1189746-27-7Relevant academic research and scientific papers
Discovery of N-(4-(3-isopropyl-2-methyl-2 H-indazol-5-yl)pyrimidin-2-yl)-4-(4-methylpiperazin-1-yl)quinazolin-7-amine as a Novel, Potent, and Oral Cyclin-Dependent Kinase Inhibitor against Haematological Malignancies
Huang, Jianhang,Wang, Xinren,Dong, Ruinan,Liu, Xiaoyue,Li, Hongmei,Zhang, Tianyi,Xu, Junyu,Liu, Chenhe,Zhang, Yanmin,Hou, Shaohua,Tang, Weifang,Lu, Tao,Chen, Yadong
, p. 12548 - 12571 (2021/09/11)
Hematologic malignancies (HM) start in blood forming tissue or in the cells of the immune system. Cyclin-dependent kinases (CDKs) regulate cell cycle progression, and some of them control cellular transcription. CDK inhibition can trigger apoptosis and could be particularly useful in hematological malignancies. Herein, we describe our efforts toward the discovery of a novel series of quinazoline derivatives as CDK inhibitors. Intensive structural modifications lead to the identification of compound 37d as the most active inhibitors of CDKs 1, 2, 4, 8 and 9 with balancing potency and selectivity against CDKs. Further biological studies revealed that compound 37d can arrest the cell cycle and induce apoptosis via activating PARP and caspase 3. More importantly, compound 37d showed good antitumor efficacy in multiple HM mice xenograft models with no obvious toxicity. These results indicated that CDK 1, 2, 4, 8, and 9 inhibitors could be potentially used to treat certain hematologic malignancies.
HETEROBICYCLIC COMPOUNDS FOR INHIBITING THE ACTIVITY OF SHP2
-
Paragraph 0577-0579; 0580; 0581, (2020/02/16)
A compound of formula (I):wherein Ring A, Q, R1,R2, R3, R4, R5, R6, R7, R8, R9, R10, R11,X, a,b, c and d are as defined in the specification.
SUBSTITUTED QUINOXALINE DERIVATIVES
-
Page/Page column 244; 345, (2016/12/01)
The present invention relates to substituted quinoxaline derivatives. These compounds are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.
Heterocyclic compound with Wnt signal path inhibitory activity and application thereof
-
, (2016/10/08)
The invention provides a heterocyclic compound with Wnt signal path inhibitory activity. The heterocyclic compound and chemically acceptable salt, isotope, isomer and a crystal structure thereof are provided with a structure shown as the general formula I (see the formula in the description). The invention further provides application of the heterocyclic compound with the Wnt signal path inhibitory activity. The heterocyclic compound with the Wnt signal path inhibitory activity serves as effective antagonist of a Wnt signal path, and can be used for treating or preventing diseases caused by abnormity of the Wnt signal path.
3-INDAZOLYL-4-PYRIDYLISOTHIAZOLES
-
Page/Page column 6, (2009/10/18)
The present invention provides 3-indazoyl-4-pyridylisothiazoles or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and methods of using the same, as well as processes for preparing the same, and intermediates thereof.
