| Autor: |
Yan-Ni Lin, Hua-Cheng Yang, Wei-Yi Pi, Zi-Cheng Li, Ying-Lan Zhao, You-Fu Luo, Yuquan Wei, Ying-Hong Yang, Jian-Zhong Yang, Hong He, Wei Ang, Tao Yang |
| Jazyk: |
angličtina |
| Rok vydání: |
2012 |
| Předmět: |
|
| Zdroj: |
Molecules, Vol 17, Iss 3, Pp 2351-2366 (2012) |
| Druh dokumentu: |
article |
| ISSN: |
1420-3049 |
| DOI: |
10.3390/molecules17032351 |
| Popis: |
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. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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