123580-67-6Relevant academic research and scientific papers
Piperazine-containing myricetin derivative and preparation method thereof (by machine translation)
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, (2019/08/07)
The invention discloses a piperazine-amide-containing myricetin derivative, and is characterized in that the general formula is as shown in the specification: Wherein, R1 More than one hydrogen atom, methoxy, nitro, methyl, trifluoromethyl or halogen atom is contained in the ortho, meta or para position on the phenyl ring. The compound has certain inhibitory activity on hepGG2 cells and SGCCCC7901 cells, is small in toxicity to normal cells, and can be used for preparing anti-tumor drugs. (by machine translation)
Exploration of (S)-3-aminopyrrolidine as a potentially interesting scaffold for discovery of novel Abl and PI3K dual inhibitors
Zhang, Cunlong,Tan, Chunyan,Zu, Xuyu,Zhai, Xin,Liu, Feng,Chu, Bizhu,Ma, Xiaohua,Chen, Yuzong,Gong, Ping,Jiang, Yuyang
, p. 1404 - 1414 (2011/04/22)
Based on the literature-reported compensatory effect of PI3K on Abl inhibition and the improved preclinical effect of drug combination of Abl and PI3K inhibitors, a series of compounds bearing novel scaffold of (S)-3-aminopyrrolidine was identified as Abl and PI3K dual inhibitors through support vector machine screening tool, which were subsequently synthesized and tested. Most compounds demonstrated promising cytoxicity against a CML leukemia cell-line K562 and moderate inhibition against Abl and PI3K kinases. These compounds induced no apoptosis in K562 cell-line, suggesting that their cytotoxic activities are unlikely duo to other known anti-CML mechanisms. Molecular docking study further showed that the compound 5k could bind with both Abl and PI3K, but the weaker binding with Abl compared to Imatinib is consistent with its low kinase inhibitory rates. These plus literature-reported evidences suggest that the promising cytotoxic effect of our novel compounds might be due to the collective effect of Abl and PI3K inhibition.
