3H-Pyrazolo[4,3-f]quinoline-Based Kinase Inhibitors Inhibit the Proliferation of Acute Myeloid Leukemia Cells In Vivo was written by Dayal, Neetu;Reznickova, Eva;Hernandez, Delmis E.;Perina, Miroslav;Torregrosa-Allen, Sandra;Elzey, Bennett D.;Skerlova, Jana;Ajani, Haresh;Djukic, Stefan;Vojackova, Veronika;Lepsik, Martin;Rezacova, Pavlina;Krystof, Vladimir;Jorda, Radek;Sintim, Herman O.. And the article was included in Journal of Medicinal Chemistry in 2021.Application In Synthesis of Benzo[d]isothiazol-5-amine This article mentions the following:
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. In the experiment, the researchers used many compounds, for example, Benzo[d]isothiazol-5-amine (cas: 53473-85-1Application In Synthesis of Benzo[d]isothiazol-5-amine).
Benzo[d]isothiazol-5-amine (cas: 53473-85-1) belongs to isothiazole derivatives. The chemistry of isothiazoles is being intensively developed, which is evidenced by the wide range of selective transformations involving the isothiazole heterocycle and the high biological activity of its derivatives that can be used as effective new drugs and plant protection chemicals. Various penicillins and cephalosporins having an isothiazole ring system have shown considerable antibacterial efficacy against Gram-positive and Gram-negative bacteria.Application In Synthesis of Benzo[d]isothiazol-5-amine
Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com