Synthesis, cytotoxic, and carbonic anhydrase inhibitory effects of new 2-(3-(4-methoxyphenyl)-5-(aryl)-4,5-dihydro-1H-pyrazol-1-yl)benzo[d]thiazole derivatives
Yazarlar (4)
Doç. Dr. Mehtap TUĞRAK SAKARYA
Atatürk Üniversitesi, Türkiye
Atatürk Üniversitesi, Türkiye
Meikai University, Japonya
Atatürk Üniversitesi, Türkiye
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale |
| Dergi Adı | Journal of Heterocyclic Chemistry |
| Dergi ISSN | 0022-152X Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q4 |
| Makale Dili | İngilizce |
| Basım Tarihi | 07-2020 |
| Cilt No | 57 |
| Sayı | 7 |
| Sayfalar | 2762 / 2768 |
| DOI Numarası | 10.1002/jhet.3985 |
| Makale Linki | http://doi.wiley.com/10.1002/jhet.3985 |
| Özet |
| 2-(3-[4-Methoxyphenyl]-5-aryl-4,5-dihydro-1H-pyrazol-1-yl)benzo[d]thiazoles (1b-7b) were synthesized for the first time except 1b, and spectral methods such as 1H NMR, 13C NMR and HRMS were utilized to illuminate the chemical structures of the synthesized compounds. Phenyl (1b), 2-methoxyphenyl (2b), 4-methoxyphenyl (3b), 4-methoxy-3-hydroxyphenyl (4b), 2,5-dimethoxyphenyl (5b), 3,4,5-trimethoxyphenyl (6b), or thiophene-2-yl (7b) was used as a aryl part. The inhibitory effects of the compounds were evaluated toward human carbonic anhydrase I and II enzymes (hCA I and hCA II). In vitro cytotoxic effects of the compounds against human oral squamous carcinomas and human normal oral cells were carried out via MTT. The compounds (1b-7b) had Ki values of 36.87 ± 11.62-66.24 ± 2.99 μM (hCA I) and 22.66 ± 1.41-89.95 ± 6.25 μM (hCA II). Compounds 1b (Ki = 36.87 ± 11.62 μM) toward hCA I, 6b (Ki = 22.66 ± 1.41 μM) toward hCA II had significant enzyme inhibitory potency. Compound 6b had the highest tumor selectivity (TS = 29.3) and potency selectivity expression (PSE = 272.3) values. Therefore, compounds 1b and 6b with CAs inhibition effect and compound 6b with the cytotoxicity may be forwarded to further studies as potent compounds. |
| Anahtar Kelimeler |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| SCOPUS | 17 |
| Google Scholar | 17 |
| Google Scholar | 17 |