76510-61-7Relevant academic research and scientific papers
Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR
Zhang, Qiumeng,Shen, Qianqian,Gao, Lixin,Tong, Linjiang,Li, Jia,Chen, Yi,Lu, Wei
, p. 428 - 441 (2018/09/22)
Aurora A, Aurora B and Kinase Insert Domain-containing Receptor (KDR) play essential roles in sustained cancer growth. In the present study, eighteen pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives were designed and synthesized. Most of the prepa
A class of pyrazolopyrimidine diazepine derivatives with antitumor effect
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Paragraph 0051; 0067-0070, (2019/01/08)
The present invention relates to the field of medicine, wherein a pyrazolopyrimidine diazepine derivative represented by a formula I can significantly inhibit three targets such as Aurora A, Aurora Band vascular endothelial growth factor receptor 2 (VEGFR2/KDR), or two or one of the three targets, and the pharmacological experiment results show that the pyrazolopyrimidine diazepine derivative hassignificant antitumor activity, can be used to be developed into antitumor drugs for treatment or control of malignant tumors, especially drugs for treatment or control of gastric cancer, liver cancer, lung cancer, breast cancer, colon cancer and the like. The formula I is defined in the specification.
A New Synthesis of 2-Aminoindoles and 6-Aminopyrrolo[3,2- d ]pyrimidines from π-Deficient 1,2-Dihaloarenes and Geminal Enediamines
Mishina, Maria S.,Ivanov, Alexander Yu.,Lobanov, Pavel S.,Dar'In, Dmitrii V.
supporting information, p. 2851 - 2862 (2016/08/30)
An efficient approach for the synthesis of fused 2-aminopyrroles via geminal enediamines and π-deficient 1,2-dihaloarenes is presented. The two-step methodology includes aromatic nucleophilic substitution of the activated halogen of dihaloarene with enediamine C-nucleophilic center followed by Cu-catalyzed intramolecular N-arylation. This approach allows access to a variety of 2-amino-6-nitroindoles and 6-aminopyrrolo[3,2-d]pyrimidines (including N-mono- and N,N-disubstituted) in moderate and good yields under mild conditions.
INHIBITORS OF IRAK4 ACTIVITY
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Page/Page column 41; 42, (2014/05/07)
The present invention relates to compounds which modulate interleukin-l (IL-1 ) receptor-associated kinase 4 (IRAK4) and are useful in the prevention or treatment of inflammatory, cell proliferative and immune-related conditions and diseases. Specifically, provided herein are inhibitors of IRAK4 of Formula I and pharmaceutical compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
Microwave-assisted C-5 iodination of substituted pyrimidinones and pyrimidine nucleosides
Paolini, Lisa,Petricci, Elena,Corelli, Federico,Botta, Maurizio
, p. 1039 - 1042 (2007/10/03)
Direct microwave-assisted iodination of several pyrimidinones and pyrimidine nucleosides with N-iodosuccinimide to give the corresponding 5-iodo derivatives is described. Application of this reaction to polymer-bound pyrimidinones was also investigated.
CONDENSED HETEROAROMATIC RING SYSTEMS. VII. SYNTHESIS OF THIENOPYRIDINES, THIENOPYRIMIDINES, AND FUROPYRIDINES FROM o-SUBSTITUTED N-HETEROARYLACETYLENES
Sakamoto, Takao,Kondo, Yoshinori,Watanabe, Ryo,Yamanaka, Hiroshi
, p. 2719 - 2724 (2007/10/02)
The cross-coupling reaction of 2-chloro-3-iodo- and 4-chloro-3iodopyridines with phenylacetylene in the presence of dichlorobis(triphenylphosphine)palladium occured at the 3-position.The 3-ethynylpyridines containing an adjacent chloro group were converti
