3718-29-4Relevant articles and documents
Design and Synthesis of Novel Pyrazolo[3,4-d]Pyrimidines: In Vitro Cytotoxic Evaluation and Free Radical Scavenging Activity Studies
Alharthy, Rima D.
, (2020)
With evident biological importance, a new series of pyrazolo[3,4-d]pyrimidines 3a,3b and 4a,4b were synthesized via the formation of pyrazol-3-one 2a and 2b substrates. All compounds were evaluated for in vitro cytotoxic activity against MCF-7 (breast ade
Synthesis of 4,5-dihydropyrazolyl-2H-indenediones by aldol condensation of ninhydrin with 1H-pyrazol-5-ol
Soleimania, Ebrahim,Hariri, Mina,Rostamzadeh, Arman,Ghorbani, Somayeh
, p. 664 - 666 (2016/11/18)
A simple and efficient procedure for the synthesis of 2-hydroxy-2-(5-hydroxy-1H-pyrazol-4-yl)-2H-indene-1,3-dione derivatives, proceeding via aldol condensation between ninhydrin and various 3-alkyl-1H-pyrazol-5-ols is described. The syntheses were carried out in ethanol at room temperature and proceeded with short reaction times to give the products with high yields.
Synthesis, crystal structure and evaluation of cancer inhibitory activity of 4-[indol-3-yl-methylene]-1H-pyrazol-5(4H)-one derivatives
Jing, Lingling,Wang, Liang,Zhao, Yinglan,Tan, Rui,Xing, Xiumei,Liu, Ting,Huang, Wencai,Luo, Youfu,Li, Zicheng
, p. 691 - 696 (2013/02/23)
A series of 4-(1H-indol-3-yl-methylene)-1H-pyrazol-5(4H)-one derivatives have been synthesised. The Z structure of 4-[(1-methyl-1H-indol-3-yl)methylene]- 3-phenyl-1-p-tolyl-1H-pyrazol-5-one was determined by X-ray crystallography. The antitumour activity was evaluated against five cancer cells by MTT assay. [(1H-Indol-3-yl)methylene]-1-(2,4-dinitrophenyl)- 3-methyl-1H-pyrazole-5-one and 4-{4-[(1-benzyl-1H-indol-3-yl)methylene]-3-methyl-5-oxo-4,5-dihydro-1Hpyrazol- 1-yl}-benzoic acid have similar anticancer activity with 5-UF on the test cancer cells (exception of A375). Almost all the target compounds displayed antitumour activity against A549 and PC-9, and those with benzyl at 1- position of indole had higher activity against PC-9 (IC50 value lower than 30 μM). Those with benzyl at the indole and carboxyl at the phenyl part of of pyrazole were more active against PC-9 and A549 cells, providing a good indication for subsequent optimisation as lung cancer inhibitory agents.