Benzenesulfonamide decorated dihydropyrimidin(thi)ones: carbonic anhydrase profiling and antiproliferative activity
Yazarlar (13)
Dr. Öğr. Üyesi Hakan ASLAN Sinop Üniversitesi, Türkiye
Gioele Renzi Università Degli Studi Di Firenze, İtalya
Andrea Angeli Università Degli Studi Di Firenze, İtalya
Ilaria D'agostino Università Degli Studi Di Firenze, İtalya
Roberto Ronca Università Degli Studi Di Brescia, İtalya
Maria Luisa Massardi Università Degli Studi Di Brescia, İtalya
Camilla Tavani Università Degli Studi Di Brescia, İtalya
Simone Carradori University Of G. D'annunzio Chieti And Pescara, İtalya
Marta Ferraroni Università Degli Studi Di Firenze, İtalya
Paolo Governa Università Degli Studi Di Siena, İtalya
Fabrizio Manetti Università Degli Studi Di Siena, İtalya
Fabrizio Carta Università Degli Studi Di Firenze, İtalya
Claudiu T. Supuran Università Degli Studi Di Firenze, İtalya
| Makale Türü |
Özgün Makale
(SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
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| Dergi Adı | Rsc Medicinal Chemistry (Q2) | ||
| Dergi ISSN | 2632-8682 Dergi Bilgileri (2024) | ||
| Dergi Tarandığı Indeksler | SCI | ||
| Makale Dili | Ingilizce | Basım Tarihi | 01-2024 |
| Kabul Tarihi | – | Yayınlanma Tarihi | 01-01-2024 |
| Cilt / Sayı / Sayfa | 15 / 6 / 1929–1941 | DOI | 10.1039/d4md00101j |
| Makale Linki | https://doi.org/10.1039/d4md00101j | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| In the last decades, carbonic anhydrases (CAs) have become the top investigated innovative pharmacological targets and, in particular, isoforms IX and XII have been widely studied due to the evidence of their overexpression in hypoxic tumors. The frantic race to find new anticancer agents places the quick preparation of large libraries of putative bioactive compounds as the basis of a successful drug discovery and development programme. In this context, multi-component and, in general, one-step reactions are becoming very popular and, among them, Biginelli's reaction gave clean and easy-to-isolate products. Thus, we synthesized a series of Biginelli's products (10–17a–b) and similar derivatives (20–21) bearing the benzenesulfonamide moiety, which is known to inhibit CA enzymes. Through the stopped-flow technique, we were able to assess their ability to inhibit the targeted CAs IX and XII in the nanomolar … |
| Anahtar Kelimeler |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 16 |
| Scopus | 15 |
| Google Scholar | 14 |