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Dergiler / Turkish Journal of Pharmaceutical Sciences / 2018 / Cilt: 15 - Sayı: 3

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

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

FATİH TOK
RECEP İLHAN
Selin GÜNAL
PETEK BALLAR KIRMIZIBAYRAK
Bedia KOÇYİĞİT KAYMAKÇIOĞLU
Sayfa
304–308
DOI
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Yapay Zeka Hızlı Bakış & Çıkarımlar

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⚡ TL;DR(1 Cümlede Hızlı Çıkarım)

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.

📌 3 Maddede Bu Makale

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Amaç & Hipotez:Objectives: Urea and carbohydrazide derivatives are important compounds exhibiting cytotoxic activities.
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Temel Bulgular & Veri: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.
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Sonuç & Katkı: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.
🔬Tür:Araştırma Makalesi
📍Kapsam:Genişletilmiş Akademik Örneklem
⚙️Değişkenler:Alan Parametreleri

Özet

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.

Abstract

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.

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Bu Makaleye Atıf Yap

TOK, F., İLHAN, R., GÜNAL, S., KIRMIZIBAYRAK, P. B., KAYMAKÇIOĞLU, B. K. (2018). Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives. Turkish Journal of Pharmaceutical Sciences, Cilt: 15 - Sayı: 3, 304–308. https://ajindex.com/articles/403973

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