Yıl: 2018 Cilt: 15 Sayı: 3 Sayfa Aralığı: 304 - 308 Metin Dili: İngilizce DOI: 10.4274/tjps.64935 İndeks Tarihi: 21-02-2020

Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives

Öz:
Objectives: Urea and carbohydrazide derivatives are important compounds exhibiting cytotoxic activities. In this study, a series of new urea andcarbohydrazide derivatives containing an pyridine ring were synthesized and evaluated for cytotoxic activity.Materials and Methods: The proposed structures of the synthesized compounds were confirmed using elemental analysis, IR, and 1H-NMRspectroscopic techniques. The cytotoxic potencies of synthesized compounds were determined using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay (MTT) on BRCA mutant-carrying HCC1937 and Capan-1 cell lines, as well as on MCF7, HeLa, and MRC5 cells.Results: 3a, 3b, 3c and 3d showed cytotoxic activity against all cancer cell lines.Conclusion: Our data indicate that compounds 3a-d are more selective to cancer cells compared with nontumoral fibroblasts; however, thesecompounds are not more potent on HR defective cells with BRCA mutants.
Anahtar Kelime:

Konular: Farmakoloji ve Eczacılık

Bazı Yeni Karbohidrazit ve Üre Türevlerinin Tasarımı, Sentezi ve Biyolojik Aktivitelerinin Değerlendirilmesi

Öz:
Amaç: Üre ve karbohidrazit türevleri önemli sitotoksik etkinlik gösteren bileşiklerdir. Bu çalışmada, bir yeni seri piridin halkası taşıyan üre ve karbohidrazit türevleri sentezlenmiş ve sitotoksik etkileri araştırılmıştır. Gereç ve Yöntemler: Sentezlenen bileşiklerin önerilen yapıları elemental analiz, IR, 1 H-NMR spektroskopik yöntemleriyle doğrulanmıştır. Sentezlenen bileşiklerin sitotoksik etki güçleri, 3-(4,5-dimetiltiyazol-2-il)-2,5-difeniltetrazolyum bromür (MTT) kullanılarak BRCA mutasyonu taşıyan HCC1937 ve Capan-1 hücre hatları olan MCF7, HeLa ve MRC5 hücreleri üzerinde tespit edilmiştir. Bulgular: 3a, 3b, 3c ve 3d tüm kanser hücre hatlarına karşı sitotoksik etki göstermiştir. Sonuç: Verilerimiz, 3a-d bileşiklerinin kanser hücrelerinde tümöral olmayan fibroblastlarla kıyaslandığında daha seçici olduğunu, ancak bu bileşiklerin BRCA1 mutant homolog rekombinasyonal (HR) DNA onarımı hatalı hücrelerde ise daha fazla etkili olmadığını göstermektedir.
Anahtar Kelime:

Konular: Farmakoloji ve Eczacılık
Belge Türü: Makale Makale Türü: Araştırma Makalesi Erişim Türü: Erişime Açık
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APA Tok F, İLHAN R, GÜNAL S, BALLAR KIRMIZIBAYRAK P, KOÇYİĞİT KAYMAKÇIOĞLU B (2018). Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives. , 304 - 308. 10.4274/tjps.64935
Chicago Tok Fatih,İLHAN RECEP,GÜNAL Selin,BALLAR KIRMIZIBAYRAK PETEK,KOÇYİĞİT KAYMAKÇIOĞLU Bedia Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives. (2018): 304 - 308. 10.4274/tjps.64935
MLA Tok Fatih,İLHAN RECEP,GÜNAL Selin,BALLAR KIRMIZIBAYRAK PETEK,KOÇYİĞİT KAYMAKÇIOĞLU Bedia Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives. , 2018, ss.304 - 308. 10.4274/tjps.64935
AMA Tok F,İLHAN R,GÜNAL S,BALLAR KIRMIZIBAYRAK P,KOÇYİĞİT KAYMAKÇIOĞLU B Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives. . 2018; 304 - 308. 10.4274/tjps.64935
Vancouver Tok F,İLHAN R,GÜNAL S,BALLAR KIRMIZIBAYRAK P,KOÇYİĞİT KAYMAKÇIOĞLU B Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives. . 2018; 304 - 308. 10.4274/tjps.64935
IEEE Tok F,İLHAN R,GÜNAL S,BALLAR KIRMIZIBAYRAK P,KOÇYİĞİT KAYMAKÇIOĞLU B "Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives." , ss.304 - 308, 2018. 10.4274/tjps.64935
ISNAD Tok, Fatih vd. "Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives". (2018), 304-308. https://doi.org/10.4274/tjps.64935
APA Tok F, İLHAN R, GÜNAL S, BALLAR KIRMIZIBAYRAK P, KOÇYİĞİT KAYMAKÇIOĞLU B (2018). Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives. Turkish Journal of Pharmaceutical Sciences, 15(3), 304 - 308. 10.4274/tjps.64935
Chicago Tok Fatih,İLHAN RECEP,GÜNAL Selin,BALLAR KIRMIZIBAYRAK PETEK,KOÇYİĞİT KAYMAKÇIOĞLU Bedia Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives. Turkish Journal of Pharmaceutical Sciences 15, no.3 (2018): 304 - 308. 10.4274/tjps.64935
MLA Tok Fatih,İLHAN RECEP,GÜNAL Selin,BALLAR KIRMIZIBAYRAK PETEK,KOÇYİĞİT KAYMAKÇIOĞLU Bedia Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives. Turkish Journal of Pharmaceutical Sciences, vol.15, no.3, 2018, ss.304 - 308. 10.4274/tjps.64935
AMA Tok F,İLHAN R,GÜNAL S,BALLAR KIRMIZIBAYRAK P,KOÇYİĞİT KAYMAKÇIOĞLU B Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives. Turkish Journal of Pharmaceutical Sciences. 2018; 15(3): 304 - 308. 10.4274/tjps.64935
Vancouver Tok F,İLHAN R,GÜNAL S,BALLAR KIRMIZIBAYRAK P,KOÇYİĞİT KAYMAKÇIOĞLU B Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives. Turkish Journal of Pharmaceutical Sciences. 2018; 15(3): 304 - 308. 10.4274/tjps.64935
IEEE Tok F,İLHAN R,GÜNAL S,BALLAR KIRMIZIBAYRAK P,KOÇYİĞİT KAYMAKÇIOĞLU B "Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives." Turkish Journal of Pharmaceutical Sciences, 15, ss.304 - 308, 2018. 10.4274/tjps.64935
ISNAD Tok, Fatih vd. "Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives". Turkish Journal of Pharmaceutical Sciences 15/3 (2018), 304-308. https://doi.org/10.4274/tjps.64935