55023-35-3Relevant academic research and scientific papers
Discovery of structurally distinct tricyclic M4 positive allosteric modulator (PAM) chemotypes – Part 2
Bollinger, Sean R.,Bridges, Thomas M.,Capstick, Rory A.,Chang, Sichen,Cho, Hyekyung P.,Conn, P. Jeffrey,Engers, Darren W.,Engers, Julie L.,Gregro, Alison R.,Lindsley, Craig W.,Long, Madeline F.,Luscombe, Vincent B.,Niswender, Colleen M.,Rodriguez, Alice L.,Spearing, Paul K.,Temple, Kayla J.
supporting information, (2021/11/16)
This Letter details our efforts to develop novel tricyclic M4 PAM scaffolds with improved pharmacological properties. This endeavor involved a “tie-back” strategy to replace the 3-amino-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide core which lead to the discovery of two novel tricyclic cores: a 7,9-dimethylpyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine core and 2,4-dimethylthieno[2,3-b:5,4-c′]dipyridine core. Both tricyclic cores displayed low nanomolar potency against the human M4 receptor.
Synthesis and evaluation of pyrido-thieno-pyrimidines as potent and selective Cdc7 kinase inhibitors
Zhao, Chunlin,Tovar, Christian,Yin, Xuefeng,Xu, Qui,Todorov, Ivan T.,Vassilev, Lyubomir T.,Chen, Li
scheme or table, p. 319 - 323 (2011/02/26)
Cdc7 kinase plays a critical role in the regulation of DNA replication in eukaryotic cells and has been proposed as a target for cancer therapy. We have identified a class of Cdc7/Dbf4 inhibitors with a pyrido-thieno-pyrimidine core structure. Synthesis o
Synthesis of some new pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4(3H)-ones and pyrido[3′,2′: 4,5]thieno[2,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives
Ho, Yuh-Wen
, p. 1163 - 1174 (2007/10/03)
2,3-Disubstituted-pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4( 3H) -ones 8a-8c, 9a-9c were obtained by treatment of pyrido[3′,2′:4,5]thieno[3,2-d][1,3]oxazin-4(3H)-one derivative 3, 3-diacetylamino-thieno[2,3-b]pyridine derivative 5 and 3-ethoxymethyleneaminothieno[2,3-b]pyridine derivative 7a with appropriate amines, respectively. Condensation of compounds 8b, 9b with appropriate α-chlorocarbonyl compounds gave the corresponding 3-substituted carbonylmethylene-pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4(3H)-one derivatives 13a-d. 3-N-Substituted-pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4(3H)-ones 15a,b, 16a,b and 18a,b were also obtained by cyclization of carbohydrazide 14 with different reagents under a variety of conditions. On the other hand, cyclization of 3-amino-4-imino-pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4(3H)-ones 21a,b with appropriate orthoesters afforded the corresponding 3,5-dialkyl-pyrido[3′,2′:4,5]thieno[2,3-e]-1,2,4-triazolo[1,5-c] pyrimidines 22a-f.
