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检索条件"任意字段=第11届世界华人药物化学研讨会（ISCMC2018）"

共 414 条记录，以下是121-130 订阅

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Chiral ruthenium(Ⅱ) complexes as potential inhibitor against the growth of heptitic cancer via antiangiogenesis and DNA damage

Chiral ruthenium(Ⅱ) complexes as potential inhibitor agains...

引用

第11届世界华人药物化学研讨会（iscmc 2018）

作者： Gengnan Yu Jieqiong Cao Yumei Li Qiong Wu Bowen Lian Wenjie Mei School of Pharmacy Guangdong Pharmaceutical University School of Chemistry Jinan University School of Public Health Guangdong Pharmaceutical University

Ruthenium complexes have long been demeonstrated as anticancer *** a chiral ruthenium complex have been prepared and the evaluation of in vivo inhibitory activities against tumor in mice revealed that ruthenium complex can inhibit the growth of hepatitic *** antiangiogenesis result demonstrated that ruthenium complex can inhibit the growth of new vessels and show great antiangiogenesis activity to tumor with low *** TUNEL analysis comet assays and DNA binding behaviour study shown that ruthenium complex could bind to double stranded-DNA and cause the DNA damage to induce the apoptosis of tumor cells. Taken together,these results suggested that ruthenium complex have potential application as anticancer and antiangiogenesis chemical drugs with a low toxicity.

关键词： ruthenium complex anticancer antiangiogenesis DNA damage low toxicity

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Discovery of a potent inhibitor of DCN1-UBC12 interaction

Discovery of a potent inhibitor of DCN1-UBC12 interaction

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Yunkai Shi Wenjuan Zhou Yu Liu Jingjing Song Yanyan Que Wen Zhao Bin Yu Hongmin Liu School of Pharmaceutical Sciences Zhengzhou University

DCN1-UBC12 interaction is a necessary step for the neddylation of protei,which is a key process in protein *** this interaction can influence the protein degradation and can be a new therapeutic *** the prevalence and importance of the interaction,we sought to find small molecules to inhibit this *** on the hit compound previously identified in our lab,we synthesized a series of compounds and tested their inhibitory activity against *** data demonstrated that these compounds had good inhibitory activity,of which the most potent compound inhibited DCNl with an IC value of380 *** activity relationship analysis suggest that the compound could be further optimized.

关键词： DCN1-UBC12 Neddylation pathway

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Discovery of peptide borate derivatives as histone deacetylase(HDAC) and proteasome dual inhibitors for cancer treatment

Discovery of peptide borate derivatives as histone deacetyla...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Yi Zhou Xinying Yang Hao Fang Department of Medicinal Chemistry Key Laboratory of Chemical Biology(Ministry of Education)School of PharmacyShandong University

Single use of HDAC inhibitors failed to show satisfied clinical benefits in cancer *** dozens of clinical researches of combination of HDAC inhibitor and other anti-tumor agents were carried *** most successful combination,panobinostat(HDAC inhibitor),bortezomib(the first launched proteasome inhibitor) and dexamethasone,was approved by FDA in 2015 for the treatment of multiple myeloma(MM).Therefore,we designed and synthesized a series of target compounds as dual inhibitors targeting both HDAC and proteasome(Fig.1 A).In biological evaluations,ZY-1 showed potent enzymatic inhibitory activities and excellent antitumor activities(Fig.1 B-E).

