Open AccessDesign, synthesis, and biological evaluation of pyrazole-linked aloe emodin derivatives as potential anticancer agents
Author(s) -
G. Dileep Kumar,
Bandi Siva,
Sravanthi Vadlamudi,
Surendar Reddy Bathula,
Hashnu Dutta,
K. Suresh Babu
Publication year - 2021
Publication title -
rsc medicinal chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.754
H-Index - 55
ISSN - 2632-8682
DOI - 10.1039/d0md00315h
Subject(s) - aloe emodin , emodin , chemistry , apoptosis , pyrazole , ic50 , pharmacology , traditional medicine , cancer cell lines , cell cycle , cell culture , combinatorial chemistry , cancer cell , stereochemistry , in vitro , cancer , biochemistry , biology , medicine , genetics
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 IC 50 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.