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Synthesis and Antitumor Activities In Vitro of solanesylpiperazinotriamine

Chinese Chemical Letters 2006年第10期17卷 1301-1304页

作者： Chao Jie WANG Jian Hong WANG Ying GAN Zhi Yong CHEN Gang Jun DU Jin ZHAO College of Chemistry and Chemical Technology Henan University Kaifeng 475001 Key Lab of Special Function Material Henan University Kaifeng 475001 Medical College of Henan Unversity Kaifeng 475001

A series of novel antitumor agents-the solanesylpiperazinotriamine derivatives were designed and synthesized, their structures were confirmed by IR,^ 1H-NMR, MS, and element analysis. The preliminary tests showed that at low micromolar concentrations these compounds exhibited obvious toxicity on tumor cells in vitro, and the synergistic effect on clinical antitumor agent indicated that at noncytotoxic concentrations they also evidently enhanced the curative effect of vincristine.

关键词： solanesylpiperazinotriamine antitumor activity synergistic effect.

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Design,Synthesis and Synergistic Effects of Novel Derivatives of Solanesol

引用

Chemical Research in Chinese Universities 2007年第4期23卷 417-420页

作者： WANG Jian-hong WANG Chao-jie GAN Ying DU Gang-jun ZHAO Jin Key Lab of Special Functional Material College of Chemistry and Chemical Technology Medical College Henan Unversity Kaifeng 475001 P. R. China

To further explore the biological activities of solanesylamine derivatives, several novel solanesylpiperazinotri-amines and their amides were designed and synthesized, the chemical structures of target compounds were confirmed by IR, ^1H NMR, MS, and element analysis. The in vitro antitumor activities of the synthetic compounds were as-sessed by MTT test on L1210 and CHO cells. The preliminary results showed that at low micromolar concentrations these compounds exhibit obvious toxicity against tumor cells, and the synergistic effect on clinical antitumor agent in-dicated that at noncytotoxic concentrations, they also evidently enhance the curative effect of vincristine（VCR）. The synergistic effects of compounds 4a, 4c, and 9 were even superior to that of reference compound N,N＇-bis（3,4-dime-thoxybenzyl） -N- solanesyl-ethylenediamine （ SDB ）.

关键词： solanesylpiperazinotriamine Antitumor activity Synergistic effect

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