6839-90-3Relevant articles and documents
CHEMICAL ACTIVATORS OF NICOTINAMIDE MONONUCLEOTIDE ADENLYLY TRANSFERASE 2 (NMNAT2) AND USES THEREOF
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Page/Page column 22-23; 28, (2020/06/22)
The present application relates to novel semicarbazones and thiosemicarbazones, to processes for preparing them, to pharmaceutical preparations comprising them, to the use of the novel semicarbazones and thiosemicarbazones for treatment and/or prophylaxis of diseases and to the use thereof for production of a medicament for treatment and/or prophylaxis of diseases, especially of neurodegeneration and age-associated diseases or conditions associated with NAD loss. The present application also provides a method for high throughput screening of NMNAT2 activators.
Rapid induction of apoptosis in tumor cells treated with a new platinum(II) complex based on amino-thiazolidinone
Song, Xue-Qing,Liu, Ya-Hong,Shao, Jia,Zhang, Zhen-Lei,Xie, Cheng-Zhi,Qiao, Xin,Bao, Wei-Guo,Xu, Jing-Yuan
, p. 188 - 197 (2018/08/10)
Thiazolidinone derivatives have been previously shown significant anti-cancer activities. Two amino-thiazolidinone complexes, [Pt(HTone)Cl] (1) and [Cu(HTone)Cl] (3) (HTone = (Z)-2-((E)-(1-(pyridin-2-yl)ethylidene)hydrazono)thiazolidin-4-one) and one ethyl-modified [Pt(ETone)Cl2] (2) (ETone = (Z)-3-ethyl-2-((E)-(1-(pyridin-2-yl)ethylidene) hydrazono)thiazolidin-4-one)], were designed and synthesized in order to explore novel metal-based antitumor agents. MTT assay indicated that 1 and 3 were markedly cytotoxic to MCF-7, HepG-2 and NCI-H460 tumor cells, superior to both cisplatin and the HTone ligand. Massive dead cells were observed as early as 6 h when treated with 1, indicating rapid action of 1 as compared to that of other compounds. More interestingly, Hoechst 33342 staining and flow cytometry analysis illustrated that only complex 1 could induce obvious cell apoptosis within 12 h, which was associated with the high-expression of Bax and cleavage of caspase-3 from 35 kDa to 17 kDa. By means of ICP-MS assay, we found complex 1 could largely accumulate in tumor cells in a short time. Additionally, complex 1 showed no cross resistance against the cisplatin-resistant cells.
2-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: Structural design, synthesis and pharmacological evaluation
Cardoso, Marcos Veríssimo De Oliveira,Siqueira, Lucianna Rabelo Pessoa De,Silva, Elany Barbosa Da,Costa, Lívia Bandeira,Hernandes, Marcelo Zaldini,Rabello, Marcelo Montenegro,Ferreira, Rafaela Salgado,Da Cruz, Luana Faria,Magalh?es Moreira, Diogo Rodrigo,Pereira, Valéria Rêgo Alves,De Castro, Maria Carolina Accioly Brelaz,Bernhardt, Paul V.,Leite, Ana Cristina Lima
, p. 48 - 59 (2014/10/15)
The present work reports on the synthesis, anti-Trypanosoma cruzi activities and docking studies of a novel series of 2-(pyridin-2-yl)-1,3- thiazoles derived from 2-pyridine thiosemicarbazone. The majority of these compounds are potent cruzain inhibitors