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二茂钛基酰胺对乳腺癌细胞系MCF-7的细胞毒性特性

Cytotoxic properties of titanocenyl amides on breast cancer cell line mcf-7.

作者信息

Gao Li Ming, Meléndez Enrique

机构信息

Department of Chemistry, University of Puerto Rico, P.O. Box 9019, Mayagüez, PR 00681, USA.

出版信息

Met Based Drugs. 2010;2010:286298. doi: 10.1155/2010/286298. Epub 2010 May 4.

Abstract

A new titanocenyl amide containing flavone as pendant group has been synthesized by reaction of titanocenyl carboxylic acid chloride and 7-Aminoflavone and structurally characterized by spectroscopic methods. This species and eight previously synthesized titanocenyl amide complexes have been tested in breast adenocarcinoma cancer cell line, MCF-7. The functionalization of titanocene dichloride with amides enhances the cytotoxic activity in MCF-7. Two sets of titanocenyl amides can be identified, with IC(50) <100 muM and IC(50)>100 muM. The most cytotoxic species is Cp(CpCO-NH-C(6)H(4)-(CH(2))(2)CH(3))TiCl(2) with an IC(50) of 24(2) muM, followed by Cp(CpCO-NH-C(6)H(4)-Br)TiCl(2), IC(50) of 46(4) muM and Cp(CpCO-NH-C(6)H(4)-OCF(3))TiCl(2), IC(50) of 49(6) muM. There is no correlation between the nature of the para substituent on the phenyl ring and the cytotoxic properties on MCF-7 cell line.

摘要

通过二茂钛酰氯与7-氨基黄酮反应合成了一种以黄酮为侧基的新型二茂钛酰胺,并采用光谱方法对其结构进行了表征。该化合物以及之前合成的八种二茂钛酰胺配合物已在人乳腺癌细胞系MCF-7中进行了测试。二氯二茂钛用酰胺进行官能化增强了在MCF-7中的细胞毒性活性。可以鉴定出两组二茂钛酰胺,其半数抑制浓度(IC50)<100μM和IC50>100μM。细胞毒性最强的化合物是Cp(CpCO-NH-C6H4-(CH2)2CH3)TiCl2,IC50为24(2)μM,其次是Cp(CpCO-NH-C6H4-Br)TiCl2,IC50为46(4)μM和Cp(CpCO-NH-C6H4-OCF3)TiCl2,IC50为49(6)μM。苯环上对位取代基的性质与对MCF-7细胞系的细胞毒性特性之间没有相关性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6d45/2863081/ac5e917a2288/MBD2010-286298.sch.001.jpg

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