13031-53-3Relevant articles and documents
Synthesis and cytotoxic evaluation of some new phthalazinylpiperazine derivatives
Liu, Yajing,Zhang, Shulan,Li, Ye,Wang, Jianqiang,Song, Yu,Gong, Ping
experimental part, p. 287 - 293 (2012/07/01)
A new series of 1,4-disubstituted phthalazinylpiperazine derivatives 7a-f, 12a-f and 20a-f were designed and synthesized in order to develop potent and selective antitumor agents. The target compounds were screened for their cytotoxic activities against A549, HT-29 and MDA-MB-231 cancer cell lines in vitro. Among them, compounds 7a-f exhibited excellent selectivity for MDA-MB-231 with IC50 values ranging from 0.013 μM to 0.079 μM. The most promising compound, 7e (IC50 = 2.19 μM, 2.19 μM, 0.013 μM), was 9.3, 10, and 4.9 × 103 times more active than vatalanib (IC50 = 20.27 μM, 21.96 μM, 63.90 μM), respectively. A new series of 1,4-disubstituted phthalazinylpiperazine derivatives 7a-f, 12a-f and 20a-f were designed and synthesized, and their cytotoxic activities against A549, HT-29 and MDA-MB-231 cancer cell lines in vitro were compared to that of vatalanib.
Synthesis and antitumor activities of novel 1,4-substituted phthalazine derivatives
Zhang, Shu Lan,Liu, Ya Jing,Zhao, Yan Fang,Guo, Qiu Ting,Gong, Ping
scheme or table, p. 1071 - 1074 (2011/10/05)
A series of 1,4-substituted phthalazine derivatives were 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, compounds 7a-7h showed excellent selectivity for MDA-MB-231 cell line with IC50 values from 1nmol/L to 0.92μmol/L. A preliminary SAR study of these derivatives was performed.
The Chemistry of Phthalide-3-carboxylic Acid. II. Decarboxylation of Salts in the Presence of Aldehydes
Dibbens, Justin A.,Prager, Rolf H.,Schiesser, Carl H.,Wells, Andrew J.
, p. 913 - 920 (2007/10/02)
Salts of phthalide-3-carboxylic acid decarboxylate in the presence of aromatic aldehydes to give mixtures of the 3-(arylhydroxymethyl)phthalide (2) and the 2-aryl-3-hydroxyindenone (3).The former may be obtained exclusively in the presence of the weak proton donor, triethyl(2-phenylethyl)ammonium chloride, and the latter in the presence of crown ethers or after longer reaction times.A study of the effect of different cations allows a mechanism to be deduced.