17570-98-8Relevant articles and documents
Benzothiazolyl and Benzoxazolyl Hydrazones Function as Zinc Metallochaperones to Reactivate Mutant p53
Gilleran, John A.,Yu, Xin,Blayney, Alan J.,Bencivenga, Anthony F.,Na, Bing,Augeri, David J.,Blanden, Adam R.,Kimball, S. David,Loh, Stewart N.,Roberge, Jacques Y.,Carpizo, Darren R.
, p. 2024 - 2045 (2021)
We identified a set of thiosemicarbazone (TSC) metal ion chelators that reactivate specific zinc-deficient p53 mutants using a mechanism called zinc metallochaperones (ZMCs) that restore zinc binding by shuttling zinc into cells. We defined biophysical and cellular assays necessary for structure-activity relationship studies using this mechanism. We investigated an alternative class of zinc scaffolds that differ from TSCs by substitution of the thiocarbamoyl moiety with benzothiazolyl, benzoxazolyl, and benzimidazolyl hydrazones. Members of this series bound zinc with similar affinity and functioned to reactivate mutant p53 comparable to the TSCs. Acute toxicity and efficacy assays in rodents demonstrated C1 to be significantly less toxic than the TSCs while demonstrating equivalent growth inhibition. We identified C85 as a ZMC with diminished copper binding that functions as a chemotherapy and radiation sensitizer. We conclude that the benzothiazolyl, benzoxazolyl, and benzimidazolyl hydrazones can function as ZMCs to reactivate mutant p53 in vitro and in vivo.
Two metal complex derivatives of pyridine thiazole ligand: synthesis, characterization and biological activity
Zou, Xunzhong,Shi, Pingyi,Feng, Ansheng,Mei, Meng,Li, Yu
, p. 263 - 272 (2021)
In this work, two new metal(II) complexes with ligand based on pyridine thiazolone group, [Zn(L)2(TsO)2]2DMF (1), {[Cd(L)(NO3)2H2O)]DMF}n(2) (where L = 4-(pyridin-4-yl)-2-(2-(pyridin-2- ylm
SUBSTITUTED PYRAZOLO[4,3-b]PYRIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
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Page/Page column 60, (2020/12/30)
Substituted pyrazolo[4,3-b]pyridines as GluN2B receptor ligands. Such compounds may be used in GluN2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by GluN2B rece
