Literature DB >> 1271401

Inhibition of dihydrofolate reductase. Structure-activity correlations of quinazolines.

J Y Fukunaga, C Hansch, E E Steller.   

Abstract

A quantitative structure-activity relationship (QSAR) has been formulated for quinazolines causing 50% inhibition of liver dihydrofolate reductase. The QSAR for the quinazolines is compared with QSAR for triazine and pyrimidine inhibitors. The three QSAR suggest new possibilities for the design of inhibitors of mammalian dihydrofolate reductase.

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Year:  1976        PMID： 1271401     DOI： 10.1021/jm00227a006

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  3 in total

Review 1.  Chemical space of Escherichia coli dihydrofolate reductase inhibitors: New approaches for discovering novel drugs for old bugs.

Authors:  Bharath Srinivasan; Sam Tonddast-Navaei; Ambrish Roy; Hongyi Zhou; Jeffrey Skolnick
Journal:  Med Res Rev       Date:  2018-09-07       Impact factor: 12.944

2.  Ligand binding studies, preliminary structure-activity relationship and detailed mechanistic characterization of 1-phenyl-6,6-dimethyl-1,3,5-triazine-2,4-diamine derivatives as inhibitors of Escherichia coli dihydrofolate reductase.

Authors:  Bharath Srinivasan; Sam Tonddast-Navaei; Jeffrey Skolnick
Journal:  Eur J Med Chem       Date:  2015-09-05       Impact factor: 6.514

3.  Rational Design of Novel Allosteric Dihydrofolate Reductase Inhibitors Showing Antibacterial Effects on Drug-Resistant Escherichia coli Escape Variants.

Authors:  Bharath Srinivasan; João V Rodrigues; Sam Tonddast-Navaei; Eugene Shakhnovich; Jeffrey Skolnick
Journal:  ACS Chem Biol       Date:  2017-05-31       Impact factor: 5.100
  3 in total

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