373627-28-2Relevant articles and documents
Synthesis, biological evaluation and molecular docking studies of pyrazole derivatives coupling with a thiourea moiety as novel CDKs inhibitors
Sun, Jian,Lv, Xian-Hai,Qiu, Han-Yue,Wang, Yan-Ting,Du, Qian-Ru,Li, Dong-Dong,Yang, Yong-Hua,Zhu, Hai-Liang
, p. 1 - 9 (2013)
It was discovered that a number of cyclin dependent kinase inhibitors containing the pyrazole core structure exhibited high inhibitory potency against broad-range CDKs and corresponding anti-proliferative activities. This information guided us to design and synthesize a series of 1,3-diphenyl-N- (phenylcarbamothioyl)-1H-pyrazole-4-carboxamide derivatives (5a-10d), and evaluate their biological activities as CDKs inhibitors. Among all the synthesized compounds, compound 10b inhibited CDK2 with an IC50 value of 25 nM, counteracting tumor cell proliferation of three cancer cell lines (H460, MCF-7, A549) in the micromolar range (from 0.75 μM to 4.21 μM), In addition, flow cytometry indicated that compound 10b could induce cycle G 0/G1 phase arrest in A549 cells with a dose dependent. Taken together, compound 10b could be selected for further preclinical evaluation.
4-Functionally substituted 3-heterylpyrazoles: III. 3-aryl(heteryl)pyrazole-4-carboxylic acids and their derivatives
Bratenko,Chornous,Vovk
, p. 552 - 555 (2007/10/03)
3-Aryl(heteryl)-4-formylpyrazoles were cleanly oxidized by potassium permanganate in water-pyridine medium to afford in high yield 3-aryl(heteryl)pyrazole-4-carboxylic acids, that were further converted into the corresponding chlorides and amides.