Synthesis, characterization, anticancer, antimicrobial and carbonic anhydrase inhibition profiles of novel (3aR, 4S, 7R, 7aS)-2-(4-((E)-3-(3-aryl) acryloyl) phenyl)-3a, 4, 7 …
Yazarlar (9)
Umit M Kocyigit
Yakup Budak
Prof. Dr. Meliha Burcu GÜRDERE Türkiye
Şaban Tekin
Tuğba Kul Köprülü
Fatih Ertürk
Kezban Özcan
İlhami Gülçin
Mustafa Ceylan Tokat Gaziosmanpaşa Üniversitesi
| Makale Türü | Özgün Makale (Uluslararası alan indekslerindeki dergilerde yayınlanan tam makale) | ||
| Dergi Adı | Bioorganic chemistry | ||
| Makale Dili | – | Basım Tarihi | 02-2017 |
| Cilt / Sayı / Sayfa | 70 / 0 / 118–125 | DOI | – |
| Makale Linki | https://www.sciencedirect.com/science/article/pii/S0045206816303261 | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| In the present study, a series of new hybrid compounds containing chalcone and methanoisoindole units 7a-n ((3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl) phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione) were synthesized, characterized and investigated for their anticancer activity against C6 gliocarcinoma cell in rats, and antimicrobial activity against some human pathogen microorganisms. The compounds 7e, 7h, 7j, 7k, 7L and 7n showed very high anticancer activity with the inhibition range of 80.51–97.02% compared to 5-FU. Some of the compounds exhibited anti-microbial activity. Also, they evaluated for inhibition effects against human carbonic anhydrase I, and II isoenzymes (hCA I and II) with Ki values in the range of 405.26–635.68 pM for hCA I, and 245.40–489.60 pM for hCA II, respectively. These results demonstrated that 3aR,4S,7R,7aS)-2-(4-((E)-3-(3-aryl)acryloyl)phenyl)-3a,4,7 … |
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