A modular approach to trim cellular targets in anticancer drug discovery

作者：Rios Luci Carla; Dominguez Kelly Raquel; Leon Leticia G; Diaz Rodriguez Elena; Freire Raimundo; Pandiella Atanasio; Cikotiene Inga; Padron Jose M^*

来源：Bioorganic & Medicinal Chemistry Letters, 2011, 21(22): 6641-6645.

DOI：10.1016/j.bmcl.2011.09.069

• Phenotypic Drug Discovery
• Antitumor agents
• Cell cycle
• Mitotic arrest
• Structure-activity relationships

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.

• 出版日期2011-11-15