557770-90-8Relevant articles and documents
As Aurora kinase inhibitors of the substituted quinazoline derivatives
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, (2019/04/04)
The invention relates to a substituted quinazoline derivative as an aurora kinase inhibitor, which is shown as structural formula (I) or (Ia), tautomers, hydrates, solvates or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the tautomers, hydrates, solvates and pharmaceutically acceptable salts as drug active ingredients, and application of the compounds and the pharmaceutical compositions in preparation of medicines for protection, treatment, curing or alleviation of proliferative diseases of patients.
Discovery of 4-aminoquinazoline - Urea derivatives as Aurora kinase inhibitors with antiproliferative activity
Cai, Jin,Li, Lili,Hong, Kwon Ho,Wu, Xiaoqing,Chen, Junqing,Wang, Peng,Cao, Meng,Zong, Xi,Ji, Min
, p. 5813 - 5823 (2014/12/11)
Two series of 20 novel 4-aminoquinazoline - urea derivatives have been designed and synthesized. The entire target compounds were investigated for their in vitro antiproliferative activity against six human cancer cell lines (K562, U937, A549, NCI-H661, HT29 and LoVo) using the MTT-based assay. Most compounds showed significant antiproliferative activities against four solid tumor cell lines, but no or poor activities against two leukemia cell lines. Furthermore, the target compounds were screened for Aurora A/B kinases inhibitory activity. Among them, 7c, 7d, 8c, and 8d are more potent against Aurora A kinase than ZM447439. Docking study of compounds 7d and ZM447439 revealed that they bound strongly to the ATP-binding sites of Aurora A and B. Thus, they may be promising lead compounds for the development of novel anti-tumor drug potentially via inhibiting Aurora kinases.
Switching the Chemoselectivity in the Amination of 4-Chloroquinazolines with Aminopyrazoles
Shen, Zhenlu,Hong, Yiming,He, Xiaofei,Mo, Weimin,Hu, Baoxiang,Sun, Nan,Hu, Xinquan
supporting information; experimental part, p. 552 - 555 (2010/05/18)
[Chemical equation presented] The chemoselectivity in the amination of 4-chloroquinazolines with 3-amino-1H-pyrazoles was studied. Under the conditions of Pd2(dba)3/ Xantphos/Na2CO3, 4-chloroquinazolines underwent selective amination with the cyclic secondary amino group of 3-amino-1H-pyrazoles. whereas 4-chloroquinazolines were exclusively aminated with the primary amino group of 3-amino-1H-pyrazoles via SNAr substitution In the presence of HCl.