618913-77-2Relevant academic research and scientific papers
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
, (2020/04/10)
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.
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
