107558-48-5Relevant articles and documents
Simple preparation method of 4-substituted methyl-1-(2H)-phthalazinone
-
, (2019/08/30)
The invention provides a simple preparation method of 4-substituted methyl-1-(2H)-phthalazinone (I). According to the method, condensation is carried out on a two G substituted benzene (II) and a compound represented by a formula III in the presence of a solvent A and an alkali, a compound represented by a formula IV is obtained through hydrolysis, and then, condensation is carried out on the compound represented by the formula IV or an esterification product of the compound represented by the formula IV and hydrazine hydrate to prepare 4-(pyridin-4-yl)-methyl-1-(2H)-phthalazinone (IA) or 4-(4-fluoro-3-carboxyphenyl)methyl-1-(2H)-phthalazinone (IB) which can be used for preparing vatalanib and olaparib. The preparation method is simple and convenient in technological process, is high in reaction reproducibility, is easy to operate, and is good in product stability and high in purity.
Synthesis and antitumor activities of novel 1,4-disubstituted phthalazine derivatives
Zhang, Shulan,Zhao, Yanfang,Liu, Yajing,Chen, Dong,Lan, Weihuan,Zhao, Qiaoling,Dong, Chengcheng,Xia, Lin,Gong, Ping
experimental part, p. 3504 - 3510 (2010/08/06)
In an attempt to develop potent and selective antitumor agents,a series of novel 1,4-disubstituted phthalazine derivatives was designed and synthesized. All the prepared compounds were screened for their cytotoxic activities against A549,HT-29 and MDA-MB-231 cell lines in vitro. Among them,seven compounds (7a7e,7j and 7i) displayed excellent selectivity for MDA-MB-231 cells with IC50 values in the nM range,a desirable range for pharmacological testing. The most promising compound,7a (IC50 = 3.79 μ M,2.32 μ M,0.84 nM),was 5.6-,10.8-and 6.9 × 104-times more active than PTK-787 (IC50 = 21.16 μ M,22.11 μ M,57.72 μ M),respectively.
DIARYLAMINE-CONTAINING COMPOUNDS AND COMPOSITIONS, AND THEIR USE AS MODULATORS OF STEROID HORMONE NUCLEAR RECEPTORS
-
Page/Page column 60, (2008/06/13)
Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of steroid hormone nuclear receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent diseases or conditions associated with the activity of steroid hormone nuclear receptors.