72785-29-6Relevant articles and documents
4,5-Diaryl-3H-1,2-dithiole-3-thiones and related compounds as combretastatin A-4/oltipraz hybrids: Synthesis, molecular modelling and evaluation as antiproliferative agents and inhibitors of tubulin
Wang, Zhiwei,Qi, Huan,Shen, Qirong,Lu, Guodong,Li, Mingyang,Bao, Kai,Wu, Yingliang,Zhang, Weige
, p. 520 - 529 (2016)
A new series of 4,5-diaryl-3H-1,2-dithiole-3-thiones and related compounds were designed and synthesised as combretastatin A-4/oltipraz hybrids. We evaluated the antiproliferative activities, inhibition of tubulin polymerization, and cell-cycle effects of
Small molecules that protect against β-amyloid-induced cytotoxicity by inhibiting aggregation of β-amyloid
Lee, Yun Suk,Kim, Hye Yun,Kim, Youngsoo,Seo, Jae Hong,Roh, Eun Joo,Han, Hogyu,Shin, Kye Jung
experimental part, p. 4921 - 4935 (2012/10/08)
Aggregated β-amyloid (Aβ) plays crucial roles in Alzheimer's disease (AD) pathogenesis, therefore blockade of Aβ aggregation is considered as a potential therapeutic target. We designed and synthesized small molecules to reduce Aβ-induced cytotoxicity by inhibiting Aβ aggregation. The small molecules were screened via ThT, MTT, and cell-based cytotoxicity assay (Aβ burden assay). Selected compounds 1c, 1d, 1e, and 1f were then investigated by evaluating their effects on cognitive impairment of acute AD mice model. Learning and memory dysfunction by injection of Aβ(1-42) was recovered by administration of these molecules. Especially, 1d showed the best recovery activity in Y-maze task, object recognition task, and passive avoidance task with dose dependent manner. These results suggest that 1d has high potential as a therapeutic agent for AD.
Synthesis of 5-substituted benzyl-2,4-diamino pyrimidine derivatives as c-Fms kinase inhibitors
Xu, Li Bao,Sun, Wei,Liu, Hong Ying,Wang, Li Li,Xiao, Jun Hai,Yang, Xiao Hong,Li, Song
scheme or table, p. 1318 - 1321 (2011/10/09)
A serials of novel 5-substituted benzyl-2,4-diamino pyrimidine derivatives have been synthesized and evaluated as inhibitors of c-Fms kinase by the standard MTT method. The results showed that compound 15,5-[3-methoxy-4-(pyridine-3-yl)benzyl]-2,4-diamino pyrimidine, had an IC50 of 1.45μmol/L in inhibiting the proliferation of M-CSF-dependent myeloid leukemia cells in mice (NFS-60), which was similar with GW2580, a selective inhibitor of c-Fms kinase.