NDLI: Metronidazole-coumarin conjugates and 3-cyano-7-hydroxy-coumarin act as isoform-selective carbonic anhydrase inhibitors

Content Provider	Taylor & Francis Online
Author	Maresca, Alfonso Winum, Jean-Yves Supuran, Claudiu T. Bonneau, Adeline
Abstract	Reaction of 6-/7-hydroxycoumarin with metronidazole afforded conjugates which incorporate two interesting chemotypes which may inhibit carbonic anhydrases (CAs, EC 4.2.1.1) due to the presence of the coumarin moiety and possess radiosensitizing effects due to the presence of the nitroazole. Another dual action compound, which may act both as CA inhibitor as well as monocarboxylate transporter inhibitor, is 3-cyano-7-hydroxy-coumarin. These compounds have been investigated as inhibitors of 11 human CA isoforms. Submicromolar inhibition was observed against hCA VA, hCA VB, hCA VI, hCA VII, hCA IX, hCA XII and hCA XIV, whereas isoforms hCA I, II and XIII were not inhibited by these compounds. These coumarins thus act as isoform-selective CA inhibitors with the possibility to target isoforms involved in pathologies such as obesity (CA VA/VB) or cancer (CA IX and XII) without inhibiting the physiologically dominant, highly abundant hCA I and II.
Starting Page	397
Ending Page	401
Page Count	5
File Format	PDF HTM / HTML
ISSN	14756366 14756374
DOI	10.3109/14756366.2011.650692
Journal	Journal of Enzyme Inhibition and Medicinal Chemistry
Volume Number	28
Issue Number	2
Language	English
Publisher	Taylor & Francis
Publisher Date	2013-02-05
Access Restriction	Open
Subject Keyword	Carbonic anhydrase Coumarin Nitroazole Metronidazole Enzyme inhibitor Monocarboxylate transporter
Content Type	Text
Resource Type	Article
Subject	Drug Discovery Medicine Pharmacology

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