Issue 5, 2021

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

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 (6a–6e) 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, 6b and 6e manifested potent activity with IC50 values of 1.32 & 1.6 μM and 0.99 & 2.68 μM against MDA-MB-231 and MCF-7 cells, respectively. Moreover, 6b and 6e 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.

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

Supplementary files

Article information

Article type
Research Article
Submitted
16 Sep 2020
Accepted
15 Mar 2021
First published
26 Apr 2021

RSC Med. Chem., 2021,12, 791-796

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

G. D. Kumar, B. Siva, S. Vadlamudi, S. R. Bathula, H. Dutta and K. Suresh Babu, RSC Med. Chem., 2021, 12, 791 DOI: 10.1039/D0MD00315H

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