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Design, synthesis and bioevaluation of novel 6-substituted aminoindazole derivatives as anticancer agents. 2020
Ngo Xuan Hoang, and
Van-Hai Hoang, and
Thi-Thu-Trang Luu, and
Hung N Luu, and
Thien Ngo, and
Duong Van Hieu, and
Nguyen Huu Long, and
Le Viet Anh, and
Son Tung Ngo, and
Yen Thi Kim Nguyen, and
Byung Woo Han, and
Thanh Xuan Nguyen, and
Dinh Thi Thanh Hai, and
Tran Thi Thu Hien, and
Phuong-Thao Tran
Hanoi University of Pharmacy 13-15 Le Thanh Tong Hanoi 100000 Vietnam thaotp119@gmail.com.
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.
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