scholarly journals Mapping Selective Inhibition of the Cancer-Related Carbonic Anhydrase IX Using Structure–Activity Relationships of Glucosyl-Based Sulfamates

2015 ◽  
Vol 58 (16) ◽  
pp. 6630-6638 ◽  
Author(s):  
Brian P. Mahon ◽  
Carrie L. Lomelino ◽  
Janina Ladwig ◽  
Gregory M. Rankin ◽  
Jenna M. Driscoll ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Selective Inhibition ◽  
Carbonic Anhydrase Ix ◽  
Structure Activity Relationships ◽  
Structure Activity

scholarly journals Structure activity study of carbonic anhydrase IX: Selective inhibition with ureido-substituted benzenesulfonamides

2017 ◽  
Vol 132 ◽  
pp. 184-191 ◽  
Author(s):  
Mam Y. Mboge ◽  
Brian P. Mahon ◽  
Nicole Lamas ◽  
Lillien Socorro ◽  
Fabrizio Carta ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Selective Inhibition ◽  
Carbonic Anhydrase Ix ◽  
Structure Activity

scholarly journals Synthesis and Human Carbonic Anhydrase I, II, IX, and XII Inhibition Studies of Sulphonamides Incorporating Mono-, Bi- and Tricyclic Imide Moieties

2021 ◽  
Vol 14 (7) ◽  
pp. 693
Author(s):  
Kalyan K. Sethi ◽  
KM Abha Mishra ◽  
Saurabh M. Verma ◽  
Daniela Vullo ◽  
Fabrizio Carta ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Carbonic Anhydrase ◽  
Docking Studies ◽  
Carbonic Anhydrases ◽  
Molecular Docking Studies ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Carbonic Anhydrase I ◽  
Human Carbonic Anhydrase ◽  
Inhibition Studies

New derivatives were synthesised by reaction of amino-containing aromatic sulphonamides with mono-, bi-, and tricyclic anhydrides. These sulphonamides were investigated as human carbonic anhydrases (hCAs, EC 4.2.1.1) I, II, IX, and XII inhibitors. hCA I was inhibited with inhibition constants (Kis) ranging from 49 to >10,000 nM. The physiologically dominant hCA II was significantly inhibited by most of the sulphonamide with the Kis ranging between 2.4 and 4515 nM. hCA IX and hCA XII were inhibited by these sulphonamides in the range of 9.7 to 7766 nM and 14 to 316 nM, respectively. The structure–activity relationships (SAR) are rationalised with the help of molecular docking studies.

Structure-Activity Relationships of 1,2-Disubstituted Benzimidazoles: Selective Inhibition of Heme Oxygenase-2 Activity

ChemMedChem ◽  
2015 ◽  
Vol 10 (8) ◽  
pp. 1435-1441 ◽  
Author(s):  
Xianqi Kong ◽  
Dragic Vukomanovic ◽  
Kanji Nakatsu ◽  
Walter A. Szarek
Keyword(s):  
Heme Oxygenase ◽  
Selective Inhibition ◽  
Structure Activity Relationships ◽  
Structure Activity
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