444731-72-0Relevant articles and documents
Preparation method of pazopanib intermediate
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, (2021/03/24)
The invention provides a preparation method of a pazopanib key intermediate 2,3-dimethyl-N-(2-chloropyrimidin-4-yl)-N-methyl-2H-indazole-6-amine. The method comprises the following steps: by taking 6-halogenated-2,3-dimethyl-2H-indazole as a raw material, conducting reacting to obtain N,2,3-trimethyl-2H-indazole-6-amine; and further carrying out a reaction to obtain the 2,3-dimethyl-N-(2-chloropyrimidin-4-yl)-N-methyl-2H-indazole-6-amine. The method has the advantages of short synthesis route, accessible raw materials, low cost, mild reaction conditions, high safety and high yield, and is suitable for industrial mass production.
Design, synthesis and bioevaluation of novel 6-substituted aminoindazole derivatives as anticancer agents
Anh, Le Viet,Hai, Dinh Thi Thanh,Han, Byung Woo,Hien, Tran Thi Thu,Hoang, Ngo Xuan,Hoang, Van-Hai,Long, Nguyen Huu,Luu, Hung N.,Luu, Thi-Thu-Trang,Ngo, Son Tung,Ngo, Thien,Nguyen, Thanh Xuan,Nguyen, Yen Thi Kim,Tran, Phuong-Thao,Van Hieu, Duong
, p. 45199 - 45206 (2020/12/30)
In the present study, a series of 6-substituted aminoindazole derivatives were designed, synthesized, and evaluated for bio-activities. The compounds were initially designed as indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors based on the structural feature of five IDO1 inhibitors, which are currently on clinical trials, and the important anticancer activity of the indazole scaffold. One of them, compound N-(4-fluorobenzyl)-1,3-dimethyl-1H-indazol-6-amine (36), exhibited a potent anti-proliferative activity with an IC50 value of 0.4 ± 0.3 μM in human colorectal cancer cells (HCT116). This compound also remarkably suppressed the IDO1 protein expression. In the cell-cycle studies, the suppressive activity of compound 36 in HCT116 cells was related to the G2/M cell cycle arrest. Altogether, the current findings demonstrate that compound 36 would be promising for further development as a potential anticancer agent.
2,3-dimethyl-6-urea -2H-indazoles and its preparation method and application
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, (2016/10/09)
The invention discloses a 2, 3-dimethyl-6-urea-2H-indazole compound shown by the following general formula (I), medicinal salt or a solvent compound thereof, wherein Ar is substituted or unsubstituted phenyl or aromatic matrix. The invention also discloses a preparation method and application of the compound. The compound can regulate signal transduction of tyrosine kinase, inhibit bad cellular proliferation, and particularly has obvious curative effect for tumors.