Syntheses and cell-based phenotypic screen of novel 7-amino pyrido[2,3-d]pyrimidine-6-carbonitrile derivatives as potential antiproliferative agents |
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Authors: | 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 |
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Institution: | State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu, Sichuan 610041, China. |
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Abstract: | A series of N-3-substituted 7-aminopyrido2,3-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. |
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