The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 3-Iodo-1H-indazol-5-amine, is researched, Molecular C7H6IN3, CAS is 599183-36-5, about 3H-Pyrazolo[4,3-f]quinoline-Based Kinase Inhibitors Inhibit the Proliferation of Acute Myeloid Leukemia Cells In Vivo, the main research direction is pyrazoloquinoline preparation antitumor activity tyrosine kinase inhibition mol docking.Category: piperazines.
Herein, various 3H-pyrazolo[4,3-f]quinoline-containing compounds e.g., I were rapidly assembled via the Doebner-Povarov multicomponent reaction from the readily available 5-aminoindazoles, ketones and aldehydes in good yields. The most active compounds potently inhibit the recombinant FLT3 kinase and its mutant forms with nanomolar IC50 values. Docking studies with the FLT3 kinase showed a type I binding mode, where the 3H-pyrazolo group interacts with Cys694 in the hinge region. The compounds blocked the proliferation of AML cell lines harboring oncogenic FLT3-ITD mutations with remarkable IC50 values, which were comparable to the approved FLT3 inhibitor quizartinib. The compounds also inhibited the growth of leukemia in a mouse-disseminated AML model, and hence, the novel 3H-pyrazolo[4,3-f]quinoline-containing kinase inhibitors are potential lead compounds to develop into anticancer agents, especially for kinase-driven cancers.
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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics