.

出版信息

RSC Med Chem. 2021 Apr 26;12(5):791-796. doi: 10.1039/d0md00315h. eCollection 2021 May 26.

DOI:10.1039/d0md00315h
PMID:34124677
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8152798/
Abstract

In connection with our continuous efforts to generate new derivatives from lead compounds isolated from traditional medicinal plants, a series of aloe-emodin derivatives () were synthesized and assessed for their potential anticancer activity against a panel of cancer cell lines. The results showed that most of the derivatives are more active than the aloe-emodin and particularly, and manifested potent activity with IC values of 1.32 & 1.6 μM and 0.99 & 2.68 μM against MDA-MB-231 and MCF-7 cells, respectively. Moreover, and induce early and late apoptosis as well as arrest the cell cycle at the G2/M phase in MDA-MB-231 cells. In conclusion, the results confirmed that the aloe-emodin derivatives could be a potential drug candidate for better treatment of breast cancer.

摘要

为了持续努力从传统药用植物中分离出的先导化合物生成新的衍生物，我们合成了一系列芦荟大黄素衍生物（），并评估了它们对一组癌细胞系的潜在抗癌活性。结果表明，大多数衍生物比芦荟大黄素更具活性，特别是，和表现出强大的活性，对MDA-MB-231和MCF-7细胞的IC值分别为1.32和1.6 μM以及0.99和2.68 μM。此外，和诱导MDA-MB-231细胞早期和晚期凋亡，并使细胞周期停滞在G2/M期。总之，结果证实芦荟大黄素衍生物可能是更好治疗乳腺癌的潜在药物候选物。

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