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Novel sulfonamide bearing coumarin scaffolds as selective inhibitors of tumor associated carbonic anhydrase isoforms IX and XII.

Abstract：

:Four novel scaffolds consisting of total 24 compounds (1a-1o, 2a-2c, 3a-3c and 4a-4c) bearing aromatic sulfonamide and coumarin moieties connected through various linkers were synthesized in order to synergize the inhibition potential of both the moieties against four selected human carbonic anhydrase isoforms (hCA I, II, IX & XII). All compounds were found to be potent inhibitors of tumor associated hCA IX & XII while at the same time required large amounts to inhibit off-targeted housekeeping hCA I & II. Selectivity was more pronounced against hCA II over I, and hCA XII over IX. Results were compared with antitumor drug acetazolamide. One derivative 2b of series 2 was found to be a better selective inhibitor of hCA IX and XII.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Chandak N,Ceruso M,Supuran CT,Sharma PK

doi

10.1016/j.bmc.2016.04.052

subject

Has Abstract

pub_date

2016-07-01 00:00:00

pages

2882-2886

issue

13

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)30295-4

journal_volume

24

pub_type

杂志文章

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