Scopus
🔓 Açık Erişim
Synthesis, cytotoxicity and carbonic anhydrase inhibitory activities of new pyrazolines
Journal of Enzyme Inhibition and Medicinal Chemistry · Kasım 2016
Makale Bilgileri
DergiJournal of Enzyme Inhibition and Medicinal Chemistry
Yayın TarihiKasım 2016
Cilt / Sayfa31 · 20-24
Scopus ID2-s2.0-85006263475
Erişim🔓 Açık Erişim
Özet
A series of polymethoxylated-pyrazoline benzene sulfonamides were synthesized, investigated for their cytotoxic activities on tumor and non-tumor cell lines and inhibitory effects on carbonic anhydrase isoenzymes (hCA I and hCA II). Although tumor selectivity (TS) of the compounds were less than the reference compounds 5-Fluorouracil and Melphalan, trimethoxy derivatives 4, 5, and 6 were more selective than dimethoxy derivatives 2 and 3 as judged by the cytotoxicity assay with the cells both types originated from the gingival tissue. The compound 6 (4-[3-(4-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl] benzene sulfonamide) showed the highest TS values and can be considered as a lead molecule of the series for further investigations. All compounds synthesized showed superior CA inhibitory activity than the reference compound acetazolamide on hCA I, and II isoenzymes, with inhibition constants in the range of 26.5–55.5 nM against hCA I and of 18.9–28.8 nM against hCA II, respectively.
Yazarlar (9)
1
Kaan Kucukoglu
ORCID: 0000-0001-8977-9775
2
Fatih Oral
3
Tevfik Aydin
4
Cem Yamali
ORCID: 0000-0002-4833-7900
5
Oztekin Algul
6
H. Sakagami
7
Gülçin
8
Claudiu T. Supuran
ORCID: 0000-0003-4262-0323
9
H. I. Gul
Anahtar Kelimeler
Carbonic anhydrase
cytotoxicity
dental cells
pyrazoline
sulfonamide
tumor selectivity
Kurumlar
Atatürk Üniversitesi
Erzurum Turkey
College of Sciences
Riyadh Saudi Arabia
Meikai University
Sakado Japan
Mersin Üniversitesi
Mersin Turkey
Università degli Studi di Firenze
Florence Italy
Metrikler
55
Atıf
9
Yazar
6
Anahtar Kelime