Citation
Alafeefy, Ahmed M., et al. "Inhibition of Human Carbonic Anhydrase Isozymes I, II, IX and XII With a New Series of Sulfonamides Incorporating Aroylhydrazone-, [1,2,4]triazolo[3,4-b][1,3,4]thiadiazinyl- or 2-(cyanophenylmethylene)-1,3,4-thiadiazol-3(2H)-yl Moieties." Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 30, no. 1, 2015, pp. 52-6.
Alafeefy AM, Abdel-Aziz HA, Vullo D, et al. Inhibition of human carbonic anhydrase isozymes I, II, IX and XII with a new series of sulfonamides incorporating aroylhydrazone-, [1,2,4]triazolo[3,4-b][1,3,4]thiadiazinyl- or 2-(cyanophenylmethylene)-1,3,4-thiadiazol-3(2H)-yl moieties. J Enzyme Inhib Med Chem. 2015;30(1):52-6.
Alafeefy, A. M., Abdel-Aziz, H. A., Vullo, D., Al-Tamimi, A. M., Awaad, A. S., Mohamed, M. A., Capasso, C., & Supuran, C. T. (2015). Inhibition of human carbonic anhydrase isozymes I, II, IX and XII with a new series of sulfonamides incorporating aroylhydrazone-, [1,2,4]triazolo[3,4-b][1,3,4]thiadiazinyl- or 2-(cyanophenylmethylene)-1,3,4-thiadiazol-3(2H)-yl moieties. Journal of Enzyme Inhibition and Medicinal Chemistry, 30(1), 52-6. https://doi.org/10.3109/14756366.2013.877897
Alafeefy AM, et al. Inhibition of Human Carbonic Anhydrase Isozymes I, II, IX and XII With a New Series of Sulfonamides Incorporating Aroylhydrazone-, [1,2,4]triazolo[3,4-b][1,3,4]thiadiazinyl- or 2-(cyanophenylmethylene)-1,3,4-thiadiazol-3(2H)-yl Moieties. J Enzyme Inhib Med Chem. 2015;30(1):52-6. PubMed PMID: 24666294.
TY - JOUR
T1 - Inhibition of human carbonic anhydrase isozymes I, II, IX and XII with a new series of sulfonamides incorporating aroylhydrazone-, [1,2,4]triazolo[3,4-b][1,3,4]thiadiazinyl- or 2-(cyanophenylmethylene)-1,3,4-thiadiazol-3(2H)-yl moieties.
AU - Alafeefy,Ahmed M,
AU - Abdel-Aziz,Hatem A,
AU - Vullo,Daniela,
AU - Al-Tamimi,Abdul-Malek S,
AU - Awaad,Amani S,
AU - Mohamed,Menshawy A,
AU - Capasso,Clemente,
AU - Supuran,Claudiu T,
Y1 - 2014/03/25/
PY - 2014/3/27/entrez
PY - 2014/3/29/pubmed
PY - 2015/9/16/medline
KW - Cancer-associated isoform
KW - carbonic anhydrase
KW - enzyme inhibitor
KW - sulfonamide
SP - 52
EP - 6
JF - Journal of enzyme inhibition and medicinal chemistry
JO - J Enzyme Inhib Med Chem
VL - 30
IS - 1
N2 - A series of benzenesulfonamides incorporating aroylhydrazone, piperidinyl, sulfone, [1,2,4]triazolo[3,4-b][1,3,4]thiadiazinyl- or 2-(cyanophenyl-methylene)-1,3,4-thiadiazol-3(2H)-yl moieties was investigated as inhibitors of four α-carbonic anhydrases (CAs, EC 4.2.1.1), the human (h) isoforms hCA I, II (cytosolic, offtarget enzymes) and hCA IX and XII (transmembrane, tumor-associated isoforms). Low nanomolar activity was observed against hCA II (KIs of 0.56-17.1 nM) with these sulfonamides, whereas the slow cytosolic isoform hCA I was less inhibited by these compounds (KIs of 86.4 nM-32.8 µM). Most of these sulfonamides significantly inhibited CA IX, with KIs in the range of 4.5-47.0 nM, although some of the derivatives incorporating bulkier bicyclic moieties, as well as 2-thienyl fragments, showed a weaker activity against this isoform (KIs in the range 50.1-553 nM). All the investigated compounds also inhibited CA XII with KIs in the range 0.85-376 nM. The best inhibitors were those incorporating bulky [1,2,4]triazolo[3,4-b][1,3,4]thiadiazinyl moieties and 1,3,4-thiadiazol-3(2H)-yl groups.
SN - 1475-6374
UR - https://www.unboundmedicine.com/medline/citation/24666294/Inhibition_of_human_carbonic_anhydrase_isozymes_I_II_IX_and_XII_with_a_new_series_of_sulfonamides_incorporating_aroylhydrazone__[124]triazolo[34_b][134]thiadiazinyl__or_2__cyanophenylmethylene__134_thiadiazol_3_2H__yl_moieties_
L2 - https://www.tandfonline.com/doi/full/10.3109/14756366.2013.877897
DB - PRIME
DP - Unbound Medicine
ER -
