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Synthesis and bioactivity studies on new 4-(3-(4-Substitutedphenyl)-3a,4-dihydro-3H-indeno[1,2-c]pyrazol-2-yl) benzenesulfonamides

Halise İnci Gül, Mehtap TUĞRAK, Hiroshi Sakagami, Parham TASLIMI, İlhami Gülçin, Claudiu T. SUPURAN

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY Cilt 31 · Sayı 6 · ss. 1619–1624 · 01.01.2016
DOI ile aç

Özet

A series of new 4-(3-(4-substitutedphenyl)-3a, 4-dihydro-3H-indeno[1,2-c] pyrazol-2-yl) benzenesulfonamides (7-12) was synthesized starting from 2-(4-substitutedbenzylidene)-2,3-dihydro-1H-inden-1-one (1-6) and 4-hydrazinobenzenesulfonamide. The substituted benzaldehydes from which the key intermediate was prepared by introducing 2- or 4-substituents such as fluorine, hydroxy, methoxy, or the 3,4,5-trimethoxy moieties. The compounds were tested for their cytotoxicity, tumor-specificity and potential as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The 3,4,5-trimethoxy and the 4-hydroxy derivatives showed interesting cytotoxic activities, which may be crucial for further anti-tumor activity studies, whereas some of these sulfonamides strongly inhibited both human (h) cytosolic isoforms hCA I and II.

Anahtar kelimeler

cytotoxicity ISOFORMS I BIOLOGICAL EVALUATION Benzenesulfonamide Pyrazole SULFONAMIDES carbonic anhydrase/enzyme inhibition indane tumor selectivity CARBONIC-ANHYDRASE INHIBITORS ISOENZYMES INHIBITORS ANTICANCER AGENTS PYRAZOLINE DERIVATIVES ANTIMICROBIAL AGENTS CYTOTOXIC ACTIVITIES CELL-LINES

Atıf için künye

Gül, H. İ., TUĞRAK, M., Sakagami, H., TASLIMI, P., Gülçin, İ., & SUPURAN, C. T. (2016). Synthesis and bioactivity studies on new 4-(3-(4-Substitutedphenyl)-3a,4-dihydro-3H-indeno[1,2-c]pyrazol-2-yl) benzenesulfonamides. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 31(6), 1619–1624. https://doi.org/10.3109/14756366.2016.1160077

BibTeX 
@article{gul2016-19860,
  author = {Gül, Halise İnci and TUĞRAK, Mehtap and Sakagami, Hiroshi and TASLIMI, Parham and Gülçin, İlhami and SUPURAN, Claudiu T.},
  title = {Synthesis and bioactivity studies on new 4-(3-(4-Substitutedphenyl)-3a,4-dihydro-3H-indeno[1,2-c]pyrazol-2-yl) benzenesulfonamides},
  journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
  year = {2016},
  volume = {31},
  number = {6},
  pages = {1619--1624},
  issn = {1475-6366},
  doi = {10.3109/14756366.2016.1160077},
  url = {https://akademik.atauni.edu.tr/yayinlar/19860-synthesis-and-bioactivity-studies-on-new-4-3-4-substitutedphenyl-3a4-dihydro-3h}
}