摘要：
DBU-promoted trifluoromethylation of aryl iodides with difluoromethyltriphenylphosphonium bromide (DFPB) in the presence of copper source is described. In this transformation, DBU not only acts as base to deprotonate the difluoromethyl group in DFPB to generate difluoromethylene phosphonium ylide Ph_3P~+CF_2~-,but also converts the difluorocarbene generated from ylide Ph_3P~+CF_2~-- into trifluoromethyl anion, finally resulting in the trifluoromethylation of aryl iodides. The reactions proceeded smoothly to afford expected products in moderate to good yields.
摘要：
A novel series of iodo-chrysin derivatives with resorcinol as raw materials were synthesized according to Baker-Venkataraman reaction and their inhibitory activities in vitro against thyroid cancer cell lines (SW-579 and TT) were evaluated by the standard methyl thiazole tetrazolium (MTT) method. Biological test results showed that these derivatives possessed stronger anti-thyroid cancer activities than 5-FU. Compound 21 showed the strongest activity against SW-579 cell lines with IC50 value of 3.4μM and compound 10 showed the strongest activity against TT cell lines with IC50 value of 6.2μM, it was better than 5-FU (59.3μΜ, 18.4μM respectively).
作者机构：
[Xu Yao,; Zehua Yang,; Zhuo Liu,; Jin Long,; Menghui Xiang,; Yi Gao,,; Baojun Su,,; Ye Zhang,,; Hong Li,,; Siyu Wu,,; Tingjuan Wu,,; Xing Zheng,] Institute of Pharmacy & Pharmacology, University of South China;[Xu Yao,; Zehua Yang,; Zhuo Liu,; Jin Long,; Menghui Xiang,; Yi Gao,,; Baojun Su,,; Ye Zhang,,; Hong Li,,; Siyu Wu,,; Tingjuan Wu,,; Xing Zheng,] Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study;[Xu Yao,; Zehua Yang,; Zhuo Liu,; Jin Long,; Menghui Xiang,; Yi Gao,,; Baojun Su,,; Ye Zhang,,; Hong Li,,; Siyu Wu,,; Tingjuan Wu,,; Xing Zheng,] Research Interest Group, University of South China
摘要：
A novel series of fluorinated apigenin derivatives were synthesized and in vitro inhibitory activities against HL-60,HT-29 and SGC-7901 tumor cell lines were evaluated by the standard methyl thiazole tetrazolium（MTT） method. The results showed that some of fluorinated apgenin derivatives had higher anticancer activity than 5-Fu.
通讯机构：
[Zheng, Xing] U;[Zhao, Weili] F;[Zheng, Xing] H;Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.;Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China.
关键词：
fluorescent probe;palladium;living cell
摘要：
A novel turn-on fluorescent probe for the detection of palladium has been designed. The probe can selectively and sensitively detect palladium in solution, and the limit of detection was calculated to be 11.4 nmol?L~(-1). Furthermore, the probe was successfully used for fluorescence imaging of palladium in living cells.
摘要：
Context: Hepatocellular carcinoma (HCC) is a common cancer around the world, with high mortality rate. Currently, there is no effective drug for the therapy of HCC. Ursolic acid (UA) is a natural product which exists in various medicinal herbs and fruits, exhibiting multiple biological effects such as its outstanding anticancer and hepatoprotective activity, which has drawn many pharmacists' attention. Objective: This paper summarizes the current status of the hepatoprotective activity of UA analogues and explains the related mechanism, providing a clear direction for the development of novel anti-HCC drugs. Methods: All of the data resources were derived from PubMed. By comparing the IC50 values and analyzing the structure-activity relationships, we listed compounds with good pharmacological activity from the relevant literature, and summarized their anti-HCC mechanism. Results: From the database, 58 new UA derivatives possessing wonderful anticancer and hepatoprotective effects were listed, and the relevant anti-HCC mechanism were discussed. Conclusion: UA's anti-HCC effect is the result of combined action of many mechanisms. These 58 new UA derivatives, particularly compounds 45 and 53, can be used as potential drugs for the treatment of liver cancer.
摘要：
Macrophage-activating lipopeptide-2 (MALP-2) has been shown to promote the development of atherosclerosis. ATP-binding cassette transporter A1 (ABCA1), a transmembrane protein, plays a critical role in mediating cholesterol export from macrophages to apolipoprotein A-I (apoA-I). However, whether MALP-2 can regulate the expression of ABCA1 is still largely unknown. The aim of this study was to explore the effects of MALP-2 on ABCA1 expression in THP-1 macrophages and the underlying mechanisms. Our results showed that the treatment of cells with MALP-2 decreased ABCA1 level and suppressed cholesterol efflux in both concentration- and time-dependent manners. The contents of intracellular cholesterol were significantly increased in the presence of MALP-2. Moreover, MALP-2-mediated inhibition of ABCA1 expression was abolished by siRNA of either Toll-like receptor 2 (TLR2) or nuclear factor κB (NF-κB). A similar effect was produced by treatment with the NF-κB inhibitor pyrrolidine dithiocarbamate. In addition, MALP-2-induced activation of NF-κB markedly increased zinc finger protein 202 (ZNF202) level, and ZNF202 siRNA impaired the effects of MALP-2 on ABCA1 expression. Taken together, these results suggest that MALP-2 can decrease ABCA1 expression and subsequent cholesterol efflux through activation of the TLR2/NF-κB/ZNF202 signaling pathway in THP-1 macrophages.
