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Synthesis of Naringenin Amino Acid Esters as Potential CDK2 Inhibitors

机译:柚皮素氨基酸酯的合成作为潜在的CDK2抑制剂

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摘要

The central role of cyclin-dependent kinases (CDKs) in cell cycle regulation makes them a promising target for studying inhibitory molecules that can modify the degree of cell proliferation.The discovery of specific inhibitors of CDKs such as polyhydroxylated flavones has opened the way to investigation and design of antimitotic compounds.Among the polyhydroxylated flavones,flavopiridol (1,Figure 1 )has completed phase I clinical trial where it showed antitumor effect in patients with refractory neoplasms.
机译:细胞周期蛋白依赖性激酶(CDKs)在细胞周期调控中的核心作用使其成为研究可改变细胞增殖程度的抑制性分子的有希望的靶标.CDKs特异性抑制剂如多羟基黄酮的发现为研究开辟了道路。在多羟基黄酮中,黄酮哌啶醇(1,图1)已经完成了I期临床试验,在难治性肿瘤患者中显示出抗肿瘤作用。

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