摘要:
A method for the facile synthesis of valuable 3‐selenospiro[4,5]decatrienones via CuBr2‐catalyzed three‐component reaction of N‐(4‐methoxyaryl)‐N‐methyl‐3‐phenylpropiolamide, Se powder, and boronic acids under air is disclosed. This method feature wide substrate scope, good functional group tolerance, employing earth‐abundant metal as the catalyst and green air as the oxidant, which increase its practicability. Abstract Herein, a method for the assembly of biologically valuable 3‐selenospiro[4,5]decatrienones through CuBr2‐catalyzed ispo‐cyclization of Se powder, boronic acids, and N‐(p‐methoxyaryl)propiolamides has been established. In this protocol, noble transition metal, prefunctionalized selenylation reagent, and strong chemical oxidant are not employed. This method feature wide substrate scope, good functional group tolerance, easy operation, and employing earth‐abundant metal as catalyst and green air as oxidant. Furthermore, several derivatizations of 3‐selenospiro[4,5]decatrienones are performed to showcase the practicability of our strategy.
通讯机构:
[Cai, JH ] U;[Zhao, F ] H;[Wang, DH ] S;Univ South China, Coll Chem & Chem Engn, Hengyang 421001, Hunan, Peoples R China.;Hunan Univ Med, Sch Pharmaceut Sci, Hunan Prov Key Lab Synthet Biol Tradit Chinese Med, Huaihua 418000, Hunan, Peoples R China.
摘要:
Herein, we disclosed a highly efficient pathway toward 3-selenylated chromone derivatives via electrocatalytic cascade selenylation/cyclization/deamination of 2-hydroxyaryl enaminones with diselenides. This method showed mild conditions, easy operation, wide substrate scope, and good functional group tolerance. Furthermore, this electrosynthesis strategy was amendable to scale-up the reaction. Additionally, the preliminary experiments revealed that this reaction probably proceeded via a cation pathway instead of a radical pathway.
摘要:
Abstract Herein, we demonstrate the synthesis of azafluoranthene derivatives under mild conditions via [2+2+2] cycloaddition of 1,6‐diynes and nitriles catalyzed by CoBr2/dppp, exhibiting good atom economy. This procedure uses an inexpensive ligand and an earth‐abundant metal as catalyst to lower the cost of synthesis. Several azafluoranthenes are produced in 28–95% yields using this approach, featuring mild conditions, wide substrate scope, and good functional group tolerance. The fluorescence spectra of some azafluoranthenes indicate that these scaffolds have good photophysical properties for material science.
期刊:
CURRENT PHARMACEUTICAL BIOTECHNOLOGY,2024年 ISSN:1389-2010
通讯作者:
Yang, XY
作者机构:
[Yang, Xiaoyan; Yang, XY; Xie, Haimei; Lei, Xiaoyong; Yu, Jia] Univ South China, Hengyang Med Coll, Sch Pharmaceut Sci, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.;[Ou, Zhiwen] Univ South China, Chuanshan Coll, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.;[Yang, Xiaoyan; Lei, Xiaoyong] Univ South China, Hunan Prov Key Lab Tumor Microenvironm Respons Dru, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.
通讯机构:
[Yang, XY ] U;Univ South China, Hengyang Med Coll, Sch Pharmaceut Sci, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.
关键词:
PKM2;cancer;circRNA.;lncRNA;miRNA;ncRNAs
摘要:
Cancer is one of the main reasons for death, and it threatens human life and health. Both the environment and genes can lead to cancers. It dates back more than a million years; more importantly, tumor cells can not be detected until they grow to a large number. Currently, cancers are treated with surgical excision or non-surgical procedures. By studying the interaction between ncRNAs and PKM2, we aim to provide new targets for diagnosis, treatment, and prognosis for cancers. Read relevant articles and made a summary and classification. Non-coding RNAs (ncRNAs) are RNAs that do not code for proteins. They perform a function in transcription and translation and can be used as targets for cancer therapy. Pyruvate kinase M2 (PKM2) is a form of PKM, and it catalyzes the glycolysis of the final cellular processes to promote tumorigenesis. Not only that, but it also plays non-metabolic functions, including the expression of the gene, cell proliferation, cell migration, and tumor angiogenesis in cancer cells. The existing studies have found that microRNAs (miRNAs), long non-coding RNAs (lncRNAs), and circular RNAs (circRNAs) can promote or inhibit the aerobic glycolysis of cancer cells by affecting PKM2, which increases or decrease the risk of cancers and affect the progression of cancers. This review focuses on the mechanism of ncRNAs regulating PKM2 in cancers and summarizes the roles of some ncRNAs.