通讯机构：
[Jiang, Zhong-Xing] W;Wuhan Univ, Key Lab Combinatorial Biosynth & Drug Discovery, Minist Educ, Wuhan 430071, Peoples R China.
摘要：
To achieve high sensitivity for 19F MRI, a class of novel dendritic molecules with multiple pseudosymmetrical fluorines was designed and efficiently synthesized. Through iterative bromination and Williamson ether synthesis under mild conditions, a fluorinated dendrimer with 540 pseudosymmetrical fluorines was conveniently prepared without performing the group protection in a convergent way. The dendrimer is characterized by a strong 19F NMR peak and short relaxation times. Eventually, an appreciably enhanced 19F MRI at an extremely low concentration (18.5 μM) was achieved, which demonstrated the potential utility of such dendritic molecules in highly sensitive 19F MRI.
期刊：
Journal of Heterocyclic Chemistry,2015年52(1):296-301 ISSN：0022-152X
通讯作者：
Zheng, Xing
作者机构：
[Liu, Yun-Mei; Wang, Hui; Wang, Yu-Hong; Yao, Xu; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.;[Liao, Duan-Fang; Zheng, Xing] Hunan Univ Chinese Med, Div Stem Cell Regulat & Applicat, State Key Lab Chinese Med Powder & Med Innovat Hu, Changsha 410208, Hunan, Peoples R China.;[Tong, Min] Xianyang Cent Hosp, Xianyang 712000, Shanxi, Peoples R China.
通讯机构：
[Zheng, Xing] U;Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.
摘要：
A series of trifluoromethylated aurone derivatives were synthesized, and the structure of 6-hydroxy-4-trifluoromethylated aurone was determined by single crystal X-ray analysis. Their anticancer activities against leucocythemia (HL-60) and colorectal adenocarcinoma (HT-29) were evaluated by the standard MTT method in vitro with 5-fluorouracil as a positive contrast drug. The results showed that all the (Z)-trifluoromethylated aurone derivatives had potential anticancer activities.
摘要：
Cross-coupling between difluorocarbene and carbene-derived intermediates generated from diazocompounds was developed to give gem-difluoroolefins, which constitutes a fast practical pathway to achieve hindered gem-difluoroolefins. The cross-coupling between difluorocarbene and aryl diazoacetates proceeded smoothly in the presence of a copper source, whereas its coupling with diaryl diazomethanes occurred well under metal-free conditions. A mechanism involving a copper–difluorocarbene complex was proposed.
通讯机构：
[Zheng, Xing] U;Univ South China, Inst Pharm Pharmacol, Hengyang 421001, Peoples R China.
摘要：
Both 19F MRI and optical imaging are powerful noninvasive molecular imaging modalities in biomedical applications. To integrate these two complementary imaging modalities, the design and synthesis of a novel 19F MRI/fluorescence dual-modal imaging agent is reported herein. Through Sonogashira coupling reaction between the fluorinated phenylacetylene and 1,2,4,5-tetraiodobenzene, a fluorophore with 48 symmetrical fluorines at its periphery was constructed with high efficacy. High aqueous solubility was achieved by PEGylation of the fluorophore with monodisperse PEGs. However, an unexpected self-assembly of the PEGylated amphiphilic fluorophore in water “turned off” the 19F NMR signal. However, hydrogenation of the triple bonds or introduction of branched monodisperse PEGs was able to efficiently tune the self-assembly, resulting in the “turning on” of the 19F NMR signal. One of these amphiphiles combines the advantages of label-free fluorescence, high 19F MRI sensitivity, biocompatibility, and excellent aqueous solubility. The results demonstrate the great potential of such amphiphiles for real-time 19F MRI and fluorescence dual-modality imaging.
作者机构：
[Xiao, Yan; Song, Chen; Zheng, Qutong; Lei, Xiaoyong; Chen, Hongfei; Zeng, Xianliang; Zhang, Yinxiang; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[Xiao, Yan; Song, Chen; Zheng, Qutong; Lei, Xiaoyong; Chen, Hongfei; Zeng, Xianliang; Zhang, Yinxiang; Zheng, Xing] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.;[Song, Chen; Zhang, Yinxiang] Univ South China, Res Interest Grp Pharm, Hengyang 421001, Peoples R China.
通讯机构：
[Zheng, Xing] U;Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
摘要：
Resveratrol (3,5,4-trihydroxy-trans-stilbene) is a well-known natural polyphenol compound. It is reported that resveratrol poees strong anti-oxidative, anti-inflammatory, cardiovascular protective and cancer chemo-preventive effects. Therefore, there has been a considerable interest in its biological activity, pharmacological activity and also synthetic resveratrol analogues in recent years. Up to now, many new resveratrol derivatives have been synthesized and some new biological activities of these compounds have been found, so in the treatment of Alzheimer's disease and the inhibition of influenza H1N1 neuraminidase. Structure-activity studies revealed that crucial elements of parental components are required for specific effects. This review summarizes the available literatures on the structure-activity relationships and pharmacological properties of resveratrol analogues.
