Synthesis of 12-quinoline substituted andrographolide derivatives and their preliminary evaluation as anti-aggregation drugs
Xue Li
A * , Jiafeng Yu A , Xianhao Wu A , Cui Hu A and Xiaoqing Wang A
+ Author Affiliations
- Author Affiliations
A Drug Research Center, Jiangxi Provincial Institute of Traditional Chinese Medicine, Nanchang 330046, PR China.
Australian Journal of Chemistry 76(2) 100-114 https://doi.org/10.1071/CH22248
Submitted: 28 November 2022 Accepted: 6 February 2023 Published: 28 February 2023
© 2023 The Author(s) (or their employer(s)). Published by CSIRO Publishing. This is an open access article distributed under the Creative Commons Attribution-NonCommercial 4.0 International License (CC BY-NC)
Abstract
Based on the structure of the natural product andrographolide, a series of novel 12-quinoline substituted derivatives 9 were designed and synthesized. In preliminary biological evaluation, these synthesized compounds showed prominent anti-platelet aggregation activities in response to thrombin and adenosine diphosphate (ADP) agonists. Among them, compound 9o (inhibition rate 55.73%, IC50 0.36 µM/L) had the highest anti-platelet aggregation activity induced by ADP. Compound 9q (inhibition rate 54.31%, IC50 0.30 µM/L) showed the highest anti-platelet aggregation activity induced by thrombin. Most of the derivatives had no significant cytotoxicity. Our research results provide a novel candidate drug structure for anti-platelet aggregation and enrich the scope of application of andrographolide derivatives.
Keywords: 12-quinoline substituted andrographolide derivatives, ADP, andrographolide, anti-platelet aggregation, design, Inhibition rate, synthesis, Thrombin.
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