Design, synthesis, and biological evaluation of pyrazole-linked aloe emodin derivatives as potential anticancer agents. Issue 5 (26th April 2021)

• Record Type: Journal Article
• Authors: Kumar, Guddeti Dileep; Siva, Bandi; Vadlamudi, Sravanthi; Bathula, Surendar Reddy; Dutta, Hashnu; Suresh Babu, K.
• Is Part Of: RSC medicinal chemistry. Volume 12:Issue 5(2021)
• Page Start: 791
• Page End: 796
• Publication Date: 2021-04-26
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1039/d0md00315h
• Languages: English
• ISSNs: 2632-8682

Abstract

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 potential anticancer activity against a panel of cancer cell lines. 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.