598-52-7Relevant articles and documents
Liquid chromatographic determination of noxytiolin and 1-methyl-2-thiourea in serum: Application to pharmacokinetic studies in rabbits and humans
Debruyne,Moulin,Bricard,Bigot
, p. 224 - 226 (1985)
A high-performance liquid chromatographic method is described which determines noxytiolin and 1-methyl-2-thiourea concentrations in serum. Valid determination requires immediate ultracentrifugation of blood samples, rapid serum freezing, and injection into the chromatograph within 6 h. A number of pharmacokinetic parameters were calculated from serum concentration data in rabbits and humans. An unknown metabolite was detected in both species but its structure was not identified.
Pyrimidone compound and application thereof
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Paragraph 0888-0891, (2019/07/08)
The invention discloses a pyrimidone compound, pharmaceutically acceptable salt and solvate thereof, and provides a method for preparing the compounds, a composition containing the compounds and medicinal application of the compounds in preparation of medicines for treating diseases or disorders related to EED protein and/or PRC2 protein complex action mechanisms.
Design, synthesis and biological evaluation of novel HSP70 inhibitors: N, N′-disubstituted thiourea derivatives
Zeng, Yan-Qun,Cao, Rui-Yuan,Yang, Jian-Ling,Li, Xing-Zhou,Li, Song,Zhong, Wu
, p. 83 - 95 (2016/05/24)
As novel heat shock protein 70 (HSP70) inhibitors, N, N′-disubstituted thiourea derivatives were designed and synthesized based on the X-ray structure of the ATPase domain (nucleotide binding domain, NBD). An ATPase activity inhibition assay revealed that these compounds effectively inhibited HSP70 ATPase activity. The results revealed that the compounds 370/371/374/379/380//392/394/397/404/405 and 407 can inhibit the HSP70 ATPase turnover with high percentages of inhibition: 50.42, 38.46, 50.45, 44.12, 47.13, 50.50, 40.95, 65.36, 46.23, 35.78, and 58.37 in 200 μM, respectively. Significant synergies with lapatinib were observed for compound 379 and compound 405 in the BT474 breast cancer cell line. A structure-function analysis revealed that most of the thiourea derivatives exhibited cooperative action with lapatinib in the BT474 cancer cell line and the BT/LapR1.0 lapatinib-resistant cell line. HSP70 inhibitors may be developed as synergetic drugs in drug-resistant cancer therapy.