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Akademisyenler > Feyzi Sinan TOKALI > Yayın Detayı

Synthesis, Characterization, and In Vitro & In Silico Biological Evaluation of Novel Polyphenols Bearing Quinazolin-4(3H)-one Ring as Promising Anti Prostate Cancer Agents    
Yazarlar (4)
Halil Şenol
Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Zeynep Çağman
Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Furkan Çakır
Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Doç. Dr. Feyzi Sinan TOKALI Doç. Dr. Feyzi Sinan TOKALI
Kafkas Üniversitesi, Türkiye
Devamını Göster
Özet
AbstractIn this study, 12 novel polyphenols containing the quinazolin-4(3H)-one ring were synthesized and characterized using 1H/13C NMR and HRMS analyses, yielding the target compounds in excellent yields (88–96%). Biological evaluation revealed significant cytotoxic activity against PC3 prostate cancer and 3T3 fibroblast cell lines, with compounds 2,2′-(propane-1,3-diyl)bis-3-(2,4-dihydroxybenzylideneamino)quinazolin-4(3H)-one (5) and 2,2′-(propane-1,3-diyl)bis-3-(2,3,4-trihydroxybenzylideneamino)quinazolin-4(3H)-one (6) demonstrating the highest anticancer potential. Compound 6 exhibited the highest selectivity (IC50 = 5.72 µM, SI = 68), outperforming the reference drug, doxorubicin. In silico studies, including molecular docking and dynamics simulations, showed strong binding affinities for mTOR, P110α, and PARP1, particularly for compound 6. Key interactions, such as hydrogen bonds and π-π stacking, contributed to the stability of the 6–mTOR complex. These results highlight compounds 5 and 6 as promising candidates for prostate cancer therapy, with compound 6 showing superior selectivity and interaction profiles, providing the groundwork for further preclinical development.
Anahtar Kelimeler
hydrazone | quinazolin-4(3H)-one | prostate cancer | cytotoxicity | molecular docking | molecular dynamics
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale
Dergi Adı Synlett
Dergi ISSN 0936-5214 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q3
Makale Dili İngilizce
Basım Tarihi 01-2025
Cilt No 36
Sayı 16
Sayfalar 2623 / 2630
Doi Numarası 10.1055/a-2500-7537
Makale Linki https://doi.org/10.1055/a-2500-7537
BM Sürdürülebilir Kalkınma Amaçları
Atıf Sayıları
WoS 3
Synthesis, Characterization, and In Vitro & In Silico Biological Evaluation of Novel Polyphenols Bearing Quinazolin-4(3H)-one Ring as Promising Anti Prostate Cancer Agents

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