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设计、合成及新型喹唑啉衍生物的生物评估作为潜在的抗癌药物。

Design, synthesis and biological evaluation of novel quinazoline derivatives as potential anti-cancer agents.

机构信息

Department of Pharmaceutical Chemistry, College of Pharmacy, AlKharj University, Saudi Arabia.

出版信息

J Enzyme Inhib Med Chem. 2012 Aug;27(4):541-5. doi: 10.3109/14756366.2011.601302. Epub 2011 Aug 18.

Abstract

Twenty-two quinazoline derivatives have been synthesised and examined for their anti-tumour activity against three tumour cell lines, namely human breast cancer cell line (MCF-7), human cervical cancer cell line (HeLa) and human hepatoma cell line (HepG2). Twelve of the tested compounds have shown promising anti-tumour activity with an IC(50) range of 5.0-9.7 µg/mL. Regarding the spectrum of activity, five compounds exhibited interesting anti-proliferative properties against the three tested cell lines comparable to the reference drug (dasatinib).

摘要

已经合成了 22 种喹唑啉衍生物,并对它们的抗肿瘤活性进行了测试,针对三种肿瘤细胞系,即人乳腺癌细胞系(MCF-7)、人宫颈癌细胞系(HeLa)和人肝癌细胞系(HepG2)。在测试的 12 种化合物中,有 12 种表现出了有希望的抗肿瘤活性,IC(50)范围在 5.0-9.7μg/ml 之间。关于活性谱,有 5 种化合物对三种测试的细胞系表现出了有趣的抗增殖特性,与参考药物(达沙替尼)相当。

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