55153-64-5Relevant academic research and scientific papers
Synthesis and antibacterial in vitro activity of novel analogues of nematophin
Himmler, Thomas,Pirro, Franz,Schmeer, Norbert
, p. 2045 - 2050 (1998)
The synthesis and in vitro antibacterial activity of new derivatives and analogues of nematophin are described. It was shown that the unsubstituted amide NH-group is essential for bioactivity. Alkyl- or aryl-substitution at the 1-position results in a distinct increase of antibacterial activity. Addition of protein (blood or serum) to the culture media reduces the inhibitory activity on bacteria.
Synthesis of polycyclic spiro-fused indolines via IBX-mediated cascade cyclization
Zhang, Zhiguo,Song, Xiaoqing,Li, Guofeng,Li, Xiang,Zheng, Dan,Zhao, Xuna,Miao, Huanran,Zhang, Guisheng,Liu, Lantao
, p. 1423 - 1426 (2021)
We report a 2-iodoxybenzoic acid (IBX)-mediated intarmolecular oxidative spiro-fused tandem cyclization reaction of tryptophan analogs bearing an N-arylamides side-chain to rapidly afford polycyclic spiroindolines featuring multiple stereocenters includin
Iodide/H2O2 catalyzed intramolecular oxidative amination for the synthesis of 3,20-pyrrolidinyl spirooxindoles
Gao, Yu-Ting,Jin, Xiao-Yang,Liu, Qi,Liu, An-Di,Cheng, Liang,Wang, Dong,Liu, Li
supporting information, (2018/09/12)
An ammonium iodide/hydrogen peroxide-mediated intramolecular oxidative amination of 3-aminoalkyl-2-oxindoles was achieved, affording the corresponding 3,20-pyrrolidinyl spirooxindoles and their 6- or 7-membered analogous in moderate to high yields. This metal-free procedure features very mild reaction conditions, non-toxicity and easily handled hydrogen peroxide as a clean oxidant.
Design, synthesis and activity evaluation of some novel indole derivatives
He, Dian,Yang, Zhu-Qing,Hou, Meng
, p. 1729 - 1734 (2015/03/04)
A series of novel indole derivatives as CDK4 inhibitors were designed and synthesized though the condensation reaction between the indolic acid and the corresponding substituted amine. The key step of our synthetic process is the efficient condensation reaction conducted by two different methods. The MTT and kinase assays were conducted used to assess the antitumor activity and cyclin-dependent kinases (CDKs) inhibitory activity. The most active compound 8b has an IC50 of 10-25 μM for the inhibition of four different tumor cells and CDK4. The higher activities of 8b were influenced by more conformational freedom resulted form the non-planar structure and by the stronger hydrogen bonding capability. Thus, the strategy we adapt to design potent, non-toxic CDK4 inhibitors is successful.
