441067-49-8Relevant articles and documents
A sub-milligram-synthesis protocol for in vitro screening of HDAC11 inhibitors
Tian, Yinping,Jin, Jin,Wang, Congying,Lv, Wenhui,Li, Xuewei,Che, Xiaona,Gong, Yanchao,Li, Yanjun,Li, Quanli,Hou, Jingli,Wang, Peng G.,Shen, Jie
supporting information, p. 2434 - 2437 (2016/07/07)
This work demonstrated the high efficiency of a sub-milligram-synthesis based medicinal chemistry method. Totally 72 compounds, consisting a tri-substituted pyrrolidine core, were prepared. Around 0.1 mg of each compound was solid-phase synthesized. Based on the additive property of UV absorptions of unconjugated chromophores of a molecule, these compounds were quantified by UV measurement. A hit, whose IC50 value was 1.2 μM in HDAC11 inhibition assays, highlights the applicability of the approach reported here in future optimization works.
PHENYL AMINO PYRIMIDINE BICYCLIC COMPOUNDS AND USES THEREOF
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, (2014/01/17)
The present invention relates to phenyl amino pyrimidine bicyclic compounds formula (I) which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
Design and stereoselective synthesis of four peptide nucleic acid monomers with cyclic structures in backbone
Watanabe, Akiko,Kiyota, Naotoshi,Yamasaki, Tetsuo,Tanda, Kazuhiro,Miyagoe, Tatsunori,Sakamoto, Masanori,Otsuka, Masami
experimental part, p. 1132 - 1139 (2011/11/05)
Four isomers of the monomer of peptide nucleic acid (PNA) were derived from (2S,4R)-4-hydroxyproline; they had different stereochemistries at the C 2 and C4 positions in the pyrrolidine ring. These different backbone conformations corresponding to four different stereochemistries were realized through a combination of inversions at the C2 and the C4 positions in pyrrolidine ring. The obtained backbone frameworks were reacted with N-benzoyl thymine to give the corresponding PNA monomers. Spectroscopic comparison of the resultant monomers confirmed their stereochemistries.