131231-24-8Relevant articles and documents
Selective Targeting of the TPX2 Site of Importin-α Using Fragment-Based Ligand Design
Holvey, Rhian S.,Valkov, Eugene,Neal, David,Stewart, Murray,Abell, Chris
, p. 1232 - 1239 (2015)
Protein-protein interactions are difficult therapeutic targets, and inhibiting pathologically relevant interactions without disrupting other essential ones presents an additional challenge. Herein we report how this might be achieved for the potential ant
Iron(II)-Based Metalloradical Activation: Switch from Traditional Click Chemistry to Denitrogenative Annulation
Roy, Satyajit,Khatua, Hillol,Das, Sandip Kumar,Chattopadhyay, Buddhadeb
supporting information, p. 11439 - 11443 (2019/07/17)
A unique concept for the intermolecular denitrogenative annulation of 1,2,3,4-tetrazoles and alkynes was discovered by using a catalytic amount of Fe(TPP)Cl and Zn dust. The reaction precludes the traditional, more favored click reaction between an organic azide and alkynes, and instead proceeds by an unprecedented metalloradical activation. The method is anticipated to advance access to the construction of important basic nitrogen heterocycles, which will in turn enable discoveries of new drug candidates.
Synthesis and characterization of Sant-75 derivatives as Hedgehog-pathway inhibitors
Che, Chao,Li, Song,Yang, Bo,Xin, Shengchang,Yu, Zhixiong,Shao, Taofeng,Tao, Chuanye,Lin, Shuo,Yang, Zhen
scheme or table, p. 841 - 849 (2012/07/28)
Sant-75 is a newly identified potent inhibitor of the hedgehog pathway. We designed a diversity-oriented synthesis program, and synthesized a series of Sant-75 analogues, which lays the foundation for further investigation of the structure-activity relationship of this important class of hedgehog-pathway inhibitors.