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Synthesis of 1,4-bis(indolin-1-ylmethyl)benzene Derivatives and Their Structure-Activity Relationships for the Interaction of Human Carbonic Anhydrase Isoforms I and II

Synthesis of 1,4-bis(indolin-1-ylmethyl)benzene Derivatives and Their Structure-Activity Relationships for the Interaction of Human Carbonic Anhydrase Isoforms I and II

Oktay Talaz, Hüseyin Cavdar, Serdar Durdagi, Hacer Azak, Deniz Ekinci

Bioorg Med Chem. 2013 Mar 15;21(6):1477-82.

PMID: 23121721

Abstract:

Several 1,4-bis(indolin-1-ylmethyl)benzene-based compounds containing substituents such as five, six and seven cyclic derivatives on indeno part (9a-c) were prepared and tested against two members of the pH regulatory enzyme family, carbonic anhydrase (CA). The inhibitory potencies of the compounds at the human isoforms hCA I and hCA II targets were analyzed and KI values were calculated. KI values of compounds for hCA I and hCA II human isozymes were measured in the range of 39.3-42.6μM and 0.17-0.29μM, respectively. The structurally related compound indole was also tested in order to understand the structure-activity relationship. Most of the compounds showed good CA inhibitory efficacy. In silico docking studies of these derivatives within hCA I and II were also carried out and results are supported the kinetic assays.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP9001030-A	Carbonic Anhydrase Isozyme II human		9001-03-0	Price

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