Document Detail


Selective carbonic anhydrase IX inhibitors based on coumarin scaffold as promising antimetastatic agents: WO2012070024.
MedLine Citation:
PMID:  23387899     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Human carbonic anhydrase (hCA) IX is involved in tumorigenesis and metastasis through pathways modulating extracellular pH regulation and cell adhesion control. As a consequence, hCA IX represents a promising antitumor target for the development of new drugs in order to treat/image hypoxic cancers, and different agents targeting hCA IX are currently in Phase I - III clinical trials. Among novel chemotypes, coumarins and their congeners were shown to be potent and selective hCA IX inhibitors (CAI) in vitro with an alternative mechanism of action in respect to sulfonamide-based inhibitors. Furthermore, treatment of mice harboring CA IX-positive 4T1 mammary tumors with these selective coumarin-based CA IX inhibitors resulted in significant reduction of tumor growth and metastasis formation in both spontaneous and experimental models of metastasis.
Authors:
Simone Carradori
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-2-7
Journal Detail:
Title:  Expert opinion on therapeutic patents     Volume:  -     ISSN:  1744-7674     ISO Abbreviation:  Expert Opin Ther Pat     Publication Date:  2013 Feb 
Date Detail:
Created Date:  2013-2-7     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9516419     Medline TA:  Expert Opin Ther Pat     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
Sapienza University of Rome, Department of Drug Chemistry and Technologies , P.le A. Moro 5, 00185 Rome , Italy +0039 06 4969 3242 ; +0039 06 4969 3923 ; simone.carradori@uniroma1.it.
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