Literature DB >> 28964980

QSAR study of pyrazolo[4,3-e][1,2,4]triazine sulfonamides against tumor-associated human carbonic anhydrase isoforms IX and XII.

Joanna Matysiak1, Alicja Skrzypek2, Paweł Tarasiuk3, Mariusz Mojzych4.   

Abstract

The QSAR models for a set of pyrazolo[4,3-e][1,2,4]triazines incorporating benzenesulfonamide moiety combined directly with the heterocyclic ring or by NH linkage were generated. The inhibitory potency of compounds against human carbonic anhydrase isoforms IX and XII and antiproliferative activity against human MCF-7 cells were used as the dependent variables. The Codessa pro software was used for the descriptors calculation and the Best Multi-Linear Regression (BMLR) algorithm was employed to build the QSAR models. It was found that quantum descriptors are critical of the compounds activities. The selected models have good predictive accuracy confirmed by a set of the statistical quantities recommended by OECD.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Carbonic anhydrase; MLR; Molecular descriptor; Pyrazolotriazine sulfonamide; QSAR

Mesh:

Substances:

Year:  2017        PMID: 28964980     DOI: 10.1016/j.compbiolchem.2017.09.006

Source DB:  PubMed          Journal:  Comput Biol Chem        ISSN: 1476-9271            Impact factor:   2.877


  2 in total

1.  Design, Synthesis, and Biological Evaluation of 1,2,3-Triazole-Linked Triazino[5,6-B]Indole-Benzene Sulfonamide Conjugates as Potent Carbonic Anhydrase I, II, IX, and XIII Inhibitors.

Authors:  Krishna Kartheek Chinchilli; Andrea Angeli; Pavitra S Thacker; Laxman Naik Korra; Rashmita Biswas; Mohammed Arifuddin; Claudiu T Supuran
Journal:  Metabolites       Date:  2020-05-15

2.  The Effect of Novel 7-methyl-5-phenyl-pyrazolo[4,3-e]tetrazolo[4,5-b][1,2,4]triazine Sulfonamide Derivatives on Apoptosis and Autophagy in DLD-1 and HT-29 Colon Cancer Cells.

Authors:  Agnieszka Gornowicz; Anna Szymanowska; Mariusz Mojzych; Krzysztof Bielawski; Anna Bielawska
Journal:  Int J Mol Sci       Date:  2020-07-23       Impact factor: 5.923

  2 in total

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