Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement

Testing of an expanded, 800-compound set of analogues of the earlier described Strecker-type α-aminonitriles (selected from publicly available Enamine Ltd. Screening Collection) in thermal shift assay against bovine carbonic anhydrase (bCA) led to further validation of this new class of inhibitors a...

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Autores principales: Krasavin, Mikhail, Kalinin, Stanislav, Zozulya, Sergey, Griniukova, Anastasia, Borysko, Petro, Angeli, Andrea, Supuran, Claudiu T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2019
Materias:
Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6882446/
https://www.ncbi.nlm.nih.gov/pubmed/31752557
http://dx.doi.org/10.1080/14756366.2019.1693556
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author Krasavin, Mikhail
Kalinin, Stanislav
Zozulya, Sergey
Griniukova, Anastasia
Borysko, Petro
Angeli, Andrea
Supuran, Claudiu T.
author_facet Krasavin, Mikhail
Kalinin, Stanislav
Zozulya, Sergey
Griniukova, Anastasia
Borysko, Petro
Angeli, Andrea
Supuran, Claudiu T.
author_sort Krasavin, Mikhail
collection PubMed
description Testing of an expanded, 800-compound set of analogues of the earlier described Strecker-type α-aminonitriles (selected from publicly available Enamine Ltd. Screening Collection) in thermal shift assay against bovine carbonic anhydrase (bCA) led to further validation of this new class of inhibitors and identification a new, refined chemotype represented by inhibitors with 10-improved potency. [Image: see text]
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spelling pubmed-68824462019-12-13 Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement Krasavin, Mikhail Kalinin, Stanislav Zozulya, Sergey Griniukova, Anastasia Borysko, Petro Angeli, Andrea Supuran, Claudiu T. J Enzyme Inhib Med Chem Research Paper Testing of an expanded, 800-compound set of analogues of the earlier described Strecker-type α-aminonitriles (selected from publicly available Enamine Ltd. Screening Collection) in thermal shift assay against bovine carbonic anhydrase (bCA) led to further validation of this new class of inhibitors and identification a new, refined chemotype represented by inhibitors with 10-improved potency. [Image: see text] Taylor & Francis 2019-11-22 /pmc/articles/PMC6882446/ /pubmed/31752557 http://dx.doi.org/10.1080/14756366.2019.1693556 Text en © 2019 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Paper
Krasavin, Mikhail
Kalinin, Stanislav
Zozulya, Sergey
Griniukova, Anastasia
Borysko, Petro
Angeli, Andrea
Supuran, Claudiu T.
Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement
title Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement
title_full Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement
title_fullStr Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement
title_full_unstemmed Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement
title_short Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement
title_sort further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase ii inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6882446/
https://www.ncbi.nlm.nih.gov/pubmed/31752557
http://dx.doi.org/10.1080/14756366.2019.1693556
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