Dergiler / Turkish Journal of Chemistry / 2017 / Cilt: 41 - Sayı: 2

Synthesis and in vitro anticancer evaluation of 1,4-phenylene-bis-pyrimidine-2-amine derivatives

Sayfa
263–271
Yayın Tarihi
2017-04-01
DOI
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⚡ TL;DR(1 Cümlede Hızlı Çıkarım)

The anticancer activity of 5h was better than that of 5-FU at high concentrations cell-selectively against C6 cells.

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Amaç & Hipotez:A series of 1,4-phenylene-bis-chalcones 3a-3h were synthesized by the reaction of terephthalaldehyde with substituted arylketones in this study.
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Temel Bulgular & Veri:The novel 1,4-phenylene-bis-pyrimidine-2-amine derivatives 5a-5h were obtained by the addition of guanidine hydrochloride to 1,4-phenylene-bis-chalcone 3a-3h in ethanolic KOH under reflux conditions.
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Sonuç & Katkı:The anticancer activity of 5h was better than that of 5-FU at high concentrations cell-selectively against C6 cells.
🔬Tür:Araştırma Makalesi
📍Kapsam:Genişletilmiş Akademik Örneklem
⚙️Değişkenler:4-Phenylene-bis-chalcone · 4-phenylene-bis-pyrimidine · HeLa

Abstract

A series of 1,4-phenylene-bis-chalcones 3a-3h were synthesized by the reaction of terephthalaldehyde with substituted arylketones in this study. The novel 1,4-phenylene-bis-pyrimidine-2-amine derivatives 5a-5h were obtained by the addition of guanidine hydrochloride to 1,4-phenylene-bis-chalcone 3a-3h in ethanolic KOH under reflux conditions. The structure of the compounds was explained by means of IR, $^{1}$H NMR, $^{13}$C NMR, and elemental analyses. The anticancer activities of 3a-3h and 5a-5h were investigated against rat brain tumor cells and human uterus carcinoma in vitro$.$ Activity tests were performed as dose-dependent assays at eight concentrations. The positive control was 5-fluorouracil (5-FU). Compounds 3c and 3d were examined and they showed high activities as compared to 5-FU against C6 (rat brain tumor) and HeLa (human uterus carcinoma) cells. The anticancer activity of 5h was better than that of 5-FU at high concentrations cell-selectively against C6 cells.

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Bu Makaleye Atıf Yap

GÜRDERE, M. B., KAMO, E., YAĞLIOĞLU, A. Ş., BUDAK, Y., CEYLAN, M. (2017). Synthesis and in vitro anticancer evaluation of 1,4-phenylene-bis-pyrimidine-2-amine derivatives. Turkish Journal of Chemistry, Cilt: 41 - Sayı: 2, 263–271. https://ajindex.com/articles/184672

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