Synthesis and biological evaluation of some new mono Mannich bases with piperazines as possible anticancer agents and carbonic anhydrase inhibitors
Yazarlar (7)
Doç. Dr. Mehtap TUĞRAK SAKARYA
Atatürk Üniversitesi, Türkiye
Atatürk Üniversitesi, Türkiye
Meikai University, Japonya
Meikai University, Japonya
Atatürk Üniversitesi, Türkiye
Anadolu 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 |
| Makale Dili | İngilizce |
| Basım Tarihi | 09-2019 |
| Cilt No | 90 |
| Sayı | 1 |
| Sayfalar | 103095 / 0 |
| DOI Numarası | 10.1016/j.bioorg.2019.103095 |
| Makale Linki | https://linkinghub.elsevier.com/retrieve/pii/S0045206819300021 |
| Özet |
| New mono Mannich bases, (2-(4-hydroxy-3-((4-substituephenylpiperazin-1-yl)methyl)benzylidene)-2,3-dihydro-1H-inden-1-one), were prepared to evaluate their cytotoxic/anticancer properties and also their inhibitory effects on human carbonic anhydrase I and II isoenzymes (hCA I and II). Amine part was changed as [N-phenylpiperazine (1), N-benzylpiperazine (2), 1-(2-fluorophenyl)piperazine (3), 1-(4-fluorophenyl)piperazine (4), 1-(2-methoxyphenyl)piperazine (5)]. The structure of the synthesized compounds was characterized by 1H NMR, 13C NMR and HRMS spectra. Cytotoxicity results of the series pointed out that the compound 4 had the highest tumor selectivity value (TS: 59.4) possibly by inducing necrotic cell death in series. Additionally, all compounds synthesized showed a good inhibition profile towards hCA I and II isoenzymes with the Ki values between 29.6 and 58.4 nM and 38.1–69.7 nM, respectively. These values were lower than the reference compound AZA. However, it seems that the compounds 4 and 2 can be considered as lead compounds of CA studies with the lowest Ki values in series for further designs. |
| Anahtar Kelimeler |
| Carbonic anhydrase | Chalcone | Cytotoxicity | Mannich bases | Phenol |
Science Direct
Synthesis and biological evaluation of some new mono Mannich bases with piperazines as possible anticancer agents and carbonic anhydrase inhibitors
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| SCOPUS | 72 |
| Google Scholar | 83 |