A modular approach to trim cellular targets in anticancer drug discovery

被引：7

作者：

Rios-Luci, Carla ^{[1
]}

Dominguez-Kelly, Raquel ^{[2
]}

Leon, Leticia G. ^{[1
]}

Diaz-Rodriguez, Elena ^{[3
]}

Freire, Raimundo ^{[2
]}

Pandiella, Atanasio ^{[3
]}

Cikotiene, Inga ^{[4
]}

Padron, Jose M. ^{[1
]}

机构：

[1] Univ La Laguna, BioLab, Inst Univ Bioorgan Antonio Gonzalez IUBO AG, San Cristobal la Laguna 38206, Spain

[2] Hosp Univ Canarias, Unidad Invest, San Cristobal la Laguna 38320, Spain

[3] Univ Salamanca, Ctr Invest Canc, IBMCC CSIC, Salamanca 37007, Spain

[4] Vilnius Univ, Dept Organ Chem, Fac Chem, LT-03225 Vilnius, Lithuania

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 22期

关键词：

Phenotypic Drug Discovery; Antitumor agents; Cell cycle; Mitotic arrest; Structure-activity relationships; ANTIPROLIFERATIVE ACTIVITY; INHIBITION; CHECKPOINTS; AURORA; CDK1;

D O I：

10.1016/j.bmcl.2011.09.069

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A Phenotypic Drug Discovery strategy was applied to study a set of pyrimidine analogs prepared by means of intramolecular oxidation-reduction reactions of N-substituted-N-(2,6-disubstituted-5-nitro-4-pyrimidinyl) aminoacetic acid methyl esters in basic media. The combined and rational use of specific assays allowed in short time reducing from all possible cellular targets to those involved in metaphase to anaphase transition. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：6641 / 6645

页数：5

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