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New bioactive 5-arylcarboximidamidopyrazolo[3,4- c ]pyridines: Synthesis, cytotoxic activity, mechanistic investigation and structure-activity relationships

European Journal of Medicinal Chemistry, ISSN: 0223-5234, Vol: 218, Page: 113387
2021
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Article Description

In this study, a series of novel substituted pyrazolo[3,4- c ]pyridin-5-ylamidines was synthesized and their cytotoxicity against three cancer cell lines (MDA-MB-231, HT-1080, PC-3), as well as a human normal cell line (AG01523) was evaluated. A number of derivatives could strongly reduce cancer cells proliferation and exhibit apoptotic induction capability, while reasonable structure-activity relationships could be extracted. Certain analogues were endowed with low toxicity against normal cells. Cell cycle analysis revealed that most of the active compounds induced a G 0 /G 1 arrest of HT-1080 cells. Moreover, the potential mechanisms of the cytotoxic activity of the promising compounds were investigated in HT-1080 cells, upon study of their effects on the phosphorylation of Akt, ERK and p38 MAPK. Most of the active derivatives inhibit phosphorylation of Akt and ERK and/or induce p38 MAPK phosphorylation, providing a potential indication on the mode of action of this class.

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