Emine ALBAYRAK, Özer IŞILAR, Mutluhan BIYIKOĞLU, Ayşe ŞAHİN YAĞLIOĞLU, Adnan BULUT

Ferrosenil Kalkonların Sentezi ve Anti-kanser Aktiviteleri; İlaç Benzerlik Hesaplamaları

Claisen - Schmidt kondenzasyonu ve Friedel - Crafts açilleme tepkimeleri ile 1-8 farklı ferrosenil çalkon sentezlendi. Yapıları 1H NMR, 13C NMR and FT-IR ile aydınlatılmıştır. Çalkonların sitotoksik ve antiproliferatif aktiviteleri, HeLa (rahim kanseri) ve PC3 (prostat kanseri) hücre hatlarına karşı tarandı. Çok düşük konsantrasyonda (5 µM) bile özellikle PC3 hücresine karşı mükemmel anti-kanser aktivite gösterdiler. Ayrıca fizikokimyasal özellikleri, ilaç benzerliği hesaplamaları ve beş kuralı (RO5) araştırıldı.

Anahtar Kelimeler:

Ferrosen, Çalkon, PC3, HeLa, Anti-kanser, İlaç benzerlik

The Synthesis and Anti-cancer Activities of Ferrocenyl Chalcones; Drug-Likeness Calculations

A series of 1-8 different ferrocenyl chalcones were synthesized through the Claisen–Schmidt condensation and the Friedel−Crafts acylation. Their structures were confirmed by means of 1H, 13C NMR and FT-IR. The cytotoxic and antiproliferative activities of the chalcones were screened against HeLa (cervix cancer) and PC3 (prostate cancer) cell lines. They showed excellent anti-cancer activities especially against PC3 cell even at very low concentration (5 µM). Also, their physicochemical properties, drug-likeness calculations and the rule of five (RO5) were investigated.

Keywords:

Ferrocene, Chalcone, PC3, HeLa, Anti-cancer, Drug-likeness,

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