Literature DB >> 6694162

Inhibition of human dihydrofolate reductase by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(substituted-phenyl)-s-triazine s. A quantitative structure-activity relationship analysis.

B A Hathaway, Z R Guo, C Hansch, T J Delcamp, S S Susten, J H Freisheim.   

Abstract

The inhibitory activity of 101 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(substituted-phenyl)-s-triazines against purified dihydrofolate reductase from human lymphoblastoid cell (WIL 2) has been studied. From the obtained Kiapp values, quantitative structure-activity relationships (QSAR) have been derived. The QSAR from human dihydrofolate reductase are compared with QSAR for triazines inhibiting bovine and murine tumor DHFR, as well with QSAR for their inhibitory action on murine tumor cell culture.

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Year:  1984        PMID： 6694162     DOI： 10.1021/jm00368a007

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


  4 in total

1.  CoMFA analysis of tgDHFR and rlDHFR based on antifolates with 6-5 fused ring system using the all-orientation search (AOS) routine and a modified cross-validated r(2)-guided region selection (q(2)-GRS) routine and its initial application.

Authors:  Aleem Gangjee; Xin Lin; Lisa R Biondo; Sherry F Queener
Journal:  Bioorg Med Chem       Date:  2010-01-06       Impact factor: 3.641

Review 2.  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

3.  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

4.  Structure-activity relationship and comparative docking studies for cycloguanil analogs as PfDHFR-TS inhibitors.

Authors:  Prasanna Sivaprakasam; Perrer N Tosso; Robert J Doerksen
Journal:  J Chem Inf Model       Date:  2009-07       Impact factor: 4.956
  4 in total

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