118630-34-5Relevant articles and documents
A Arylheterocycle chirality bcr - abl inhibitor and its preparation method and application
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Paragraph 0121; 0122, (2016/10/09)
The invention discloses aromatic heterocyclic biphenyl Bcr-Abl inhibitors as well as a preparation method and application thereof. A structural formula of the inhibitors is shown in the specification, wherein in the structural formula, Ar is aromatic heterocycle; R is a mono-substituent or a di-substituent, and the substituent is alkyl or halogen. The series of inhibitors have a certain inhibiting effect on ABL1 kinase in vitro, can inhibit tumor cell proliferation and can be used for preparing antitumor drugs, especially CML (chronic myelocytic leukemia) drugs. The preparation method of the aromatic heterocyclic biphenyl Bcr-Abl inhibitors, which is provided by the invention, has the advantages of easiness in obtainment of raw materials, mild reaction conditions, simplicity in operation of reaction processes and cheap used reagents.
Discovery of novel Bcr-Abl inhibitors with diacylated piperazine as the flexible linker
Pan, Xiaoyan,Dong, Jinyun,Shi, Yaling,Shao, Ruili,Wei, Fen,Wang, Jinfeng,Zhang, Jie
, p. 7050 - 7066 (2015/06/25)
Forty-two compounds (series 8, 9 and 10) incorporated with diacylated piperazine have been synthesized and evaluated as novel Bcr-Abl inhibitors based on 'six-atom linker'. Five of them, 8d, 8h, 8l, 10m and 10p, displayed potent Bcr-Abl inhibitory activity comparable with Imatinib. Moreover, compounds 8e, 10q, 10s, and 10u were potent Bcr-Abl inhibitors with IC50 values at the sub-micromolecular level. Most compounds exhibited moderate to high antiproliferative activity against K562 cells. In particular, compound 9e was the most promising Bcr-Abl inhibitor. Docking studies revealed that the binding modes of these compounds were similar with Imatinib. These compounds could be considered as promising lead compounds for further optimization.
5-(1-Piperazinyl)-1H-1,2,4-triazol-3-amines as antihypertensive agents
Meyer,Tomcufcik,Chan,Haug
, p. 593 - 597 (2007/10/02)
A series of 5-(1-piperazinyl)-1H-1,2,4-triazol-3-amines was synthesized and screened for antihypertensive and diuretic activity in spontaneously hypertensive rats (SHR). One compound, 5-[4-[(3-chlorophenyl)methyl]-1-piperazinyl]-1H-1,2,4-triazol-3-amine (8), was selected to define the mechanism of its antihypertensive activity. Studies in SHR suggest ganglionic blocking activity. Short-lived antihypertensive activity was observed in conscious renal hypertensive dogs.