Carbonic anhydrase inhibitors. Inhibition of cytosolic isozymes I and II and transmembrane, cancer-associated isozyme IX with lipophilic sulfonamides

被引：29

作者：

Franchi, M

Vullo, D

Gallori, E

Pastorek, J

Russo, A

Scozzafava, A

Pastorekova, S

Supuran, CT

机构：

[1] Univ Florence, Lab Chim Bioinorgan, I-50019 Florence, Italy

[2] Univ Florence, Dipartimento Biol Anim & Genet, I-50122 Florence, Italy

[3] Slovak Acad Sci, Inst Virol, Bratislava 84245, Slovakia

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2003年 / 18卷 / 04期

关键词：

carbonic anhydrase; isozyme I; II; IX; lipophilic; sulfonamide; anticancer drug;

D O I：

10.1080/1475636031000138778

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：

A series of new compounds was obtained by reaction of aromatic/heterocyclic sulfonamides incorporating amino groups with N , N -diphenylcarbamoyl chloride and diphenylacetyl chloride. These sulfonamides were assayed for the inhibition of three carbonic anhydrase (CA, EC 4.2.1.1) isozymes: the cytosolic CA I and CA II, and the transmembrane, cancer-associated isozyme CA IX. Good inhibitors against all these isoforms were detected, and the inhibition profile of the newly investigated isozyme IX was observed to be different from that of the cytosolic isozymes, I and II. This may lead to the development of novel anticancer therapies based on the selective inhibition of CA IX.

引用

页码：333 / 338

页数：6

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