Effect of new olivacine derivatives on p53 protein level

• DOI: 10.1007/s43440-019-00004-1
• Publication Date: 2020-01-08T14:02:50Z
• Authors: Tomasz Gębarowski; Benita Wiatrak; Katarzyna Gębczak; Beata Tylińska; Kazimierz Gąsioro...
• Keywords: Pharmacotherapy

The p53 protein is a transcription factor for many genes, including genes involved in inhibiting cell proliferation and inducing apoptosis genotoxically damaged tumor-transformed cells. In more than 55% of cases human cancers, loss the essential function found. numerous reports, it has been shown that small molecules (chemical compounds) can restore suppressor mutant tumor aim this study was to evaluate potential anticancer activity three newly synthesized olivacine derivatives.The performed using two lines-CCRF/CEM (containing protein) A549 non-mutant, wild-type protein). cells were incubated with derivatives 18 h then assays carried out: measurement amount p21 proteins, detection apoptosis, cycle analysis, rhodamine 123 accumulation assay (evaluation P-glycoprotein inhibition). Multiple-criteria decision analysis used compare tested compounds.Each compound caused reconstitution protein. addition, one compounds showed significant antitumor both For all compounds, stronger effect on level observed reference compound-ellipticine.The effects new (pyridocarbazoles) suggest they are good candidates drugs.