96923-01-2Relevant articles and documents
Rational Design and Evaluation of 6-(Pyrimidin-2-ylamino)-3,4-dihydroquinoxalin-2(1 H)-ones as Polypharmacological Inhibitors of BET and Kinases
Lv, Kaikai,Chen, Weicong,Chen, Danqi,Mou, Jie,Zhang, Huijie,Fan, Tiantian,Li, Yanlian,Cao, Danyan,Wang, Xin,Chen, Lin,Shen, Jingkang,Pei, Dongsheng,Xiong, Bing
, p. 9787 - 9802 (2020/10/19)
Cancer exhibits diverse heterogeneity with a complicated molecular basis that usually harbors genetic and epigenetic abnormality, which poses a big challenge for single-target agents. In the current work, we proposed a hybrid strategy by incorporating pharmacophores that bind to the acetylated lysine binding pocket of BET proteins with a typical kinase hinge binder to generate novel polypharmacological inhibitors of BET and kinases. Through elaborating the core structure of 6-(pyrimidin-2-ylamino)-3,4-dihydroquinoxalin-2(1H)-one, we demonstrated that this rational design can produce high potent inhibitors of CDK9 and BET proteins. In this series, compound 40 was identified as the potential lead compound with balanced activities of BRD4 (IC50 = 12.7 nM) and CDK9 (IC50 = 22.4 nM), as well as good antiproliferative activities on a small cancer cell panel. Together, the current study provided a new method for the discovery of bromodomain and kinase dual inhibitors rather than only being discovered by serendipity.
Poly(: O -aminothiophenol)-stabilized Pd nanoparticles as efficient heterogenous catalysts for Suzuki cross-coupling reactions
Chen, Yuan,Wang, Minggui,Zhang, Long,Liu, Yan,Han, Jie
, p. 47104 - 47110 (2017/10/16)
Poly(o-aminothiophenol) (PATP)-stabilized Pd nanoparticles with Pd nanoparticles embedded in a polymer matrix have been obtained through a facile one-step route by mixing o-aminothiophenol monomer and Pd(NO3)2 in an acidic aqueous solution without additional template or surfactant. The redox reaction between o-aminothiophenol and Pd(NO3)2 leads to the simultaneous formation of a PATP polymer and Pd nanoparticles. The PATP-stabilized Pd nanoparticles have been characterized by TEM, FTIR, XRD, ICP-MS and XPS. Catalytic results showed that PATP-stabilized Pd nanoparticles were highly stable and active catalysts for Suzuki cross-coupling reactions, where high yields could be achieved with arylboronic acid and aryl halides bearing a variety of substituents.
Pd/mannose promoted tandem cross coupling-nitro reduction: Expedient synthesis of aminobiphenyls and aminostilbenes
Rohilla, Sandeep,Pant, Pradeep,Jain, Nidhi
, p. 31311 - 31317 (2015/04/22)
The dual role of d-mannose as a ligand for Pd catalyzed cross-coupling, and as a hydrogen source for nitro reduction is demonstrated in a modular cross coupling-nitro reduction sequence. The synthetic utility and generality of this green protocol has been illustrated by the synthesis of 20 aminobiphenyl and 10 aminostilbene derivatives in high yields through a one-pot Suzuki coupling-nitro reduction and a Heck coupling-nitro reduction, respectively, starting from halonitroarenes as substrates.
