500859-97-2Relevant articles and documents
Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease
Cao, Zhongcheng,Song, Qing,Yu, Guangjun,Liu, Zhuoling,Cong, Shiqing,Tan, Zhenghuai,Deng, Yong
, (2021/03/01)
To discover novel multifunctional agents for the treatment of Alzheimer's disease, a series of 3-benzylidene/benzylphthalide Mannich base derivatives were designed, synthesized and evaluated. The biological screening results indicated that most of these d
Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties
Li, Yan,Qiang, Xiaoming,Luo, Li,Yang, Xia,Xiao, Ganyuan,Zheng, Yunxiaozhu,Cao, Zhongcheng,Su, Fu,Deng, Yong,Sang, Zhipei
, p. 714 - 726 (2016/12/30)
A series of homoisoflavonoid Mannich base derivatives were designed, synthesized and evaluated as multifunctional agents against Alzheimer's disease. It demonstrated that most of the derivatives were selective AChE and MAO-B dual inhibitors with good mult
Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy
Torrente, Esther,Parodi, Chiara,Ercolani, Luisa,De Mei, Claudia,Ferrari, Alessio,Scarpelli, Rita,Grimaldi, Benedetto
supporting information, p. 5900 - 5915 (2015/08/24)
Autophagy inhibition is emerging as a promising anticancer strategy. We recently reported that the circadian nuclear receptor REV-ERBβ plays an unexpected role in sustaining cancer cell survival when the autophagy flux is compromised. We also identified 4-[[[1-(2-fluorophenyl)cyclopentyl]amino]methyl]-2-[(4-methylpiperazin-1-yl)methyl]phenol, 1 (ARN5187), as a novel dual inhibitor of REV-ERBβ and autophagy. 1 had improved cytotoxicity against BT-474 breast cancer cells compared to chloroquine, a clinically relevant autophagy inhibitor. Here, we present the results of structure-activity studies, based around 1, that disclose the first class of dual inhibitors of REV-ERBβ and autophagy. This study led to identification of 18 and 28, which were more effective REV-ERBβ antagonists than 1 and were more cytotoxic to BT-474. The combination of optimal chemical and structural moieties of these analogs generated 30, which elicited 15-fold greater REV-ERBβ inhibitory and cytotoxic activities compared to 1. Furthermore, 30 induced death in a panel of tumor cell lines at doses 5-50 times lower than an equitoxic amount of chloroquine but did not affect the viability of normal mammary epithelial cells.
DIARYLALKYLAMINE REV-ERB ANTAGONISTS AND THEIR USE AS MEDICAMENTS
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Page/Page column 43; 44; 66; 72; 73; 74, (2015/04/28)
The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof : It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses as anti-proliferative and pro-apoptotic agents for cancer therapy.
NOVEL AMINOMETHYL-PHENOL DERIVATIVES AS ANTIMALARIAL AGENTS
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Page/Page column 69, (2014/05/24)
The invention relates to novel aminomethyl-phenol derivatives of formula I wherein R1 to R4, X, A and B are as defined for formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention
Metal complexes with nitronyl nitroxide substituted phenolate ligands providing new magnetic exchange interaction pathways - Synthesis, structures, magnetic dilution studies, and Ab initio calculations
Schatzschneider, Ulrich,Weyhermueller, Thomas,Rentschler, Eva
, p. 2569 - 2586 (2007/10/03)
The synthesis and magnetic properties of seven new nitronyl nitroxide substituted phenolates with chelating amine groups are reported. Copper(II) and nickel(II) complexes prepared with these ligands are structurally and magnetically characterized, showing
