193290-27-6Relevant articles and documents
Antiproliferative activity and SARs of caffeic acid esters with mono-substituted phenylethanols moiety
Xie, Jin,Yang, Fengzhi,Zhang, Man,Lam, Celine,Qiao, Yixue,Xiao, Jia,Zhang, Dongdong,Ge, Yuxuan,Fu, Lei,Xie, Dongsheng
, p. 131 - 134 (2016/12/27)
A series of CAPE derivatives with mono-substituted phenylethanols moiety were synthesized and evaluated by MTT assay on growth of 4 human cancer cell lines (Hela, DU-145, MCF-7 and ECA-109). The substituent effects on the antiproliferative activity were systematically investigated for the first time. It was found that electron-donating and hydrophobic substituents at 2′-position of phenylethanol moiety could significantly enhance CAPE's antiproliferative activity. 2′-Propoxyl derivative, as a novel caffeic acid ester, exhibited exquisite potency (IC50?=?0.4?±?0.02 & 0.6?±?0.03?μM against Hela and DU-145 respectively).
CHEMICAL COMPOUNDS 428
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Page/Page column 57, (2010/11/30)
Compounds of formula (I): wherein variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are described.
Design, synthesis and biological activity of YM-60828 derivatives: Potent and orally-bioavailable factor Xa inhibitors based on naphthoanilide and naphthalensulfonanilide templates
Hirayama, Fukushi,Koshio, Hiroyuki,Ishihara, Tsukasa,Watanuki, Susumu,Hachiya, Shunichiro,Kaizawa, Hiroyuki,Kuramochi, Takahiro,Katayama, Naoko,Kurihara, Hiroyuki,Taniuchi, Yuta,Sato, Kazuo,Sakai-Moritani, Yumiko,Kaku, Seiji,Kawasaki, Tomihisa,Matsumoto, Yuzo,Sakamoto, Shuichi,Tsukamoto, Shin-ichi
, p. 2597 - 2610 (2007/10/03)
Factor Xa (FXa) is a serine protease which plays a pivotal role in the coagulation cascade. The inhibition of FXa has received great interest as a potential target for the development of new antithrombotic drug. Herein we describe a series of novel 7-amidino-2-naphthoanilide and 7-amidino-2-naphthalensulfonanilide derivatives which are potent FXa inhibitors. These scaffolds are rigid and are allowed to adopt an L-shape conformation which was estimated as the active conformation based on a docking study of YM-60828 with FXa. Optimization of the side chain at the central aniline nitrogen of 7-amidino-2-naphthoanilide has led to several potent and orally active FXa inhibitors. 5h (YM-169964), the best compound of these series, showed potent FXa inhibitory activity (IC50=3.9 nM) and effectively prolonged prothrombin time by 9.6-fold ex vivo at an oral dose of 3 mg/kg in squirrel monkeys.
