2675-89-0Relevant articles and documents
Studies in sulfur-nitrogen nucleophilicity
Caserio, Marjorie C.,Kim, Jhong K.
, (2018)
As part of a study of nitrogen vs sulfur nucleophiles, the behavior of methylation products from dimethyl-(2-methylthioethyl)amine CH3SCH2CH2N(CH3)2 1 is described. Of the 2 potential products (a sulf
Design, synthesis, and biological evaluation of 2,6,7-substituted pyrrolo[2,3-d]pyrimidines as cyclin dependent kinase inhibitor in pancreatic cancer cells
Shi, Xingpeng,Quan, Yanni,Wang, Yixuan,Wang, Ying,Li, Yanping
supporting information, (2020/12/29)
Pancreatic cancer is a highly malignant tumor, and more effective treatment is urgently needed to lengthen the life of patients. In this paper a class of new 2,6,7-substituted pyrrolo[2,3-d]pyrimidine derivatives of CDK 4/6 inhibitor ribociclib (1) was de
Novel selective ido1 inhibitors with isoxazolo[5,4-d]pyrimidin-4(5h)-one scaffold
?vajger, Urban,Bratkovi?, Toma?,Dol?ak, Ana,Gobec, Stanislav,Mlinari?, Larisa,Ogorevc, Eva,Sova, Matej
, (2021/04/02)
Indoleamine 2,3-dioxygenase 1 (IDO1) is a promising target in immunomodulation of several pathological conditions, especially cancers. Here we present the synthesis of a series of IDO1 inhibitors with the novel isoxazolo[5,4-d]pyrimidin-4(5H)-one scaffold. A focused library was prepared using a 6-or 7-step synthetic procedure to allow a systematic investigation of the structure-activity relationships of the described scaffold. Chemistry-driven modifications lead us to the discovery of our best-in-class inhibitors possessing p-trifluoromethyl (23), p-cyclohexyl (32), or p-methoxycarbonyl (20, 39) substituted aniline moieties with IC50 values in the low micromolar range. In addition to hIDO1, compounds were tested for their inhibition of indoleamine 2,3-dioxygenase 2 and tryptophan dioxygenase, and found to be selective for hIDO1. Our results thus demon-strate a successful study on IDO1-selective isoxazolo[5,4-d]pyrimidin-4(5H)-one inhibitors, defining promising chemical probes with a novel scaffold for further development of potent small-molecule immunomodulators.
Design, synthesis and evaluation of new indolylpyrimidylpiperazines for gastrointestinal cancer therapy
Tan, Aaron,Babak, Maria V.,Venkatesan, Gopalakrishnan,Lim, Clarissa,Klotz, Karl-Norbert,Herr, Deron Raymond,Cheong, Siew Lee,Federico, Stephanie,Spalluto, Giampiero,Ong, Wei-Yi,Chen, Yu Zong,Loo, Jason Siau Ee,Pastori, Giorgia
, (2019/11/02)
Human A3 adenosine receptor hA3AR has been implicated in gastrointestinal cancer, where its cellular expression has been found increased, thus suggesting its potential as a molecular target for novel anticancer compounds. Observation