Synthesis, Antitumor Activity, and SAR of N-Substituted [gamma]-Aminopropylsilatrane Derivatives

γ-Aminopropylsilatrane has been reported to possess biological activity against tumor cancer cells with low cytotoxicity in many kinds of silatranes. So some N-substituted γ-aminopropylsilatrane derivatives were synthesized and assayed by a primary anticancer screening against HT-29, Hela, and MDAMB...

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Bibliographic Details
Published in:Phosphorus, sulfur, and silicon and the related elements sulfur, and silicon and the related elements, 2014-04, Vol.189 (4), p.511
Main Authors: Ping, Guo, Yue-Wu, Wang, Xin-Tong, Luo, Xiao-Lu, Qi, Le-Ping, Hou, Zi-Xin, Xie, Fa-Qing, Ye
Format: Article
Language:English
Subjects:
Derivatives
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Summary:γ-Aminopropylsilatrane has been reported to possess biological activity against tumor cancer cells with low cytotoxicity in many kinds of silatranes. So some N-substituted γ-aminopropylsilatrane derivatives were synthesized and assayed by a primary anticancer screening against HT-29, Hela, and MDAMB435 cells by the use of the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method. The structures of these derivatives were confirmed by 1H NMR, electrospray ionization-mass spectrometry, and elemental analysis. The structure-activity relationship showed that the N-substituted derivatives exhibit better activity in which the γ-amino group of the silatrane is connected with stronger electron-withdrawing groups. [PUBLICATION ABSTRACT]
ISSN:1042-6507
1563-5325
DOI:10.1080/10426507.2013.829835