Synthesis and Promising in Vitro Antiproliferative Activity of Sulfones of a 5-Nitrothiazole Series

被引：14

作者：

Cohen, Anita ^{[1
,2
]}

Crozet, Maxime D. ^{[1
]}

Rathelot, Pascal ^{[1
]}

Azas, Nadine ^{[2
]}

Vanelle, Patrice ^{[1
]}

机构：

[1] Aix Marseille Univ, CNRS, ICR, Lab Pharmacochim Radicalaire,Fac Pharm,UMR 7273, F-13385 Marseille 05, France

[2] Aix Marseille Univ, Fac Pharm, IP TPT UMR MD3, F-13385 Marseille 05, France

来源：

MOLECULES | 2013年 / 18卷 / 01期

关键词：

5-nitrothiazole; sulfones; microwave irradiation; in vitro antiproliferative; HepG2 cell line; activity cellular specificity; MICROWAVE-PROMOTED SYNTHESIS; ASSISTED SYNTHESIS; SRN1; REACTIONS; DERIVATIVES; REACTIVITY; BETA;

D O I：

10.3390/molecules18010097

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis in water of new sulfone derivatives under microwave irradiation is described. This eco-friendly process leads to the expected products in good yields by reaction of various substituted sulfinates (commercially available or obtained by reduction of the corresponding sulfonyl chlorides) with 4-chloromethyl-2-methyl-5-nitro-1,3-thiazole. In order to evaluate the antiproliferative effect of these compounds, several sulfone derivatives are also dichlorinated on the C alpha next to the sulfonyl group. An evaluation on different cancer cell lines reveals promising selective in vitro antiproliferative activity toward HepG2 human cell lines by dihydrogenated sulfones, suggesting further research should be to explore their anticancer potential in the treatment of liver cancer.

引用

页码：97 / 113

页数：17

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