N-(indazolyl)benzamido derivatives as CDK1 inhibitors: design, synthesis, biological activity, and molecular docking studies.

Raffa D; Maggio B; Cascioferro S; Raimondi MV; Daidone G; Plescia S; Schillaci D; Cusimano MG; Titone L; Colomba C; Tolomeo M

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N-(indazolyl)benzamido derivatives as CDK1 inhibitors: design, synthesis, biological activity, and molecular docking studies.

机译：N-（吲唑基）苯甲酰胺衍生物作为CDK1抑制剂：设计，合成，生物活性和分子对接研究。

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A series of N-1H-indazole-1-carboxamides has been synthesized and their effects on both CDK1/cyclin B and the K-562 (human chronic myelogenus leukemia) cell line were evaluated. Using a computational model, we have observed that all the most active compounds 9e, f, i-n exhibited the same binding mode of purvanalol A in the ATP-binding cleft. Although they were able to moderately inhibit the leukemic cell line K-562 and to show inhibitory activity against the Cdc2-Cyclin B kinase in the low micromolar range, they turned out to be non-cytotoxic against HuDe (IZSL) primary cell cultures from human derm. These preliminary results are quite encouraging in view of the low toxicity demonstrated by the above-mentioned compounds.

机译：已合成了一系列N-1H-吲唑-1-羧酰胺，并评估了它们对CDK1 / cyclin B和K-562（人类慢性粒细胞白血病）细胞系的作用。使用计算模型，我们已经观察到，在ATP结合裂隙中，所有活性最高的化合物9e，f，i-n表现出相同的泛醇A结合模式。尽管它们能够在低微摩尔范围内适度抑制白血病细胞系K-562并显示出对Cdc2-Cyclin B激酶的抑制活性，但它们却对人类的HuDe（IZSL）原代细胞培养物无细胞毒性真皮。考虑到上述化合物显示出低毒性，这些初步结果令人鼓舞。

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《Archiv der Pharmazie》 |2009年第5期|共9页
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Raffa D; Maggio B; Cascioferro S; Raimondi MV; Daidone G; Plescia S; Schillaci D; Cusimano MG; Titone L; Colomba C; Tolomeo M;
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机译：N-（吲哚基）苯甲酰胺衍生物作为CDK1抑制剂：设计，合成，生物活性和分子对接研究

N-(indazolyl)benzamido derivatives as CDK1 inhibitors: design, synthesis, biological activity, and molecular docking studies.

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