A chalcone derivative binds a putative allosteric site of YopH: Inhibition of a virulence factor of Yersinia

Souza, Ana Caroline Arruda de; Mori, Mattia; Sens, Larissa; Rocha, Ruth F; Tizziani, Tiago; Souza, Luiz Felipe Schmitz de; Chiaradia-Delatorre, Louise Domeneghini; Botta, Maurizio; Nunes, Ricardo José; Terenzi, Hernán; Menegatti, Angela Camila Orbem

doi:10.1016/j.bmcl.2020.127350

Cited by 5 publications

(2 citation statements)

References 37 publications

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“…All compounds were identified with melting point determination, 1 H, and 13 C Nuclear Magnetic Resonance (NMR) spectroscopy, and High-Resolution Mass Spectra (HRMS), according to our previous studies and supporting data [34].…”

Section: Synthesis and Characterization Of Chalconesmentioning

confidence: 99%

Q1VA, a Synthetic Chalcone, Induces Apoptosis and Decreases Invasion on Primary Culture of Human Glioblastoma

et al. 2023

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Glioblastoma (GBM) is the most commonly occurring type of primary tumor of the central nervous system (CNS) and is considered the worst type of glioma. Despite the current standard treatment for newly diagnosed GBM, which involves surgery followed by chemotherapy with temozolomide (TMZ) and radiation therapy, the average survival time for patients with GBM is only about 15 months. This is due to GBM’s tendency to recur, its high proliferative rates, its ability to evade apoptosis, and its ability to invade healthy tissue. Therefore, it is crucial to explore new treatment options for GBM. This study investigated the potential anticancer activities of a new series of synthetic chalcones, which are natural compounds found in the biosynthesis of flavonoids in plants. Primary cell culture of glioblastoma (GBM1) from surgical resection was used to evaluate the effects of synthetic chalcones on viability, cell death, reactive oxygen species (ROS), mitochondrial membrane potential (ΔΨm), cell cycle, and invasion. One chalcone, Q1VA (at concentrations of 10, 50, and 100 μM for 24 h) induced cytotoxicity by increasing apoptosis levels and depolarizing the mitochondrial membrane, as evidenced by a TMRE assay. Further analysis using the molecular fluorescent probe H2DCFDA indicated that the increased levels of reactive oxygen species (ROS) might be linked to altered mitochondrial membrane potential and cell death. Furthermore, viable cells were observed to be delayed in the cell cycle, primarily in the M phase, and the invasion process was reduced. The findings of this study indicate that Q1VA is a potential adjuvant therapeutic agent for GBM due to its significant antitumor effects. If its safety and efficacy can be confirmed in animal models, Q1VA may be considered for clinical trials in humans. However, additional research is required to determine the optimal dosage, treatment schedule, and potential side effects of Q1VA.

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Section: Synthesis and Characterization Of Chalconesmentioning

confidence: 99%

Q1VA, a Synthetic Chalcone, Induces Apoptosis and Decreases Invasion on Primary Culture of Human Glioblastoma

et al. 2023

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“…所有目标产物经 1 H NMR、 13 C NMR 和 HRMS 谱图确证, 以化合物 6b (图 2)为例, 其确证结果如下: δ 8.01 为苯环上 C6'、C2'位对称氢的吸收峰, δ 7.76 为苯环上盐酸溶液调节 pH 至 6～7, 固体析出, 抽滤, 用冷乙醇多次冲洗纯化, 旋干得到产物 3a～3j. 其合成按照文献报道的方法进行, 表征数据与文献一致 [29][30][31][32] , 其收率及熔点如表 3 所示.…”

Section: 谱图解析unclassified

Synthesis and Evaluationin vitroof Dihydrothiophenopyridine-Chalcone Derivatives as Anticancer Activity Agents

Liu¹,

Xu²,

Wang³

et al. 2021

Chinese Journal of Organic Chemistry

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摘要以 2-噻吩乙胺与自制的查尔酮酸进行酰化反应得到酰胺类中间体 5a～5j, 经 Bischer-Napieralski 环合反应合成了 10 个未见报道的二氢噻吩并吡啶-查尔酮衍生物 6a～6j, 再经去氢反应获得 2 个噻吩并吡啶-查尔酮衍生物 7a 和 7b. 通过噻唑蓝(MTT)法对 11 种细胞进行体外抗癌活性及安全性测试. 结果表明, 化合物 6a (p-F)、6d (o-Br)和 6h (m-OCH3) 对 HeLa、SGC-7901 细胞的抗癌活性优于紫杉醇. 当短时间处理(＜4 h)时, 6j (3,4,5-OCH3)在不影响正常细胞 MCF-10A 的情况下对癌细胞 MCF-7 显示强效抗癌效果, 值得进一步研究和开发.

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Carboxylated chalcones and related flavonoids as inhibitors of xanthine oxidase

et al. 2023

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A chalcone derivative binds a putative allosteric site of YopH: Inhibition of a virulence factor of Yersinia

Cited by 5 publications

References 37 publications

Q1VA, a Synthetic Chalcone, Induces Apoptosis and Decreases Invasion on Primary Culture of Human Glioblastoma

Q1VA, a Synthetic Chalcone, Induces Apoptosis and Decreases Invasion on Primary Culture of Human Glioblastoma

Synthesis and Evaluationin vitroof Dihydrothiophenopyridine-Chalcone Derivatives as Anticancer Activity Agents

Carboxylated chalcones and related flavonoids as inhibitors of xanthine oxidase

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