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Evaluation and SAR analysis of the cytotoxicity of tanshinones in colon cancer cells

Chinese Journal of Natural Medicines 2014年第3期12卷 167-171页

作者： WANG Lin LIU An ZHANG Fei-Long Yeung John H.K. LI Xu-Qin CHO Chi-Hin School of Biomedical Sciences Faculty of MedicineThe Chinese University of Hong Kong Institute of Chinese Materia Medica China Academy of Chinese Medical Sciences Department of Chemistry University of Science and Technology Beijing

AIM:This study was designed to evaluate the anti-cancer actions of tanshinone I and tanshinone IIA,and six derivatives of tanshinone IIA on normal and cancerous colon *** activity relationship(SAR) analysis was conducted to delineate the significance of the structural modifications of tanshinones for improved anti-cancer ***:Tanshinone derivatives were designed and synthesized according to the *** cytotoxicity of different compounds on colon cancer cells was determined by the MTT *** activity of the tanshinones was measured by flow cytometry(FCM).RESULTS:Tanshinone I and tanshinone IIA both exhibited significant cytotoxicity on colon cancer *** are more effective in p53+/+ colon cancer cell *** was also noted that the anti-cancer activity of tanshinone I was more potent and *** of the derivatives of tanshinone IIA(N1 and N2) also exhibited cytotoxicity on colon cancer ***:The anti-colon cancer activity of tanshinone I was more potent and selective than tanshinone IIA,and is p53 *** derivatives obtained by structural modifications of tanshinone IIA exhibited lower cytotoxicity on both normal and colon cancer *** steric and electronic characteristics point of view,it was concluded that structural modifications of ring A and furan or dihydrofuran ring D on the basic structure of tanshinones influences the *** increase of the delocalization of the A and B rings could enhance the cytotoxicity of such compounds,while a non-planar and small sized D ring region would provide improved anti-cancer activity.

关键词： Tanshinones synthetic derivatives Colon cancer Cytotoxicity SAR analysis

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