New azafluorenones with cytotoxic and carbonic anhydrase inhibitory properties: 2-aryl-4-(4-hydroxyphenyl)-5H-indeno[1,2-b]pyridin-5-ones
Yazarlar (5)
Doç. Dr. Mehtap TUĞRAK SAKARYA
Atatürk Üniversitesi, Türkiye
Atatürk Üniversitesi, Türkiye
Meikai University, Japonya
Atatürk Üniversitesi, Türkiye
Università Degli Studi Di Firenze, İtalya
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale |
| Dergi Adı | Bioorganic Chemistry |
| Dergi ISSN | 0045-2068 Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q4 |
| Makale Dili | İngilizce |
| Basım Tarihi | 12-2018 |
| Cilt No | 81 |
| Sayı | 1 |
| Sayfalar | 433 / 439 |
| DOI Numarası | 10.1016/j.bioorg.2018.09.013 |
| Özet |
| New azafluorenones, 2-aryl-4-(4-hydroxyphenyl)-5H-indeno[1,2-b]pyridin-5-ones, were prepared to evaluate their cytotoxic/anticancer properties, also their inhibitory effects on hCA I and II isoenzymes. Aryl part was changed as [phenyl (H1), 4-methylphenyl (H2), 4-methoxyphenyl (H3), 4-fluorophenyl (H4), 4-bromophenyl (H5), 4-chlorophenyl (H6), 3-hydroxyphenyl (H7), and 4-hydroxyphenyl (H8)]. The structure of the synthesized compounds was characterized by 1 H NMR, 13 C NMR and HRMS spectra. Cytotoxicity results of the series pointed out that the compounds H6 (PSE: 28.0) and H5 (PSE: 27.3), with the highest potency selectivity expression (PSE) value, can be considered as leader compounds of the study in designing novel anticancer agents. Additionally, all azafluorenones synthesized showed a good inhibition profile towards hCA I and II isoenzymes in the range of 54.14–73.72 nM and 67.28–76.15 nM, respectively. The compounds H5 and H6 can be considered for further designs with their cytotoxic and CA inhibitory profiles. |
| Anahtar Kelimeler |
| Azafluorenone | Carbonic anhydrase | Cytotoxicity | Phenol |
Science Direct
New azafluorenones with cytotoxic and carbonic anhydrase inhibitory properties: 2-aryl-4-(4-hydroxyphenyl)-5H-indeno[1,2-b]pyridin-5-ones
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| SCOPUS | 65 |
| Google Scholar | 74 |
| Google Scholar | 74 |