90771-17-8Relevant articles and documents
Identification and optimization of novel 6-acylamino-2-aminoquinolines as potent Hsp90 C-terminal inhibitors
Jiang, Fen,Guo, An-ping,Xu, Jia-cheng,Wang, Hui-Jie,Mo, Xiao-fei,You, Qi-Dong,Xu, Xiao-Li
, p. 1 - 14 (2017/10/16)
In order to discover novel Hsp90 inhibitors targeting the C-terminal ATP binding pocket, a novobiocin derivative based ROCS model was constructed for virtual screening. Compound 13 was identified as the lead compound and then systematical structure activity relationship (SAR) study was conducted. These efforts led to compound 69, which exhibited potent anti-proliferative activities against MCF7 and SKBr3 breast cancer cell lines. In 4T1 mice breast cancer models, 69 exhibited potent tumor growth inhibition and anti-metastasis effect. Compound 69 as a potent antitumor agent targeting the Hsp90 C-terminal is worthy of further pre-clinical study.
An environmentally benign one pot synthesis of substituted quinolines catalysed by fluoroboric acid based ionic liquid
Rajendran, A.,Karthikeyan, C.,Rajathi, K.,Ragupathy, D.
, p. 877 - 881,5 (2020/09/09)
Organic synthesis generally required large amount of solvent, avoiding the use of organic solvents in synthesis is a paradigm shift directed at developing more benign chemistry, and with ionic liquids surprisingly can lead to access to new compounds. An elegant one-pot synthesis of quinoline derivatives has been achieved by reaction of substituted anilines with β-ketoester at 60°C in ethanol using an ionic liquid [Et3NH]+[BF 4]- as catalyst. All the reactions gave products with high degree of purity and excellent yield (78.93%) within the shorter span of time (20.65 min) than those reactions with conventional methods. The screening of solvents as well as the reuse of ionic liquid has been evaluated. The structure of the products has been elucidated by spectral and analytical data. The present scope and potential economic impact of the reaction are demonstrated by the synthesis of substituted quinolines. Remaining challenges and future perspectives of the new transformation are discussed.
Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones
van Oeveren, Arjan,Motamedi, Mehrnoush,Martinborough, Esther,Zhao, Shuo,Shen, Yixing,West, Sarah,Chang, William,Kallel, Adam,Marschke, Keith B.,Lopez, Francisco J.,Negro-Vilar, Andres,Zhi, Lin
, p. 1527 - 1531 (2007/10/03)
A series of selective androgen receptor modulators (SARMs) with a wide spectrum of receptor modulating activities was developed based on optimization of the 4-substituted 6-bisalkylamino-2-quinolinones (3). Significance of the trifluoromethyl group on the side chains and its interactions with amino acid residues within the androgen receptor (AR) ligand binding domain are discussed. A representative analog (9) was tested orally in a rodent model of hypogonadism and demonstrated desirable tissue selectivity.
