25710-23-0Relevant articles and documents
Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors
Sun, Yan,Fu, Rong,Lin, Songwen,Zhang, Jingbo,Ji, Ming,Zhang, Yan,Wu, Deyu,Zhang, Kehui,Tian, Hua,Zhang, Mingyi,Sheng, Li,Li, Yan,Jin, Jing,Chen, Xiaoguang,Xu, Heng
, (2021)
As abnormal PI3K signaling is a feature of many types of cancer, the development of orally active PI3K inhibitors is of great significance for targeted cancer therapy. Through integrating strategies of reducing aromatic character/increasing the fraction of sp3 carbons together with scaffold hopping, we designed and synthesized two new series of thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives for use as PI3K inhibitors. Our structure–activity relationship studies led to the identification of thieno[2,3-d]pyrimidine 6a and thiazolo[5,4-d]pyrimidine 7a, which exhibited remarkable nanomolar PI3K potency, good antiproliferative activity, favorable pharmacokinetic properties and significant in vivo anti-cancer efficacy. Notably, thiazolo[5,4-d]pyrimidine 7a had better anti-cancer activity than thieno[2,3-d]pyrimidine 6a and is worthy of further pre-clinical evaluation for its use in cancer treatment.
Thiazolopyrimidine compound and preparation method thereof Use and pharmaceutical compositions
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Paragraph 0073-0077; 0158-0162, (2021/11/10)
The invention belongs to the technical field of medicines, and particularly relates to a thiazolopyrimidine compound as well as a preparation method, application and a pharmaceutical composition thereof. The thiazolopyrimidine compound is I inhibitor as shown in formula (PI3K), and can be used for preparing medicaments for preventing and/or treating diseases related to PI3K activity, such as tumors, autoimmune diseases, kidney diseases, cardiovascular diseases, inflammations, metabolic dysfunction, endocrine dysfunction or nerve diseases.
