Abstract
Renal dipeptidase (RDP) is an enzyme overexpressed in benign and malignant colorectal tumors. In an effort to identify potent inhibitors of this enzyme, a series of aminophosphinic acid derivatives were synthesized. Compounds 3a and 3c in which the phenyl ring was para substituted with F and Br and olefin with Z geometry, showed better inhibitory activity against RDP enzyme (IC50 = 5-6 nM).
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Alkenes / chemistry
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Alkenes / pharmacology
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Bromides / chemistry
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Bromides / pharmacology
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Colorectal Neoplasms / pathology
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Dipeptidases / antagonists & inhibitors*
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Dipeptidases / metabolism
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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Fluorides / chemistry
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Fluorides / pharmacology
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Humans
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Inhibitory Concentration 50
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Kidney / enzymology
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Models, Chemical
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Phosphinic Acids / chemical synthesis*
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Phosphinic Acids / pharmacology
Substances
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Alkenes
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Bromides
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Enzyme Inhibitors
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Phosphinic Acids
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Dipeptidases
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dipeptidase
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Fluorides