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

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

1
State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu, Sichuan 610041, China
2
Key Laboratory of Drug Targeting and Drug Delivery System, Ministry of Education, West China Medical School, Sichuan University, Chengdu, Sichuan 610041, China
3
Department of Pharmaceutical and Bioengineering, School of Chemical Engineering, Sichuan University, Chengdu, Sichuan 610065, China
*
Authors to whom correspondence should be addressed.
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 (CC BY 3.0).

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MDPI and ACS Style

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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