- 作 者: ( "chune dong" OR "chun-e dong" )
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Development of Highly Efficient Estrogen Receptor β-Targeted Near-Infrared Fluorescence Probes Triggered by Endogenous Hydrogen Peroxide for Diagnostic Imaging of Prostate Cancer.Molecules (IF 4.927) Pub Date : 2023-03-02 ,DOI:10.3390/molecules28052309Pei He,Xiaofei Deng,Bin Xu,Baohua Xie,Wenting Zou,Haibing Zhou,Chune Dong
Hydrogen peroxide is one of the most important reactive oxygen species, which plays a vital role in many physiological and pathological processes. A dramatic increase in H2O2 levels is a prominent feature of cancer. Therefore, rapid and sensitive detection of H2O2 in vivo is quite conducive to an early cancer diagnosis. On the other hand, the therapeutic potential of estrogen receptor beta (ERβ) has
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Anticancer or carcinogenic? The role of estrogen receptor β in breast cancer progressionPharmacology & Therapeutics (IF 13.4) Pub Date : 2023-01-20 ,DOI:10.1016/j.pharmthera.2023.108350Kang Shen, Huiguang Yu, Baohua Xie, Qiuyu Meng, Chune Dong, Kun Shen, Hai-Bing ZhouEstrogen receptor β (ERβ) is closely related to breast cancer (BC) progression. Traditional concepts regard ERβ as a tumor suppressor. As studies show the carcinogenic effect of ERβ, some people have come to a new conclusion that ERβ serves as a tumor suppressor in estrogen receptor α (ERα)-positive breast cancer, while it is a carcinogen in ERα-negative breast cancer. However, we re-examine the role ...
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Estrogen receptor β-targeted hypoxia-responsive near-infrared fluorescence probes for prostate cancer studyEuropean Journal of Medicinal Chemistry (IF 7.088) Pub Date : 2022-06-02 ,DOI:10.1016/j.ejmech.2022.114506Baohua Xie, Qiuyu Meng, Huiguang Yu, Kang Shen, Yan Cheng, Chune Dong, Hai-Bing ZhouAberrant expression of estrogen receptor β (ERβ) and tumor hypoxia have been observed in castration-resistant prostate cancer (CRPC); therefore, hypoxia-responsive labeling of ERβ will be beneficial for the early diagnosis and treatment of CRPC. Herein, we report the first ERβ-targeted hypoxia-responsive near-infrared fluorescent probes, which showed superior ERβ selectivity and favorable optical properties ...
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Discovery of Novel Bicyclic Phenylselenyl-Containing Hybrids: An Orally Bioavailable, Potential, and Multiacting Class of Estrogen Receptor Modulators against Endocrine-Resistant Breast CancerJournal of Medicinal Chemistry (IF 8.039) Pub Date : 2022-05-24 ,DOI:10.1021/acs.jmedchem.2c00525Xiangping Deng, Baohua Xie, Qiuzi Li, Yuan Xiao, Zhiye Hu, Xiaofei Deng, Pingping Fang, Chune Dong, Hai-Bing Zhou, Jian HuangBreast cancer (BC) is a multifactorial disease and is prone to drug resistance during treatment. In this study, we described a new class of multifunctional estrogen receptor (ER) modulators ground on a prerogative indirect antagonism skeleton (OBHS, oxabicycloheptene sulfonate) of ER containing a phenylselenyl group. Compound 34b showed significant antiproliferative activities against tamoxifen-sensitive ...
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Discovery of aminothiazole derivatives as novel human enterovirus A71 capsid protein inhibitorsBioorganic Chemistry (IF 5.307) Pub Date : 2022-03-07 ,DOI:10.1016/j.bioorg.2022.105683Zhichao Xu, Qi Tang, Ting Xu, Yang Cai, Ping Lei, Yinuo Chen, Wenting Zou, Chune Dong, Ke Lan, Shuwen Wu, Hai-Bing ZhouEnterovirus A71 (EV-A71), one of the major pathogens that causes hand, foot and mouth disease (HFMD), has seriously threatened the health and safety of young children. In this study, aminothiazole derivatives were synthesized and screened against EV-A71 in Rhabdomyosarcoma (RD) cells. The best compound (12s), with a biphenyl group, showed activity against EV-A71 (EC50: 0.27 μM) but also against a series ...
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Discovery of Aryl Benzoyl Hydrazide Derivatives as Novel Potent Broad-Spectrum Inhibitors of Influenza A Virus RNA-Dependent RNA Polymerase (RdRp)Journal of Medicinal Chemistry (IF 8.039) Pub Date : 2022-02-25 ,DOI:10.1021/acs.jmedchem.1c01257Xinjin Liu, Jinsen Liang, Yongshi Yu, Xin Han, Lei Yu, Feifei Chen, Zhichao Xu, Qi Chen, Mengyu Jin, Chune Dong, Hai-Bing Zhou, Ke Lan, Shuwen WuInfluenza A viruses possess a high antigenic shift, and the approved anti-influenza drugs are extremely limited, which makes the development of novel anti-influenza drugs for the clinical treatment and prevention of influenza outbreaks imperative. Herein, we report a series of novel aryl benzoyl hydrazide analogs as potent anti-influenza agents. Particularly, analogs 10b, 10c, 10g, 11p, and 11q exhibited ...
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Estrogen Receptor β-Targeted Near-Infrared Inherently Fluorescent Probe: A Potent Tool for Estrogen Receptor β ResearchACS Sensors (IF 9.618) Pub Date : 2021-12-16 ,DOI:10.1021/acssensors.1c01771Qiuyu Meng, Baohua Xie, Huiguang Yu, Kang Shen, Xiangping Deng, Hai-Bing Zhou, Chune DongEstrogen receptor β (ERβ) is associated with many diseases, and ERβ probes can help to reveal the complex role of ERβ and promote the development of ERβ-targeted therapy. Herein, we designed and synthesized the first ERβ-targeted near-infrared (NIR) inherently fluorescent probe P5, which showed the advantages of high ERβ selectivity, good optical properties, and excellent ERβ imaging capability in ...
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Establishment of evaluation criteria for the development of high quality ERα-targeted fluorescent probes.Analyst (IF 5.227) Pub Date : 2020-08-03 ,DOI:10.1039/d0an01172jQiuyu Meng,Xiaoyu Ma,Baohua Xie,Xiaofei Deng,Jian Huang,Hai-Bing Zhou,Chune DongERα-targeted fluorescent probes are important tools for ERα study. In order to develop high quality ERα-targeted probes, a sound and complete evaluation system is essential but has not been established yet. Herein, we set up a series of evaluation criteria for ERα-targeted fluorescent probes including ERα binding affinity, fluorescence quantum yield, cytotoxicity, ERα tracking capacity, ERα selectivity ...
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Rational design of ERα targeting hypoxia turn-on fluorescent probes with antiproliferative activity for breast cancer.Chemical Communications (IF 6.065) Pub Date : 2020-07-30 ,DOI:10.1039/c9cc09754fQiuyu Meng,Baohua Xie,Xiaoyu Ma,Zhiye Hu,Fuling Zhou,Hai-Bing Zhou,Chune DongThe overexpression of estrogen receptor (ER) α is not only closely related to the development of ER+ breast cancer, but is also an important biomarker for clinical diagnosis and treatment. Herein, we report several ERα targeting hypoxia turn-on fluorescent probes with antitumor activity for breast cancer cells. Among them, probes 3 and 5 displayed good ERα targeting ability and favorable hypoxia turn-on ...
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Design, synthesis and biological evaluation of novel dual-acting modulators targeting both estrogen receptor α (ERα) and lysine-specific demethylase 1 (LSD1) for treatment of breast cancer.European Journal of Medicinal Chemistry (IF 7.088) Pub Date : 2020-04-03 ,DOI:10.1016/j.ejmech.2020.112281Ming He,Wentao Ning,Zhiye Hu,Jian Huang,Chune Dong,Hai-Bing ZhouBreast cancer is a multi-factor disease, thus more and more drug combination therapies are applied in the treatment. However, there are undeniable disadvantages in drug combination therapy. Therefore, the development of new dual-targeting drugs has become a new strategy. In this study, we have developed a series of dual-acting agents targeting both estrogen receptor α (ERα) and histone demethylase ...
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Construction of benzofuranone library via a metal-free, one-pot intermolecular condensation, and their application as efficient estrogen receptor β modulators.Chemical Communications (IF 6.065) Pub Date : 2019-10-29 ,DOI:10.1039/c9cc05756kXueke Peng,Zhiye Hu,Jing Zhang,Wentao Ning,Silong Zhang,Chune Dong,Xiaodong Shi,Hai-Bing ZhouFacile synthesis of benzofuranone was achieved through a metal-free, one-pot intermolecular condensation between α-hydroxy aryl ketones and resorcinol derivatives. A library of 20 compounds with moderate to good overall yields was prepared. These compounds showed strong binding toward estrogen receptors along with good selectivity for ERβ (>190-fold over ERα). Anti-proliferative activity on DU-145 ...
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Novel class of 7-Oxabicyclo[2.2.1]heptene sulfonamides with long alkyl chains displaying improved estrogen receptor α degradation activityEuropean Journal of Medicinal Chemistry (IF 7.088) Pub Date : 2019-08-08 ,DOI:10.1016/j.ejmech.2019.111605Zhiye Hu,Yuanyuan Li,Baohua Xie,Wentao Ning,Yuan Xiao,Yuan Huang,Chenxi Zhao,Jian Huang,Chune Dong,Hai-Bing ZhouHormone therapy is widely used in clinic for breast cancer treatment, such as tamoxifen, but long-term use can cause drug resistance. In this regard, a strategy based on small molecule-induced protein degradation, i.e. selective estrogen receptor downregulator (SERD), might be an effective alternative to hormone therapy for breast cancer. However, most of the SERD candidates involve very limited scaffolds ...
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Exploring the PROTAC degron candidates: OBHSA with different side chains as novel selective estrogen receptor degraders (SERDs)European Journal of Medicinal Chemistry (IF 7.088) Pub Date : 2019-03-26 ,DOI:10.1016/j.ejmech.2019.03.058Yuanyuan Li,Silong Zhang,Jing Zhang,Zhiye Hu,Yuan Xiao,Jian Huang,Chune Dong,Shengtang Huang,Hai-Bing ZhouAs the mutant estrogen receptor (ER) continues to be characterized, breast cancer is becoming increasingly difficult to cure when treated with hormone therapy. In this regard, a strategy to selectively and effectively degrade the ER might be an effective alternative to endocrine therapy for breast cancer. In a previous study, we identified a novel series of 7-oxabicyclo[2.2.1]heptene sulfonamide (OBHSA) ...
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Design and synthesis of heteroaromatic-based benzenesulfonamide derivatives as potent inhibitors of H5N1 influenza A virus†RSC Medicinal Chemistry (IF 3.47) Pub Date : 2018-11-23 ,DOI:10.1039/c8md00474aYongshi Yu,Tazeem Tazeem,Zhichao Xu,Liaoqi Du,Mengyu Jin,Chune Dong,Hai-Bing Zhou,Shuwen Wu
Influenza A virus is an enveloped negative single-stranded RNA virus that causes febrile respiratory infection and represents a clinically challenging threat to human health and even lives worldwide. Even more alarming is the emergence of highly pathogenic avian influenza (HPAI) strains such as H5N1, which possess much higher mortality rate (60%) than seasonal influenza strains in human infection.
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Synthesis and structure-activity relationship study of arylsulfonamides as novel potent H5N1 inhibitorsEuropean Journal of Medicinal Chemistry (IF 7.088) Pub Date : 2018-09-27 ,DOI:10.1016/j.ejmech.2018.09.065Yongshi Yu,Qi Tang,Zhichao Xu,Siliang Li,Mengyu Jin,Zixuan Zhao,Chune Dong,Shuwen Wu,Hai-Bing ZhouH5N1 virus, one subtype of highly pathogenic influenza A virus in human infection, has recently received attention due to its unpredictable and high mortality. In this study, a series of arylsulfonamide derivatives were identified as improved H5N1 inhibitors for the influenza treatment by systematic structure-activity relationship investigation. Among them, the most potent H5N1 inhibitor 3h exhibited ...
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Novel Hybrid Conjugates with Dual Suppression of Estrogenic and Inflammatory Activities Display Significantly Improved Potency against Breast CancerJournal of Medicinal Chemistry (IF 8.039) Pub Date : 2018-07-27 ,DOI:10.1021/acs.jmedchem.8b00224Wentao Ning,Zhiye Hu,Chu Tang,Lu Yang,Silong Zhang,Chune Dong,Jian Huang,Hai-Bing ZhouIn this work, we developed a small library of novel OBHS-RES hybrid compounds with dual inhibition activities targeting both the estrogen receptor α (ERα) and NF-κB by incorporating resveratrol (RES), a known inhibitor of NF-κB, into a privileged indirect antagonism structural motif (OBHS, oxabicycloheptene sulfonate) of estrogen receptor (ER). The OBHS-RES conjugates could bind well to ER and showed ...
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Estrogen receptor sensing in living cells by a high affinity turn-on fluorescent probeSensors and Actuators B: Chemical (IF 9.221) Pub Date : 2018-06-06 ,DOI:10.1016/j.snb.2018.06.022Lu Yang,Qiuyu Meng,Zhiye Hu,Wentao Ning,Jie Zheng,Chune Dong,Hai-Bing ZhouThe estrogen receptors (ERα and ERβ) are vital transcription factors that play important role in physiological functions and are responsible for many hormone-regulated diseases. Herein, we report an environment-sensitive fluorescent probe 2 with a turn-on switch for in situ visualization of the estrogen receptor in living cells. Probe 2 exhibited high ER binding affinity and showed intense fluorescence ...
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Enantioselective Chlorocyclization of Olefinic Amides with 1,3-Dichloro- 5, 5-Dimethylhydantoin (DCDMH) Catalyzed by (DHQD) 2PHALWuhan University Journal of Natural Sciences Pub Date : 2018-05-17 ,DOI:10.1007/s11859-018-1319-9Qingjun Zhou,Chao Guo,Xiwang Li,Pei He,Guichun Yang,Chune DongAn efficient catalytic asymmetric chlorocyclization of olefinic amides with 1,3-dichloro-5,5-dimethylhydantoin (DCDMH) using hydroquinidine 1,4-phthalazinediyl diether ((DHQD)2PHAL) as organocatalyst has been developed. Series of chiral chloro substituted isobenzofuran-1(3 H )-imine derivatives were obtained in good yields (up to 85%) and enantioselectivities (up to 70% ee). ...
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Enantioselective Chlorocyclization of Olefinic Amides with 1,3-Dichloro- 5, 5-Dimethylhydantoin (DCDMH) Catalyzed by (DHQD)2PHALWuhan University Journal of Natural Sciences Pub Date : 2018-05-17 ,DOI:10.1007/s11859-018-1319-9Qingjun Zhou, Chao Guo, Xiwang Li, Pei He, Guichun Yang, Chune DongAn efficient catalytic asymmetric chlorocyclization of olefinic amides with 1,3-dichloro-5,5-dimethylhydantoin (DCDMH) using hydroquinidine 1,4-phthalazinediyl diether ((DHQD)2PHAL) as organocatalyst has been developed. Series of chiral chloro substituted isobenzofuran-1(3H)-imine derivatives were obtained in good yields (up to 85%) and enantioselectivities (up to 70% ee). ...
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A high-affinity subtype-selective fluorescent probe for estrogen receptor β imaging in living cells†Chemical Communications (IF 6.065) Pub Date : 2018-03-23 ,DOI:10.1039/c8cc00483hZhiye Hu,Lu Yang,Wentao Ning,Chu Tang,Qiuyu Meng,Jie Zheng,Chune Dong,Hai-Bing ZhouEstrogen receptor β (ERβ) has recently been identified as a pharmaceutical target in hormone replacement therapy for breast cancers. However, the biological function of ERβ in disease progression remains unclear. A highly ERβ-selective fluorescent probe (FPNM) was discovered exhibiting nanomolar affinity for ERβ with an ERβ/ERα selectivity as high as 80, which allowed specific labeling of intracellular ...
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One-step pathway to selenoisobenzofuran-1(3H)-imine derivatives through highly selective selenocyclization of olefinic amides with benzeneselenyl chloride†Organic & Biomolecular Chemistry (IF 3.89) Pub Date : 2018-03-01 ,DOI:10.1039/c8ob00179kXiwang Li,Pei He,Hai-Bing Zhou,Chune DongA 1,4-diazabicyclo[2.2.2]octane (DABCO) catalyzed selenocyclization of olefinic amides was achieved under mild reaction conditions. The reaction formed various benzeneselenyl substituted isobenzofuran-1(3H)-imine derivatives in good yields. The product was determined using single-crystal X-ray analysis. For compound 2u, the relative stereochemistry was established on the basis of NOESY NMR studies ...
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Enantioselective synthesis of novel pyrano[3,2-c]chromene derivatives as AChE inhibitors via an organocatalytic domino reaction†Organic & Biomolecular Chemistry (IF 3.89) Pub Date : 2017-12-14 ,DOI:10.1039/c7ob02794jJie Zheng,Ming He,Baohua Xie,Lu Yang,Zhiye Hu,Hai-Bing Zhou,Chune DongA series of optically active pyrano[3,2-c]chromenes have been synthesized through an asymmetric domino reaction of 4-hydroxy-2H-chromen-2-ones with malononitriles. The targeted molecules were obtained in excellent yields and enantioselectivities (up to 94% yield, 99% ee). The AChE inhibitory activity studies revealed that compounds 4n (IC50 = 21.3 μM) and 4p (IC50 = 19.2 μM) displayed potent acetylcholinesterase ...
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Recent advances in gossypol derivatives and analogs: a chemistry and biology view.Future Medicinal Chemistry (IF 4.767) Pub Date : 2017-07-20 ,DOI:10.4155/fmc-2017-0046Yuzhi Lu,Jun Li,Chun-E Dong,Jian Huang,Hai-Bing Zhou,Wei WangGossypol as a natural occurring polyphenol has been studied in a wide range of therapeutic contexts for a long time. The chemical modifications on gossypol were limited due to the unique chemical properties of polyphenols. The design and synthesis of gossypol derivatives and the exploration of their biological activities are the interest of the synthetic chemists, medicinal chemists and pharmacologists ...
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Recent advances in gossypol derivatives and analogs: a chemistry and biology viewFuture Medicinal Chemistry (IF 4.767) Pub Date : 2017-07-01 ,DOI:10.4155/fmc-2017-0046Yuzhi Lu, Jun Li, Chun-E Dong, Jian Huang, Hai-Bing Zhou, Wei WangGossypol as a natural occurring polyphenol has been studied in a wide range of therapeutic contexts for a long time. The chemical modifications on gossypol were limited due to the unique chemical properties of polyphenols. The design and synthesis of gossypol derivatives and the exploration of their biological activities are the interest of the synthetic chemists, medicinal chemists and pharmacologists ...
