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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
Peng Y.1; Li J.2; Sun Y.1; Chan J.Y.-W.2; Sheng D.1; Wang K.1; Wei P.1; Ouyang P.1; Wang D.1; Lee S.M.Y.2; Zhou G.-C.1
2015
Source PublicationRSC Advances
ISSN20462069
Volume5Issue:29Pages:22510-22526
AbstractAndrographolide 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英語
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Cited Times [WOS]:16   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Affiliation1.Nanjing Tech University
2.University of Macau
Recommended Citation
GB/T 7714
Peng Y.,Li J.,Sun Y.,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 Peng Y..,Li J..,Sun Y..,Chan J.Y.-W..,Sheng D..,...&Zhou G.-C..(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 Peng Y.,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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