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

  • RSC Med Chem. 2021 Apr 26;12(5):791-796. doi: 10.1039/d0md00315h.
Guddeti Dileep Kumar  1  2 ,  Bandi Siva  1 ,  Sravanthi Vadlamudi  3 ,  Surendar Reddy Bathula  3 ,  Hashnu Dutta  4 ,  K Suresh Babu  1
Affiliations
  • 1. Centre for Natural Products & Traditional Knowledge, CSIR-Indian Institute of Chemical Technology Hyderabad 500007 India [email protected].
  • 2. Academy of Scientific and Innovative Research (AcSIR) Ghaziabad - 201002 India.
  • 3. Department of Organic Synthesis and Process Chemistry, CSIR-Indian Institute of Chemical Technology Hyderabad 500007 India.
  • 4. Department of Applied Biology, CSIR-Indian Institute of Chemical Technology Hyderabad-500 007 India.
PMID: 34124677 DOI: 10.1039/d0md00315h
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.