Issue 29, 2015

SAR studies of 3,14,19-derivatives of andrographolide on anti-proliferative activity to cancer cells and toxicity to zebrafish: an in vitro and in vivo study

Abstract

Andrographolide is bestowed with an interesting pharmacophore and has attracted numerous studies on the design and synthesis of andrographolide derivatives. In this study, a small library of 3,14,19-modified derivatives of andrographolide were synthesized and tested for their in vitro inhibitory activities to cancer cell growth and proliferation and in vivo toxicities against zebrafish embryo development. Structure anti-proliferative activity and toxicity relationships in current data revealed that the property of a substituent, substituted positions, and 14-stereochemistry together determined a compound's in vitro anti-proliferative activity against cancer cells, the in vivo toxicity to zebrafish, and the selectivity between MDA-MB-231 and A549. Taken together, our SAR studies discovered some potential leads for further development of anticancer drugs and suggested that the direct and/or indirect toxicity of an active compound with andrographolide pharmacophore should be given attention.

Graphical abstract: SAR studies of 3,14,19-derivatives of andrographolide on anti-proliferative activity to cancer cells and toxicity to zebrafish: an in vitro and in vivo study

Supplementary files

Article information

Article type
Paper
Submitted
03 jan. 2015
Accepted
10 feb. 2015
First published
10 feb. 2015

RSC Adv., 2015,5, 22510-22526

Author version available

SAR studies of 3,14,19-derivatives of andrographolide on anti-proliferative activity to cancer cells and toxicity to zebrafish: an in vitro and in vivo study

Y. Peng, J. Li, Y. Sun, J. Y. Chan, D. Sheng, K. Wang, P. Wei, P. Ouyang, D. Wang, S. M. Y. Lee and G. Zhou, RSC Adv., 2015, 5, 22510 DOI: 10.1039/C5RA00090D

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