22214-28-4Relevant articles and documents
New pentadienone oxime ester derivatives: synthesis and anti-inflammatory activity
Li, Qin,Zhang, Juping,Xue, Wei,Chen, Liu Zeng,Wang, Jie Quan,Tang, Wen Jian,Liu, Xin Hua,Zhou, Hai Ping
, p. 130 - 138 (2018)
To develop novel anti-inflammatory agents, a series of new pentadienone oxime ester compounds were designed and synthesized. The structures were determined by IR, 1H NMR, 13C NMR, and HRMS. All compounds have been screened for their anti-inflammatory activity by evaluating their inhibition against LPS-induced nitric oxide (NO) release in RAW 264.7 cell. Among them, compound 5j was found to be one of the most potent compounds in inhibiting NO and IL-6 (IC50 values were 6.66 μM and 5.07 μM, respectively). Preliminary mechanism studies show that title compound 5j could significantly suppress expressions of nitric oxide synthase, COX-2, and NO, IL-6 through Toll-like receptor 4/mitogen-activated protein kinases/NF-κB signalling pathway. These data support further studies to assess rational design of more efficient pentadienone oxime ester derivatives with anti-inflammatory activity in the future.
Novel penta-1,4-diene-3-one derivatives containing quinazoline and oxime ether fragments: Design, synthesis and bioactivity
Su, Shijun,Chen, Mei,Li, Qin,Wang, Yihui,Chen, Shuai,Sun, Nan,Xie, Chengwei,Huai, Ziyou,Huang, Yinjiu,Xue, Wei
, (2021)
A series of novel penta-1,4-diene-3-one derivatives containing quinazoline and oxime ether moieties were designed and synthesized. Their anticancer activities were evaluated by MTT assay, the results showed that most compounds exhibited extremely inhibitory effects against hepatoma SMMC-7721 cells. In particular, compounds Q2 and Q8 displayed the more potent inhibitory activity with IC50 values of 0.64 and 0.63 μM, which were better than that of gemcitabine (1.40 μM). Further mechanism studies indicated that compounds Q2, Q8, Q13 and Q19 could control the migration of SMMC-7721 cells effectively, and inhibit the proliferation of cancer cells by inhibiting the DNA replication. Western-blot results showed that compounds Q2 and Q8 induced irreversible apoptosis of SMMC-7721 cells by regulating the expression level of apoptose-related proteins. Those studies demonstrated that the penta-1,4-diene-3-one derivatives containing quinazoline and oxime ether fragments merited further research as potential anticancer agents.
Dopamine D2 receptor selective agonist and application thereof
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Paragraph 0203-0204, (2020/12/29)
The invention relates to a dopamine D2 receptor selective agonist and application thereof. Specifically, the invention discloses an agonist with selectivity to DRD2 and discloses a potential application value of the agonist in disease treatment. The invention discloses an agonist with DRD2 selectivity for the first time, and the specific targeting DRD2 of the agonist can play a role in treating low dopamine related diseases such as Parkinson's disease, attention deficit hyperactivity disorder, pituitary adenoma, hyperprolactinemia, hyperactivity leg syndrome, negative schizophrenia and the like while side effects are reduced to the maximum extent.
Quinoxaline-containing pentadiene ketone oxime ester compound and production method and application thereof
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Paragraph 0071; 0072, (2019/10/01)
The invention relates to a quinoxaline-containing pentadiene ketone oxime ester compound and a production method and application thereof. The compound is as shown in a formula A, wherein X is selectedfrom O, R1 is one of phenyl, substituted phenyl and substituted heterocyclyl, R2 is one of phenyl, substituted phenyl, substituted heterocyclyl and substituted benzyl, and R3 is a hydrogen atom or achlorine atom or the like. The compound has a good control effect on tobacco mosaic viruses.
