pmid: 31752557,   nlmid 101150203,  doi:10.1080/14756366.2019.1693556

Further validation of strecker-type ?-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

Vol. 35, Issue 35, Dec.2020

Journal of enzyme inhibition and medicinal chemistry (J Enzyme Inhib Med Chem),  ISSN 1475-6374

Abstract

Testing of an expanded, 800-compound set of analogues of the earlier described Strecker-type ?-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. [Formula: see text].


MESH Headings


Article Keywords

Differential scanning fluorimetry | carbonic anhydrase II | protein affinity | thermal shift assay |


Chemical

Similar Articles

Discovery of Strecker-type ?-aminonitriles as a new class of human carbonic anhydrase inhibitors using differential scanning fluorimetry.
Krasavin, Mikhail Stavniichuk, Roman Zozulya, Sergey Borysko, Petro Vullo, Daniela Supuran, Claudiu T
Journal of enzyme inhibition and medicinal chemistry ,vol(31), issue(6),  Dec.2016

Sulfonamides with Potent Inhibitory Action and Selectivity against the ?-Carbonic Anhydrase from Vibrio cholerae.
Ceruso, Mariangela Del Prete, Sonia Alothman, Zeid Capasso, Clemente Supuran, Claudiu T
ACS medicinal chemistry letters ,vol(5), issue(7),  Jul.2014

Four-dimensional generalized difference matrix and some double sequence spaces.
Tu?, Orhan
Journal of inequalities and applications ,vol(2017), issue(1),  

Carbonic anhydrase inhibition with natural products: novel chemotypes and inhibition mechanisms.
Supuran, Claudiu T
Molecular diversity ,vol(15), issue(2),  May.2011

New series of sulfonamides containing amino acid moiety act as effective and selective inhibitors of tumor-associated carbonic anhydrase XII.
Ceruso, Mariangela Bragagni, Marco AlOthman, Zeid Osman, Sameh M Supuran, Claudiu T
Journal of enzyme inhibition and medicinal chemistry ,vol(30), issue(3),  Jun.2015

Design, synthesis, in silico and biological evaluation of novel 2-(4-(4-substituted piperazin-1-yl)benzylidene)hydrazine carboxamides.
Kumari, Shikha Mishra, Chandra Bhushan Idrees, Danish Prakash, Amresh Yadav, Rajesh Hassan, Md Imtaiyaz Tiwari, Manisha
Molecular diversity ,vol(21), issue(1),  Feb.2017

Vanadium-catalyzed oxidative Strecker reaction: ?-C-H cyanation of para-methoxyphenyl (PMP)-protected primary amines.
Zhu, Chen Xia, Ji-Bao Chen, Chuo
Tetrahedron letters ,vol(55), issue(1),  Jan.2014

Padé approximant related to the Wallis formula.
Lin, Long Ma, Wen-Cheng Chen, Chao-Ping
Journal of inequalities and applications ,vol(2017), issue(1),  

Molecular Characterization of a Dual Domain Carbonic Anhydrase From the Ctenidium of the Giant Clam, Tridacna squamosa, and Its Expression Levels After Light Exposure, Cellular Localization, and Possible Role in the Uptake of Exogenous Inorganic Carbon.
Koh, Clarissa Z Y Hiong, Kum C Choo, Celine Y L Boo, Mel V Wong, Wai P Chew, Shit F Neo, Mei L Ip, Yuen K
Frontiers in physiology ,vol(9), issue(),  

ARENA: Inter-modality affine registration using evolutionary strategy.
Masoumi, Nima Xiao, Yiming Rivaz, Hassan
International journal of computer assisted radiology and surgery ,vol(14), issue(3),  Mar.2019


Medline data is available here.

The Search Enterprise

Contact Us