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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
Yuran Peng1; Jingjing Li2; Yicheng Sun1; Judy Yuet-Wa Chan2; Dekuan Sheng1; Kun Wang1; Ping Wei3; Pingkai Ouyang3; Decai Wang1; Simon Ming Yuen Lee2; Guo-Chun Zhou1
2015
Source PublicationRSC Advances
ISSN20462069
Volume5Issue:29Pages:22510-22526
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. This journal is

DOI10.1039/c5ra00090d
URLView the original
Language英语
WOS Research AreaChemistry
WOS SubjectChemistry, Multidisciplinary
WOS IDWOS:000350643700029
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Cited Times [WOS]:18   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorDecai Wang; Simon Ming Yuen Lee; Guo-Chun Zhou
Affiliation1.School of Pharmaceutical Sciences, Nanjing Tech University, Nanjing 211816, Jiangsu, China
2.State Key Laboratory of Quality Research in Chinese Medicine and Institute of Chinese Medical Sciences, University of Macau, Macao, China
3.College of Biotechnology and Pharmaceutical Engineering, Nanjing Tech University, Nanjing 211816, Jiangsu, China
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Yuran Peng,Jingjing Li,Yicheng Sun,et al. 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[J]. RSC Advances,2015,5(29):22510-22526.
APA Yuran Peng.,Jingjing Li.,Yicheng Sun.,Judy Yuet-Wa Chan.,Dekuan Sheng.,...&Guo-Chun Zhou.(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.RSC Advances,5(29),22510-22526.
MLA Yuran Peng,et al."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".RSC Advances 5.29(2015):22510-22526.
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