Synthesis and bioactivity studies on new 4-(3-(4- Substitutedphenyl)-3a,4-dihydro-3H-indeno[1,2- c]pyrazol-2-yl) benzenesulfonamides      
Yazarlar (6)
Halise Inci Gul
Atatürk Üniversitesi, Türkiye
Doç. Dr. Mehtap TUĞRAK SAKARYA Atatürk Üniversitesi, Türkiye
Hiroshi Sakagami
Meikai University, Japonya
Parham Taslimi
Atatürk Üniversitesi, Türkiye
Ilhami Gulcin
Atatürk Üniversitesi, Türkiye
Claudiu T. Supuran
Università Degli Studi Di Firenze, İtalya
Makale Türü Açık Erişim Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale
Dergi Adı Journal of Enzyme Inhibition and Medicinal Chemistry
Dergi ISSN 1475-6366 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q4
Makale Dili İngilizce
Basım Tarihi 06-2016
Cilt No 31
Sayı 6
Sayfalar 1619 / 1624
DOI Numarası 10.3109/14756366.2016.1160077
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
Benzenesulfonamide | carbonic anhydrase/enzyme inhibition | cytotoxicity | indane | pyrazole | tumor selectivity