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
- 13Citations
- 14Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
Citation Benchmarking is provided by Scopus and SciVal and is different from the metrics context provided by PlumX Metrics.
Metrics Details
- Citations13
- Citation Indexes13
- 13
- CrossRef6
- Captures14
- Readers14
- 14
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.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0223523421002361; http://dx.doi.org/10.1016/j.ejmech.2021.113387; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85103341419&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/33774342; https://linkinghub.elsevier.com/retrieve/pii/S0223523421002361; https://dx.doi.org/10.1016/j.ejmech.2021.113387
Elsevier BV
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