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Syntheses and Cell-Based Phenotypic Screen of Novel 7-Amino pyrido[2,3-d]pyrimidine-6-carbonitrile Derivatives as Potential Antiproliferative Agents

A series of N-3-substituted 7-aminopyrido[2,3-d]pyrimidin-6-carbonitrile derivatives was readily synthesized and their anti-proliferative activities on five types of tumor cells were evaluated through a cell-based phenotypic screening approach. Compound 3k was found to be potent on human colon cance...

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Detalles Bibliográficos
Autores principales: Yang, Tao, He, Hong, Ang, Wei, Yang, Ying-Hong, Yang, Jian-Zhong, Lin, Yan-Ni, Yang, Hua-Cheng, Pi, Wei-Yi, Li, Zi-Cheng, Zhao, Ying-Lan, Luo, You-Fu, Wei, Yuquan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268601/
https://www.ncbi.nlm.nih.gov/pubmed/22367029
http://dx.doi.org/10.3390/molecules17032351
Descripción
Sumario:A series of N-3-substituted 7-aminopyrido[2,3-d]pyrimidin-6-carbonitrile derivatives was readily synthesized and their anti-proliferative activities on five types of tumor cells were evaluated through a cell-based phenotypic screening approach. Compound 3k was found to be potent on human colon cancer SW620 cells with an IC(50) value of 12.5 μM. Structural optimization of compound 3k led to compound 4a with improved anti-proliferative potency on SW620 cells with an IC(50) value of 6.9 μM. Further cell-cycle analyses suggested that compound 4a induced apoptosis of SW620 cells in a concentration-dependent manner.