Synthesis, Structural Elucidation of Aminoacetylenicoxyquinazoline and their Antiproliferative Activities

Zuhair A Muhi-eldeen; Bara Alani; Elham N Al-Kaissi; Sanaa K Bardaweel; Mohammed Gattas; Tawfeeq Arafat

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Synthesis, Structural Elucidation of Aminoacetylenicoxyquinazoline and their Antiproliferative Activities

机译：氨基乙炔氧基喹唑啉的合成，结构鉴定及其抗增殖活性

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The aminoacetylenicoxyquinazoline were synthesized and their structures were confirmed through Infra-Red (IR), Proton Nuclear Magnetic Resonance (1H-NMR), Carbon-13 Nuclear Magnetic Resonance (13C-NMR) and elemental analysis. Docking with Epidural Growth Factor Receptor (EGFR) kinase were carried out and showed effective overlap. The aminoacetylenicoxyquinazoline were tested for their antitumor activities using breast (MCF) and colon (CaCO-2) cancer cell lines. All synthesized compounds exhibited antiproliferative activity but it was weaker than the well-known standard Doxorubicin. Further structural modifications are needed to enhance their antiproliferative effects.

机译：合成了氨基乙炔氧基喹唑啉，并通过红外（IR），质子核磁共振（1H-NMR），碳13核磁共振（13C-NMR）和元素分析确定了其结构。与硬膜外生长因子受体（EGFR）激酶对接，并显示有效重叠。使用乳腺癌（MCF）和结肠癌（CaCO-2）癌细胞系测试了氨基乙酰基氧基喹唑啉的抗肿瘤活性。所有合成的化合物均显示出抗增殖活性，但比众所周知的标准阿霉素弱。需要进一步的结构修饰以增强其抗增殖作用。

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《Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry》 |2017年第23期|共8页
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Zuhair A Muhi-eldeen; Bara Alani; Elham N Al-Kaissi; Sanaa K Bardaweel; Mohammed Gattas; Tawfeeq Arafat;
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Synthesis, Structural Elucidation of Aminoacetylenicoxyquinazoline and their Antiproliferative Activities

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