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 IC50 <100 μM and IC50>100 μM. The most cytotoxic species is Cp(CpCO-NH-C6H4-(CH2)2CH3)TiCl2 with an IC50 of 24(2) μM, followed by Cp(CpCO-NH-C6H4-Br)TiCl2, IC50 of 46(4) μM and Cp(CpCO-NH-C6H4-OCF3)TiCl2, IC50 of 49(6) μM. There is no correlation between the nature of the para substituent on the phenyl ring and the cytotoxic properties on MCF-7 cell line.
Highlights
The development of efficient metal-based anticancer drugs currently still is a scientific challenge
In 1979, Kopf and Kopf-Maier opened a new chapter in the medicinal chemistry with the discovery of the first metallocene-based organometallic anticancer agent, titanocene dichloride, Cp2TiCl2
The fact that it possesses antitumor properties in cancer cell lines that are insensitive to cisplatin as well as lower toxic effects than cisplatin, has motivated the scientific community to continue investigating this species [1,2,3,4,5,6,7,8]
Summary
The development of efficient metal-based anticancer drugs currently still is a scientific challenge The design of such species requires careful selection of the metal center and ligands surrounding their coordination sphere in order to achieve the desired biological activity but, keeping in mind that it is desirable to maintain low-toxic side effects. In 1979, Kopf and Kopf-Maier opened a new chapter in the medicinal chemistry with the discovery of the first metallocene-based organometallic anticancer agent, titanocene dichloride, Cp2TiCl2 The fact that it possesses antitumor properties in cancer cell lines that are insensitive to cisplatin as well as lower toxic effects than cisplatin, has motivated the scientific community to continue investigating this species [1,2,3,4,5,6,7,8].
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