摘要:
As lncRNAs have increasingly been investigated, they are no longer simply defined as RNAs with no transcription capability. Studies have identified significant associations between the abnormal expression of lncRNAs and human diseases, particularly the mechanisms by which lncRNAs play a part in cancers, which are of considerable attention to researchers. As a result of the complex spatial structure, the mechanisms of interaction of lncRNAs in cancer cells are also complicated and diversified. Among a series of lncRNAs, TUG1, which is now considered to be a very high-value lncRNA, has recently been identified to express abnormally in some malignancies, leading to different alterations in cancer cells proliferation, migration, invasion, apoptosis, and drug resistance, and hence promoting or inhibiting cancer progression. Current studies have implicitly indicated that TUG1 can be used as a therapeutic target for human cancers. However, the biological functions of TUG1 have been studied for a short period of time, and the complete molecular mechanism still needs to be clarified. Accordingly, this review focuses on the principal molecular mechanisms of TUG1 in human cancers and the specific mechanisms of action in different cancer development processes based on existing studies.
摘要:
<jats:title>Abstract</jats:title><jats:p>A copper‐catalyzed direct C(<jats:italic>sp</jats:italic><jats:sup><jats:italic>2</jats:italic></jats:sup>)−H bond aminosulfonylation of maleimides is demonstrated. This protocol enables concurrent construction of C(<jats:italic>sp</jats:italic><jats:sup><jats:italic>2</jats:italic></jats:sup>)−N and C(<jats:italic>sp</jats:italic><jats:sup><jats:italic>2</jats:italic></jats:sup>)−SO<jats:sub>2</jats:sub> bonds in one‐step and features high efficiency, broad substrate scopes, good functional‐group tolerance, and mild reaction conditions. Preliminary mechanistic studies indicate that the reaction probably involves a radical way. Significantly, this method is applicable to synthesize derivatives of pharmaceuticals such as Desloratadine, Fluoxetine, Atomoxetine, and Maprotiline.</jats:p>
摘要:
Sirtuins are a family of NAD+-dependent deacetylases that regulate some important biological processes, including lipid metabolism and autophagy, through their deacetylase function. Autophagy is a new discovery in the field of lipid metabolism, which may provide a new idea for the regulation of lipid metabolism. There are many tandem parts in the regulation process of lipid metabolism and autophagy of sirtuins protein family. This paper summarized these tandem parts and proposed the possibility of sirtuins regulating lipid autophagy, as well as the interaction and synergy between sirtuins protein family. Currently, some natural drugs have been reported to affect metabolism by regulating sirtuins, some of which regulate autophagy by targeting sirtuins.
Lipid metabolism disorders, such as diabetes and atherosclerosis, have seriously harmed human health and caused economic and social burden. The role of sirtuins protein family in aging has been widely concerned, but they also show value in the regulation of lipid metabolism. Autophagy is a new discovery in the field of lipid metabolism, which may provide a new idea for the regulation of lipid metabolism. There are many tandem parts in the regulation process of lipid metabolism and autophagy of sirtuins protein family. This paper summarized these tandem parts and proposed the possibility of sirtuins regulating lipid autophagy, as well as the interaction and synergy between sirtuins protein family.
摘要:
PIWI proteins have a strong correlation with PIWI-interacting RNAs (piRNAs), which are significant in development and reproduction of organisms. Recently, emerging evidences have indicated that apart from the reproductive function, PIWI/piRNAs with abnormal expression, also involve greatly in varieties of human cancers. Moreover, human PIWI proteins are usually expressed only in germ cells and hardly in somatic cells, so the abnormal expression of PIWI proteins in different types of cancer offer a promising opportunity for precision medicine. In this review, we discussed current researches about the biogenesis of piRNA, its epigenetic regulatory mechanisms in human cancers, such as N6-methyladenosine (m6A) methylation, histone modifications, DNA methylation and RNA interference, providing novel insights into the markers for clinical diagnosis, treatment and prognosis in human cancers.
摘要:
This work describes the electrochemical selenylation of alkynyl aryl ketones, which shows high efficiency in the synthesis of 3‐selenylated chromones under transition‐metal‐free and chemical‐oxidant‐free conditions. This method features mild conditions, easy operation, and wide substrate scope. Abstract An electrochemical synthesis of various 3‐selenylated chromones via selenylation of alkynyl aryl ketones without the employment of catalyst and chemical‐oxidant is described here. This method features mild conditions, high efficiency, and wide substrate scope. Furthermore, the scale‐up reaction runs smoothly which indicates the practicability of this electrosynthesis strategy.