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Molecules 2012, 17(3), 2351-2366; doi:10.3390/molecules17032351
Article

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

1, 1, 2, 3, 1, 1, 3, 1, 3, 1,* , 1,*  and 1
Received: 12 January 2012 / Revised: 17 February 2012 / Accepted: 20 February 2012 / Published: 24 February 2012
(This article belongs to the Section Medicinal Chemistry)
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Abstract

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 IC50 value of 12.5 mM. Structural optimization of compound 3k led to compound 4a with improved anti-proliferative potency on SW620 cells with an IC50 value of 6.9 mM. Further cell-cycle analyses suggested that compound 4a induced apoptosis of SW620 cells in a concentration-dependent manner.
Keywords: 7-aminopyrido[2,3-d]pyrimidin-6-carbonitrile derivatives; cell-based phenotypic screening; anti-tumor activity; structure-activity relationship (SAR); apoptosis 7-aminopyrido[2,3-d]pyrimidin-6-carbonitrile derivatives; cell-based phenotypic screening; anti-tumor activity; structure-activity relationship (SAR); apoptosis
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Yang, T.; He, H.; Ang, W.; Yang, Y.-H.; Yang, J.-Z.; Lin, Y.-N.; Yang, H.-C.; Pi, W.-Y.; Li, Z.-C.; Zhao, Y.-L.; Luo, Y.-F.; Wei, Y. Syntheses and Cell-Based Phenotypic Screen of Novel 7-Amino pyrido[2,3-d]pyrimidine-6-carbonitrile Derivatives as Potential Antiproliferative Agents. Molecules 2012, 17, 2351-2366.

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