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Makale Tam Makale Uluslararası 2018

New anticancer drug candidates sulfonamides as selective hCA IX or hCA XII inhibitors

Halise İnci Gül, Cem YAMALI, Hiroshi Sakagami, Andrea ANGELİ, Janis LEİTANS, Andris KAZAKS, Kaspars TARS, Dilan Ozmen Ozgun, Claudiu T SUPURAN

Bioorganic Chemistry Cilt 77 · ss. 411–419 · 01.04.2018
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Özet

In this study, new 4-13-(aryl)-5-substitutedphenyl-4,5-dihydro-1H-pyrazole-1-yllbenzensulfonamides (19-36) were synthesized and evaluated their cytotoxic/anticancer and CA inhibitory effects. According to results obtained, the compounds 34 (4-[5-(2,3,4-trimethoxyphenyl)-3-(thiophen-2-yl)4,5-dihydro-1H-pyrazole-1-yl benzensulfonamide, Potency-Selectivity Expression (PSE) = 141) and 36 (44 543,4,5-trimethoxyphenyl)-3-( thiophen-2-yl)-4,5-dihydro-1H-pyrazole-1-yl benzensulfonamide, PSE = 54.5) were found the leader anticancer compounds with the highest PSE values. In CA inhibitory studies, the compounds 36 and 24 (4-[5-(3,4,5-trimethoxyphenyl) 3 (4 fluorophenyl)-4,5-dihydro-1H-pyrazole-1-yl]benzensulfonamide) were found the leader CA inhibitors depending on selectivity ratios. The compound 36 was a selective inhibitor of hCA XII isoenzyme (hCA l/hCA XII = 1250 and hCA II/hCA XII = 224) while the compound 24 was a selective inhibitor of hCA IX isoenzyme (hCA l/hCA IX = 161 and hCA II/hCA IX = 177). The compounds 24, 34, and 36 can be considered to develop new anticancer drug candidates. (C) 2018 Elsevier Inc. All rights reserved.

Anahtar kelimeler

CANCER apoptosis DERIVATIVES sulfonamide anticancer BIOLOGICAL EVALUATION benzenesulfonamides carbonic anhydrases Pyrazoline CHALCONES CARBONIC-ANHYDRASE INHIBITORS Dental cells HETEROCYCLIC SULFONAMIDES CYTOTOXINS BIOACTIVITIES

Atıf için künye

Gül, H. İ., YAMALI, C., Sakagami, H., ANGELİ, A., LEİTANS, J., KAZAKS, A., TARS, K., Ozgun, D. O., & SUPURAN, C. T. (2018). New anticancer drug candidates sulfonamides as selective hCA IX or hCA XII inhibitors. Bioorganic Chemistry, 77, 411–419. https://doi.org/10.1016/j.bioorg.2018.01.021

BibTeX 
@article{gul2018-19890,
  author = {Gül, Halise İnci and YAMALI, Cem and Sakagami, Hiroshi and ANGELİ, Andrea and LEİTANS, Janis and KAZAKS, Andris and TARS, Kaspars and Ozgun, Dilan Ozmen and SUPURAN, Claudiu T},
  title = {New anticancer drug candidates sulfonamides as selective hCA IX or hCA XII inhibitors},
  journal = {Bioorganic Chemistry},
  year = {2018},
  volume = {77},
  pages = {411--419},
  issn = {0045-2068},
  doi = {10.1016/j.bioorg.2018.01.021},
  url = {https://akademik.atauni.edu.tr/yayinlar/19890-new-anticancer-drug-candidates-sulfonamides-as-selective-hca-ix-or-hca-xii}
}