Identifying the Issue
- Commonly used anti-cancer drugs come with side-effects.
- Need for better drugs to cure cancer.
Objective of the Research
- Pyrazoles are well-known pharmacophores. To explore pyrazole –andrographolide hybrids
- To synthesize novel pyrazole acetals of andrographolide and isoandrographolide with potent anti-cancer activity
Who should read this?
Research community working in cancer drug discovery and development, medicinal chemists, and pharmaceutical industry
Solution
Designed and synthesized novel pyrazole acetals of andrographolide and isoandrographolide with potent anti-cancer activity. Four compounds, having promising GI50s (50% growth inhibitory activity) on all 60-cell lines were selected for further in vitro studies. Out of these four compounds, compound 1g exhibited the best IC50 (3.08 µM) against the colon cancer cell line, HCT-116.
Key Features and Benefits
- Semi-synthetic natural products
- Potent anti-cancer activity against colon cancer cell line HCT-116
- Arresting in HCT-116 cell cycle progression in G0/G1 phase, cell apoptosis, and elevated levels of ROS in HCT-116 cells
- ADMET screening
Impact
- Synthesis of novel pyrazole acetals of andrographolide and isoandrographolide
- Investigated the synthesized compounds on 60 human cancer cell lines.
- Potent compound 1g induced G0/G1 phase arrest, cell apoptosis by increasing the levels of ROS in HCT-116 cells
Team
Siva Kumar Rokkam, Manohar Bhujel, Dolly Jain, Lakshminath Sripada, Srinivas Nanduri, Avinash Bajaj and Nageswara Rao Golakoti
Title of paper: “Synthesis of novel pyrazole acetals of andrographolide and isoandrographolide as potent anticancer agents”
Read Paper Here: https://pubs.rsc.org/en/content/articlelanding/2024/ra/d4ra00547c
