Fu, Shibo published the artcileγ-H2AX kinetics as a novel approach to high content screening for small molecule radiosensitizers, Synthetic Route of 2215-33-0, the publication is PLoS One (2012), 7(6), e38465, database is CAplus and MEDLINE.
Background: Persistence of γ-H2AX after ionizing radiation (IR) or drug therapy is a robust reporter of unrepaired DNA double strand breaks in treated cells. Methods: DU-145 prostate cancer cells were treated with a chem. library ±IR and assayed for persistence of γ-H2AX using an automated 96-well immunocytochem. assay at 4 h after treatment. Hits that resulted in persistence of γ-H2AX foci were tested for effects on cell survival. The mol. targets of hits were validated by mol., genetic and biochem. assays and in vivo activity was tested in a validated Drosophila cancer model. Results: We identified 2 compounds, MS0019266 and MS0017509, which markedly increased persistence of γ-H2AX, apoptosis and radiosensitization in DU-145 cells. Chem. evaluation demonstrated that both compounds exhibited structurally similar and biochem. assays confirmed that these compounds inhibit ribonucleotide reductase. DNA microarray anal. and immunoblotting demonstrates that MS0019266 significantly decreased polo-like kinase 1 gene and protein expression. MS0019266 demonstrated in vivo antitumor activity without significant whole organism toxicity. Conclusions: MS0019266 and MS0017509 are promising compounds that may be candidates for further development as radiosensitizing compounds as inhibitors of ribonucleotide reductase.
PLoS One published new progress about 2215-33-0. 2215-33-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, and the molecular formula is C11H10N4, Synthetic Route of 2215-33-0.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem