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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.
MedLine Citation:
PMID:  22367029     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
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 mM. 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 mM. Further cell-cycle analyses suggested that compound 4a induced apoptosis of SW620 cells in a concentration-dependent manner.
Authors:
Tao Yang; Hong He; Wei Ang; Ying-Hong Yang; Jian-Zhong Yang; Yan-Ni Lin; Hua-Cheng Yang; Wei-Yi Pi; Zi-Cheng Li; Ying-Lan Zhao; You-Fu Luo; Yuquan Wei
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Publication Detail:
Type:  Journal Article     Date:  2012-02-24
Journal Detail:
Title:  Molecules (Basel, Switzerland)     Volume:  17     ISSN:  1420-3049     ISO Abbreviation:  Molecules     Publication Date:  2012  
Date Detail:
Created Date:  2012-02-27     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  100964009     Medline TA:  Molecules     Country:  Switzerland    
Other Details:
Languages:  eng     Pagination:  2351-66     Citation Subset:  IM    
Affiliation:
State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu, Sichuan 610041, China. alancenxb@sina.com.
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