1. New aromatic monoesters of alpha-aminoaralkylphosphonic acids as inhibitors of aminopeptidase N/CD13.
- Author
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Grzywa R, Sokol AM, Sieńczyk M, Radziszewicz M, Kościołek B, Carty MP, and Oleksyszyn J
- Subjects
- Angiogenesis Inhibitors chemical synthesis, Angiogenesis Inhibitors pharmacology, CD13 Antigens metabolism, Cell Line, Tumor, Humans, Phosphinic Acids chemical synthesis, Phosphinic Acids pharmacology, Protease Inhibitors chemical synthesis, Protease Inhibitors pharmacology, Structure-Activity Relationship, Tumor Necrosis Factor-alpha metabolism, Angiogenesis Inhibitors chemistry, CD13 Antigens antagonists & inhibitors, Phosphinic Acids chemistry, Protease Inhibitors chemistry
- Abstract
A series of new aromatic monoesters of alpha-aminoaralkylphosphonic acids were synthesized by selective hydrolysis of corresponding aromatic diesters of alpha-aminoaralkylphosphonic acids. New potential inhibitors of aminopeptidase N/CD13, an enzyme important in tumour angiogenesis, were developed. Some derivatives of the homophenylalanine and norleucine related monoaryl phosphonates displayed higher inhibition potency than corresponding alpha-aminoaralkylphosphonic acids toward aminopeptidase N/CD13. The effect of one of the new inhibitors on the growth of human PANC-1 and HT-1080 cell lines was examined, either alone or in combination with TNF-alpha., (Copyright 2010 Elsevier Ltd. All rights reserved.)
- Published
- 2010
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