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- Title
Syntheses and Cell-Based Phenotypic Screen of Novel 7-Amino pyrido[2,3-d]pyrimidine-6-carbonitrile Derivatives as Potential Antiproliferative Agents.
- 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
- 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 μM. Structural optimization of compound 3k led to compound 4a with improved anti-proliferative potency on SW620 cells with an IC50 value of 6.9 μM. Further cell-cycle analyses suggested that compound 4a induced apoptosis of SW620 cells in a concentration-dependent manner.
- Subjects
STRUCTURE-activity relationship in pharmacology; APOPTOSIS; CELL death; CARBONITRILES; CELL proliferation; COLON cancer prevention; CELL cycle
- Publication
Molecules, 2012, Vol 17, Issue 3, p2351
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules17032351