关键词： histone deacetylase proteasome dual inhibitor anti-tumor

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Design,synthesis,and evaluation of carboxyl-modified oseltamivir derivatives with improved lipophilicity as neuraminidase inhibitors

Design,synthesis,and evaluation of carboxyl-modified oseltam...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Boyu Wang Kuanglei Wang Peipei Meng Yaping Hu Fei Yang Kemin Liu Zaiqiang Lei Binfeng Chen Yongshou Tian Key Laboratory of Structure-Based Drug Design and Discovery Ministry of EducationShenyang Pharmaceutical University Wuyi University

In this study,a series of carboxyl-modified oseltamivtr analogs with improved lipophilicily were designed and synthesized,and their inhibitory activities against neuraminidase from influenza A virus H5 N1 subtype were *** results demonstrated that compound 5 m exhibited potent inhibitory activity(IC = 1.30 ± 0.23 μM),and it targeted the recently discovered *** Sm（Log D =-0.12） is more lipophilic than oseltamivir carboxylate（Log D =-1.69） at pH 7.4,which is potentially propitious to improved membrane permeability and oral drug ***,Sm showed high stability in human liver *** findings of this study can be valuable in identifying neuraminidase inhibitors with optimal lipophilicily and in the exploration of 430-cavity.

关键词： Influenza virus Neuraminidase inhibitors Oseltamivir derivatives

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Design,synthesis and biological evaluation of novel indole-based hybrids

Design,synthesis and biological evaluation of novel indole-b...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Feifei Yang Liying Ma Hongmin Liu Collaborative Innovation Center of New Drug Research and Safety Evaluation Henan Province Key Laboratory of Advanced Drug Preparation Technologies(Zhengzhou UniversityMinistry of Education)

Cancer is the most serious human disease and one of the highest global *** people start to study and develop new anticancer drugs with physiological *** products play an important role in the processes of our human *** derived from therapeutic plants are indole alkaloids（Figure 1）.Indole nucleus contained in berberine have been used in the study of chemical chemistry and are considered to be a backbone with potential *** thiazole-contained compounds have been reported to possess some antibacterial,anticonvulsant,antifungal,antiviral and anticancer ***,based on the concept of molecular hybridization,we designed and synthesized a series of hybrids of indole-azole based tertiary amine,which are so easy to salt that we can study the inhibitory activity of the *** of the target compounds exhibited good anticancer activity against the gastric cancer cell *** mechanism investigations are under way and will be reported in due course.

关键词： LSD1 Cancer indole structure terminal alkynes tertiary amine

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Design,synthesis and antitumor activities of Ox/Re-sensitive prodrugs conjugating in situ with albumin

Design,synthesis and antitumor activities of Ox/Re-sensitive...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Jincheng Yang Lixue Chen Liangliang Tian Youjun Xu School of Pharmaceutical Engineering Shenyang Pharmaceutical University

The efficacy of traditional chemotherapy often suffers from rapid clearance and off-target *** our work,The human serum albumin was employed as a drug vechile,the traditional anticancer drug paclitaxel and camptothecin was linked to an N-substituted maleimide group by a biosensitive,cleavable *** intravenous administration,the prodrugs bind rapidly to the Cys-34 position of circulating albumin and accumulate in solid tumors due to passive targeting and the enhanced permeation and retention effect .The hyperpermeability of tumor vessels and the absence of functional lymphatic circulation allow the prodrug-albumin conjugates to remain in tumors for a long *** prodrugs could be triggered by a unique tumor microenvironment,high concentration of reactive oxygen species（ROS）/glutathione（GSH） to release the paclitaxel or *** bioresponsive prodrug strategy demonstrates potent chemotherapeutic efficiency in vivo and may be utilized in clinical cancer therapy.

关键词： Paclitaxel Camptothecin albumin-conjugate Ox/Re-sensitive release prodrugs

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Novel environment-sensitive fluorescent probes for p53-MDM2 protein-protein interaction

Novel environment-sensitive fluorescent probes for p53-MDM2 ...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Gaopan Dong Yan Jiang Xiang Li Lupei Du Chunquan Sheng Minyong Li Department of Medicinal Chemistry Key Laboratory of Chemical Biology(MOE)School of PharmacyShandong University Department of Medicinal Chemistry School of PharmacySecond Military Medical University

Based on the previous work,a series of novel probes with much better practical activity and selectivity in vivo and in vitro are designed and *** small-molecule fluorescent tum-on probes are no-washable and ***,all the probes showed potent inhibitory and acceptable cell toxicity compared with commercial available p53-MDM2 inhibitor Nutlin-3,their application in cell imaging and detecting p53-MDM2 protein-protein interaction have been further *** environment-sensitive fluorescent turn-on probes are more affordable and rapid in imaging,also expecting for the application in target drug screening.

关键词： cell imaging p53-MDM2 protein-protein interaction fluorescent probes

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The discovery of novel selective CXCR2 antagonists by using ligand-based pharmacophore model

The discovery of novel selective CXCR2 antagonists by using ...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Jinxin Che Zhilong Wang Haichao Sheng Youhong Hu Xin Xie Xiaowu Dong Yongzhou Hu ZJU-ENS Joint Laboratory of Medicinal Chemistry College of Pharmaceutical SciencesZhejiang University CAS Key Laboratory of Receptor Research the National Center for Drug ScreeningShanghai Institute of Materia MedicaChinese Academy of Sciences State Key Laborarory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of Sciences

Recently a growing interest has been shown for the CXC chemokine receptor 2（CXCR2）,due to their involvement in metastasis and immune physiology. In our study,compound D45 was identified with pharmacophore model which showed potent CXCR2 antagonist activity with an IC value of 10 nM,910-fold selectivity against CXCR1,90% bioavailability in rat and good in vitro anti-tumor metastatic effect in wound healing assay.

关键词： Tumor metastasis Immune suppression CXC chemokine receptor 2 Selective Pharmacophore model Bioavailability

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Design,synthesis,and biological evaluation of 14-O-derivatives of natural oridonin as antitumor agents

Design,synthesis,and biological evaluation of 14-O-derivativ...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Qingkun Shen Zheshan Quan Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain Affiliated Ministry of EducationCollege of PharmacyYanbian University

Oridonin is a widely distributed ent-kaurene in the Rabdosia plants and has recently attracted much attention due to its potent antitumor *** to reports in the literature,some novel 14-O-derivatives of oridonin showed excellent antitumor activities against several human cancer cell lines in vitro and in *** this study,five series of 14-O-derivatives of natural oridonin were designed,synthesized,and evaluated for anticancer *** of the derivatives were significantly more potent than oridonin against HCT116,Bel7402,MCF-7 cancer *** most potent compound,D6,was 50-fold more efficacious than oridonin in HCT116 cancer ***,compound D6 has been demonstrated to significantly induce apoptosis and affect cell cycle progression in human hepatoma HCT116 cells.

关键词： Oridonin Apoptosis Antitumor Synthesis

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A novel ruthenium(Ⅱ) complex inhibiting the formation of invadopodia of MDA-MB-231 cells and angiogenesis through DNA-damaged apoptosis

A novel ruthenium(Ⅱ) complex inhibiting the formation of in...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xuanhao Zhao Li Li Jieqiong Cao Yumei Li Qiong Wu Wenjie Mei School of Pharmacy Guangdong Pharmaceutical University School of Chemistry Jinan University

Ru（Ⅱ） complexes have long been extensively studied as potential inhibitors against the proliferation and migration of tumor ***,a polypyridine ruthenium（Ⅱ） complexes have been ***'s results that compound exhibited promising observably inhibitory activity against the growth of MDA-MB-231 breast cancer *** further studies showed that compound can inhibit the migration and invasion of MDA-MB-231 cells,as well as the formation of angiogenesis in ***,it's revealed that compound can inhibit the formation of invadopodia of MDA-MB-231 cells through apoptosis via DNA-damage ***,In the tumor zebrafish model,the compounds significantly inhibited the metastasis of MDA-MB-231 cells in *** summary,compound may be developed as a potent anticancer in the near future.

关键词： Ruthenium complex Migration Invadopodia Angiogenesis DNA damage

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