期刊
NATURAL PRODUCT COMMUNICATIONS
卷 17, 期 6, 页码 -出版社
SAGE PUBLICATIONS INC
DOI: 10.1177/1934578X221105692
关键词
antiinflammation; anticancer; 1; 4-dihydropyrazolo[4; 3-b]indoles; cytokine; antiproliferation
资金
- Graduate University of Science and Technology [GUST.STS.DT2019-HH01]
The research focuses on multitargeting drugs and the discovery of agents that can act on multiple biological targets. In this study, a novel synthetic route to fused-heterocycles, 1,4-dihydropyrazolo[4,3-b]indoles, was reported. Two lead compounds, 3b and 4b, showed significant inhibition of cell growth, induced apoptosis in leukemia cells, and decreased levels of tumor necrosis factor-alpha and transforming growth factor-beta. These compounds have potential as novel anticancer agents.
Research on multitargeting drugs is emerging, focusing on the discovery of agents that simultaneously act on more than one biological target. Here, a novel synthetic route to access the fused-heterocycles 1,4-dihydropyrazolo[4,3-b]indoles (4) from pyrazolo[4,3-c][2,1]benzothiazine 4,4-dioxide (3) via [H2O-SO2] elimination and an intramolecular ring-closing reaction is reported. Two lead compounds 3b and 4b were found to show significant inhibition of cell growth by suppressing cell cycle progression at the G(0)/G(1) phases and inducing apoptosis of the acute myeloid leukemia OCI-AML3 cell line. Both compounds also significantly decreased tumor necrosis factor-alpha and transforming growth factor-beta (at all tested concentrations), whereas no effect was seen on other cytokines (interleukin-4, interferon-gamma, interleukin-9, interleukin-12). Thus, these compounds are promising leads in the discovery of novel anticancer agents.
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