Chemistry is an experimental science, Recommanded Product: 58481-14-4, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 58481-14-4, Name is Ethyl 2-cyanoisonicotinate, molecular formula is C9H8N2O2, belongs to pyridine-derivatives compound. In a document, author is Hao, Shu-Yi.
Synthesis and bioevaluation of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo [3,4-b]pyridin-3-amines as tubulin polymerization inhibitors with anti-angiogenic effects
A new series of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amine derivatives as tubulin polymerization inhibitors were synthesized, and evaluated for the anti-proliferative activities. A structure-activity relationship study revealed that the free amino moiety of 1H-pyrazolo[3,4-b]pyridin-3-amine played an essential role in the anti-proliferative activities. Especially, compound 15c displayed the strongest anti-proliferation against MCF-7 cells with IC50 value of 0.067 +/- 0.003 mu M, and high selectivity over the normal human embryonic lung WI-38 cells with IC50 value of 23.41 +/- 1.53 mu M. Further mechanistic studies revealed that 15c showed strong anti-tubulin polymerization activity, changed the morphology of tubulin, and arrested the cell cycle at the G2/M transition in MCF-7 cells. Molecular docking analysis suggested that 15c well occupied the colchicinebinding pocket of tubulin. Additionally, 15c demonstrated anti-angiogenic activities with blocking the migration, invasion and tube formation, disrupting the newly formed tube, and regulating both MMP-9 and TIMP-1 in HUVEC cells. In summary, our results highlight that compound 15c is a potential antitumor compound that are worthy of further development.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 58481-14-4, in my other articles. Recommanded Product: 58481-14-4.
Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem