597565-49-6Relevant articles and documents
Synthesis and biological evaluation of heterocyclic bis-aryl amides as novel Src homology 2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitors
Feng, Bo,Gao, Li-Xin,Gao, Ya,Hou, Ting-Jun,Huang, Chao,Li, Jia,Satheeshkumar, Rajendran,Shen, Chao,Wang, Wen-Long,Xu, Lei,Zhou, Yu-Bo,Zhu, Rui,Zhu, Yun-Long
, (2020)
The Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2) is a convergent node for oncogenic cell-signaling cascades including the PD-L1/PD-1 pathway. Consequently, SHP2 has emerged as a compelling target for novel anti-cancer agents. Replacing one of phenyl ring in PTP1B inhibitor 1 with heterocyclic ring led to a series of heterocyclic bis-aryl amide derivatives. The representative compound 7b displayed SHP2 inhibitory activity with IC50 of 2.63 ± 0.08 μM, exhibited about 4-fold selectivity for SHP2 over TCPTP and had no detectable activity against SHP1 and PTP1B. These preliminary results could provide a possible opportunity for the development of novel SHP2 inhibitors with optimal potency and improved pharmacological properties.
A kind of benzene ring - aromatic ring series compound, its preparation method and medical use
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Paragraph 0152-0155, (2017/12/05)
The invention relates to a phenyl ring-aromatic ring cascaded micro-molecular organic compound which can be used as a protein-tyrosine-phosphatase subtype inhibitor and is shown in a general formula I as described in the specification. The compound can be used as a tool compound for research on the biological functions of a variety of subtypes of a protein-tyrosine-phosphatase family in cell signal transduction, so novel means is provided for prevention and treatment of cancers, metabolism and immunological diseases, cardiovascular diseases and nervous diseases. The invention also relates to a preparation method and medicinal application of the compound.
Synthesis of new cyano-substituted bis-benzothiazolyl arylfurans and arylthiophenes
Racanè, Livio,Trali?-Kulenovi?, Vesna,Boykin, David W.,Karminski-Zamola, Grace
, p. 342 - 349 (2007/10/03)
The new compounds 2-[4-(6-cyanobenzothiazol-2-yl)phenyl]-5-(6-cyano- benzothiazol-2-yl)furan (6a) and 2-[4-(6-Cyanobenzothiazol-2-yl)phenyl]-5-(6- cyano-benzothiazol-2-yl)thiophene (6b) were synthesized by multi-step reactions from the corresponding 2-fur