16798-54-2Relevant academic research and scientific papers
4-Hydroxy-2-quinolones. 40. Synthesis and biological properties of anilides of 1H-2-oxo-4-hydroxyquinoline-3-carboxylic acid
Ukrainets,Taran,Gorokhova,Taran,Jaradat,Petukhova
, p. 166 - 169 (2000)
An improved method for the synthesis of anilides of 1H-2-oxo-4-hydroxyquinoline-3-carboxylic acid was proposed. Results of the study of antithyroid and anti-tuberculosis activity of the compounds synthesized are presented.
Synthesis, Structure–Activity Relationship Studies, and ADMET Properties of 3-Aminocyclohex-2-en-1-ones as Chemokine Receptor 2 (CXCR2) Antagonists
Dai, Weiyang,Chen, Wenmin,Debnath, Bikash,Wu, Yong,Neamati, Nouri
, p. 916 - 930 (2018/05/15)
Herein we describe the synthesis and structure–activity relationships of 3-aminocyclohex-2-en-1-one derivatives as novel chemokine receptor 2 (CXCR2) antagonists. Thirteen out of 44 derivatives were found to inhibit CXCR2 downstream signaling in a Tango a
N-Phenyl-4-hydroxy-2-quinolone-3-carboxamides as selective inhibitors of mutant H1047R phosphoinositide-3-kinase (PI3Kα)
Sabbah, Dima A.,Simms, Neka A.,Wang, Wang,Dong, Yuxiang,Ezell, Edward L.,Brattain, Michael G.,Vennerstrom, Jonathan L.,Zhong, Haizhen A.
, p. 7175 - 7183 (2013/01/15)
This work describes our efforts to optimize the lead PI3Kα inhibitor N-benzyl 4-hydroxy-2-quinolone-3-carboxamide using structure-based design and molecular docking. We identified a series of N-phenyl 4-hydroxy-2-quinolone-3- carboxamides as selective inhibitors of mutant H1047R versus wild-type PI3Kα and we also showed that the cell growth inhibition by these compounds likely occurs by inhibiting the formation of pAKT and induction of apoptosis.
4-Hydroxy-2-quinolones. 110. Bromination of 1-R-4-hydroxy-2-oxo-1,2- dihydroquinoline-3-carboxylic acid anilides
Ukrainets,Tkach,Sidorenko,Gorokhova
, p. 1301 - 1307 (2008/09/18)
1-R-4-Hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acid anilides have been prepared. It has been shown experimentally that these compounds are brominated by molecular bromine in glacial acetic acid at position 4 of the anilide fragment. The antitubercular properties of the compounds synthesized are discussed.
Structure-activity relationships studies of the anti-angiogenic activities of linomide
Shi, Jiandong,Xiao, Zili,Ihnat, Michael A.,Kamat, Chandrashekhar,Pandit, Bulbul,Hu, Zhigen,Li, Pui-Kai
, p. 1187 - 1189 (2007/10/03)
The synthesis and anti-angiogenic activities of linomide and its analogues are reported. Three of the analogues are 3.3-69 times more potent than linomide at inhibiting blood vessel formation in the CAM angiogenesis assay. These compounds possessed consid
