186593-43-1Relevant articles and documents
MACROCYCLIC AZOLOPYRIDINE DERIVATIVES AS EED AND PRC2 MODULATORS
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Paragraph 1250, (2020/10/09)
The invention relates to modulators of Embryonic Ectoderm Development (EED) and/or Polycomb Repressive Complex 2 (PRC2) useful in the treatment of disorders and diseases associated with EEC and PRC2, being macrocyclic azolopyridine derivatives and compositions thereof of Formula (I), or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, enantiomer, isomer, or tautomer thereof, wherein X1, X2, X3, A1, A2, Y, R1, R2, R3, and R4 are as described herein.
Enzyme-Inspired Axially Chiral Pyridoxamines Armed with a Cooperative Lateral Amine Chain for Enantioselective Biomimetic Transamination
Liu, Yong Ethan,Lu, Zhaole,Li, Bo,Tian, Jiaxin,Liu, Feng,Zhao, Junyu,Hou, Chengkang,Li, Yingkun,Niu, Lili,Zhao, Baoguo
supporting information, p. 10730 - 10733 (2016/09/09)
Enzymatic transamination is catalyzed by pyridoxal/pyridoxamine, and it involves remarkable cooperative catalysis of a Lys residue in the transaminase. Inspired by transaminases, we developed a class of axially chiral pyridoxamines 11 bearing a lateral amine arm. The pyridoxamines exhibited high catalytic activity and excellent enantioselectivity in asymmetric transamination of α-keto acids, to give various α-amino acids in 67-99% yields with 83-94% ee's. The lateral amine arm likely participates in cooperative catalysis as the Lys residue does in biological transamination and has an important impact on the transamination in terms of activity and enantioselectivity.
Anti-tumor activity with acetylene derivatives
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Paragraph 0293-0296, (2016/10/08)
The present invention relates to an aromatic ring disubstituted acetylene derivative of formula I, a pharmaceutical composition comprising the compound, and a use of the compound and of the pharmaceutical composition in the treatment and/or prevention of tumors, where A, B, T, M, Ra, Rb, Rt, m, n, and p are as defined in the present document.