Discovery of Furopyrimidine‐Pyrazole Hybrid Compounds Targeting p53‐MDM2 Interaction as Anticancer Agents
Yazarlar (11)
Mai A. Mansour
School Of Pharmacy, Mısır
School Of Pharmacy, Mısır
Ghaneya S. Hassan
School Of Pharmacy, Mısır
School Of Pharmacy, Mısır
Maiy Y. Jaballah
Faculty Of Pharmacy, Ain Shams University, Mısır
Faculty Of Pharmacy, Ain Shams University, Mısır
Rabah A. T. Serya
Faculty Of Pharmacy, Ain Shams University, Mısır
Faculty Of Pharmacy, Ain Shams University, Mısır
Prof. Dr. Necmi Dege Ondokuz Mayis University Faculty Of Science And Arts, Türkiye
Prof. Dr. Onur ŞAHİN Sinop Üniversitesi, Türkiye
Marwa Sharaky
National Cancer Institute, Mısır
National Cancer Institute, Mısır
Xiaoliang Zhang
Tianjin Medical University, Çin
Tianjin Medical University, Çin
Ruixin Su
Tianjin Medical University, Çin
Tianjin Medical University, Çin
Dexin Kong Tianjin Medical University, Çin
Khaled A. M. Abouzid
Faculty Of Pharmacy, Ain Shams University, Mısır
Faculty Of Pharmacy, Ain Shams University, Mısır
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | Archiv Der Pharmazie (Q2) | ||
| Dergi ISSN | 0365-6233 Dergi Bilgileri (2025) | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 09-2025 |
| Kabul Tarihi | 11-08-2025 | Yayınlanma Tarihi | 01-09-2025 |
| Cilt / Sayı / Sayfa | 358 / 9 / – | DOI | 10.1002/ardp.70085 |
| Makale Linki | https://doi.org/10.1002/ardp.70085 | ||
| UAK Araştırma Alanları |
Yoğun Madde Fiziği
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| Özet |
| Inhibiting the p53‐MDM2 interaction restores the function of the tumour suppressor protein, p53, and offers a promising avenue for anticancer therapies. Herein, a novel series of pyrazoline‐derived compounds was developed and synthesised to serve as potential inhibitors of the p53‐MDM2 interaction. Scaffold hopping was adopted via replacing the cis‐imidazoline core of Nutlin‐2 with a pyrazoline core, and molecular docking confirmed the binding orientation of the designed compounds at the p53‐MDM2 interaction site. The antiproliferative activities of these compounds were evaluated against the NCI60 cell lines, where compounds 6c, 6d and 9d displayed the highest inhibitory activities. Subsequently, compound 6d was selected for the five‐doses NCI60 cell panel assay to afford a mean GI50 value of 8.39 μM. Moreover, 6d significantly reduced MDM2 expression and elevated the expression of p53 in an … |
| Anahtar Kelimeler |
| anticancer activity | MDM2 inhibition | p53-MDM2 interaction | synthesis | wild-type p53 | X-ray diffraction |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 2 |
| Scopus | 2 |
| Google Scholar | 2 |