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Rational design and optimization of selenophenes with basic side chains as novel potent selective estrogen receptor modulators (SERMs) for breast cancer therapyRSC Medicinal Chemistry (IF 3.47) Pub Date : 2017-05-24 ,DOI:10.1039/c7md00163kJunjie Luo,Zhiye Hu,Yuan Xiao,Tongxin Yang,Chune Dong,Jian Huang,Hai-Bing Zhou
To increase the diversity of estrogen receptor (ER) ligands having novel structures and activities, series of selenophene derivatives with a basic side chain (BSC) were synthesized and their biological activity as subtype-selective antagonists for the ER was explored. Compared with the selenophenes without a BSC, most compounds showed an increase in binding affinity, and several compounds displayed
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Rational design and optimization of selenophenes with basic side chains as novel potent selective estrogen receptor modulators (SERMs) for breast cancer therapyRSC Medicinal Chemistry (IF 3.47) Pub Date : 2017-05-24 ,DOI:10.1039/c7md00163kJunjie Luo,Zhiye Hu,Yuan Xiao,Tongxin Yang,Chune Dong,Jian Huang,Hai-Bing Zhou
To increase the diversity of estrogen receptor (ER) ligands having novel structures and activities, series of selenophene derivatives with a basic side chain (BSC) were synthesized and their biological activity as subtype-selective antagonists for the ER was explored. Compared with the selenophenes without a BSC, most compounds showed an increase in binding affinity, and several compounds displayed
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Rational Design and Optimization of Selenophenes with Basic Side Chains as Novel Potent Selective Estrogen Receptor Modulators (SERMs) for Breast Cancer TherapyRSC Medicinal Chemistry (IF 3.47) Pub Date : 2017-05-24 ,DOI:10.1039/c7md00163kJunjie Luo,Zhiye Hu,Yuan Xiao,Tongxin Yang,Chune Dong,Jian Huang,Hai-Bing Zhou
To increase the diversity of estrogen receptor (ER) ligands having novel structures and activities, series of selenophene derivatives with a basic side chain (BSC) were synthesized and their biological activity as subtype-selective antagonist for the ER was explored. Compared with the selenophenes without a BSC, most compounds showed an increase in binding affinity, and several compounds displayed
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Dual functional small molecule fluorescent probes for image-guided estrogen receptor-specific targeting coupled potent antiproliferative potency for breast cancer therapyBioorganic & Medicinal Chemistry (IF 3.461) Pub Date : 2017-05-04 ,DOI:10.1016/j.bmc.2017.05.002Lu Yang,Zhiye Hu,Junjie Luo,Chu Tang,Silong Zhang,Wentao Ning,Chune Dong,Jian Huang,Xianjun Liu,Hai-Bing ZhouA strategy by integrating biological imaging into early stages of the drug discovery process can improve our understanding of drug activity during preclinical and clinical study. In this article, we designed and synthesized coumarin-based nonsteroidal type fluorescence ligands for drug-target binding imaging. Among these synthesized compounds, 3e, 3f and 3h showed potent ER binding affinity and 3e ...
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Furan-carboxamide derivatives as novel inhibitors of lethal H5N1 influenza A viruses†RSC Advances (IF 4.036) Pub Date : 2017-02-01 ,DOI:10.1039/c7ra00305fYongshi Yu,Jie Zheng,Lei Cao,Shu Li,Xiwang Li,Hai-Bing Zhou,Xianjun Liu,Shuwen Wu,Chune Dong
In this study, we reported the synthesis and biological characterization of a novel series of furan-carboxamide derivatives that were potent inhibitors of the influenza A H5N1 virus. The systematic structure–activity relationship (SAR) studies demonstrated that the 2,5-dimethyl-substituted heterocyclic moiety (furan or thiophene) had significant influence on the anti-influenza activity. In particular
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Selenophenes: Introducing a New Element into the Core of Non‐Steroidal Estrogen Receptor LigandsChemMedChem (IF 3.54) Pub Date : 2017-01-09 ,DOI:10.1002/cmdc.201600593Silong Zhang,Zhiyong Wang,Zhiye Hu,Changhao Li,Chu Tang,Kathryn E. Carlson,Junjie Luo,Chune Dong,John A. Katzenellenbogen,Jian Huang,Hai-Bing Zhou
The importance of the heterocyclic core elements with peripheral phenolic and alkyl substituents as a dominant structural motif of ligands for the estrogen receptor (ER) has been well recognized. In this study we expanded the structural diversity of core elements by preparing selenium‐containing heterocycles and exploring the activities of these selenophenes on the two ERs, ERα and ERβ. Careful structure–activity
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