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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91-100 订阅

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Hydantoins as lymphoid-specific tyrosine phosphatase(LYP) allosteric inhibitor

Hydantoins as lymphoid-specific tyrosine phosphatase(LYP) al...

引用

第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xiao Liang Hao Fang Department of Medicinal Chemistry School of PharmacyShandong University

Lymphoid-specific tyrosine phosphatase（LYP）,as a member of lymphoid tyrosine phosphatase（PTPs） family,encoded by PTPN22,becomes a hit target for panel autoimmune disease *** find allosteric inhibitor NCl,which can lock the catalytic WPD-loop and targeting a LYP-specific insert,showing the non-competitive inhibiting pattern compared to other traditional LYP inhibitor because WPD-Loop in LYP is unique within PTPs family and its conformation change influents the dephosphorylation activity of *** on the structual biology results,further structual modification were performed and a series of hydantoin compounds were synthesized.

关键词： PTP LYP allosteric inhibitor

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Design and synthesis of new monoamine oxidase A inhibitor-heptamethine indocyanine dyes conjugates as target anti-tumor agents

Design and synthesis of new monoamine oxidase A inhibitor-he...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xiaoguang Yang Chun Guo School of Pharmaceutical Engineering Shenyang Pharmaceutical University

Studies have shown that high level of monoamine oxidase A（MAOA） which commonly used to treat neurological conditions such as depression promoted growth of high grade prostate cancer（PCa） progression,and the inhibitor of MAOA,such as clorgyline,induced apoptosis of cancer cells in PCa *** findings suggest that antidepressant drugs that target MAOA may have applications in treating prostate *** we developed conjugates that combine a series of novel near-infrared（NIR） heptamethine indocyanine dyes for tumor targeting with the MAOA inhibitor isoniazide（INH）.The results showed that some of them possessed prominent anti-tumor activity in PC3 ***,the combination of NIR dye specifically targeted tumor and MAOA inhibitor INH is an useful strategy and warrant further investigation.

关键词： monoamine oxidase A prostate cancer heptamethine indocyanine dyes isoniazide

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Total synthesis and SAR studies of biologically active natural products

Total synthesis and SAR studies of biologically active natur...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Yun He Chongqing Key Laboratory of Natural Product Synthesis and Drug Research School of Pharmaceutical SciencesChongqing University

Natural products are the sources of drug *** than half of the approved drugs are natural products,natural product mimics,or natural product inspired *** our efforts to discover novel agents to treat resistant bacterial infections or cancers,we have been focusing on the total synthesis and SAR studies of biological active natural products,including aetheramide,dictyodendrins,nannocystin,scrabrosins and ***,we have completed the first total synthesis of albomycins,natural antibiotics initially isolated in *** the three natural albomycins,82 exhibited low nanomolar antibacterial activities against both G-positive and G-negative *** 82 showed excellent safety profile in cells and animals,and is a promising lead for developing novel *** synthesis and SAR studies on albomycins and other naturals products in our laboratory shall be reported.

关键词： Antibiotics albomycins antibacterial resistance(AMR) structure-activity relationships(SAR)

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Synthesis and antiproliferative activity evaluation of novel chalcone-1,2,3-triazole derivatives

Synthesis and antiproliferative activity evaluation of novel...

引用

第11届世界华人药物化学研讨会（iscmc 2018）

作者： Jiajia Yang Dongjun Fu Yuyang Wang Yanbing Zhang New Drug Research and Development Center School of Pharmaceutical SciencesZhengzhou University

Chalcones have a wide range of biological activities such as anti-tumor,anti-virus,anti-oxidation and so *** novel chalcone compound（1） has a tubulin inhibitory *** on compound（1）,our group has synthesized a series of novel chalcone-1,2,3-triazoIe derivatives and evaluated their antiproliferative activity against three cancer cell lines（SK-NSH,EC-109 and MGC-803）.Among all analogues,compound（2） showed the most excellent antiproliferative activity with an IC value of 1.52 μM against SK-N-SH cancer *** mechanistic studies have shown that compound（2） may induce morphological changes in SK-N-SH cancer cells by inducing apoptosis.

关键词： chalcone-1,2,3-triazole antiproliferative activity

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Design,synthesis and cytotoxicity of novel 4-substituted coumarin derivatives as antitumor agents

Design,synthesis and cytotoxicity of novel 4-substituted cou...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Ran An Zhuang Hou Yanhua Mou Chun Guo School of Pharmaceutical Engineering Shenyang Pharmaceutical University Department of Pharmacology Shenyang Pharmaceutical University

4-substituted coumarins are very effective inhibitors against tumor-associated isoforms carbonic anhydrases Ⅸ（CAIX） in the submicromolar ***,we focus on both hydrophobic and hydrophilic halves of the CA active site *** coumarin moiety will generally adopt a conformation to interact with the hydrophobic half;similarly,the triazole and the benzoyl aniline moieties will generally interact with the hydrophilic *** to this strategy,several new compounds containing 4-substituted coumarin moiety were synthesized and had moderate anticancer activity against breast MDA-MB-231 cancer cell *** all of them revealed general promotion on cytotoxicity under ***,5 e displayed the most prominent anticancer activities of this series compounds with IC value of 0.0289μ***,the results of docking analysis showed that CA Ⅸwas likely to be one of the targets.

关键词： Anticancer coumarin hypoxia

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Enmein-type 6,7-seco-ent-kaurane diterpenoids:synthetic derivatives,antitumor activity and apoptosis related mechanism

Enmein-type 6,7-seco-ent-kaurane diterpenoids:synthetic deri...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Haonan Li Dahong Li Key Laboratory of Structure-Based Drug Design & Discovery Ministry of Educationand School of Traditional Chinese Materia MedicaShenyang Pharmaceutical University

Though enmein-type 6,7-seco-ent-kaurane diterpenoids exhibited promising activities with attractive skeletons,their natural contents were limited and difficult to be isolated from natural sources in large *** solve the shortage of large-scale compounds supply,convenient and feasible methods have been established to construct the enmein-type skeleton diterpenoid from natural *** order to improve the efficacy,we synthesized several series of enmein-type diterpenoid hybrids coupled with nitrogen mustards and NO *** molecules showed improved antitumor effects and reduced systemic ***,the apoptosis related mechanisms were also ***,enmein-type diterpenoid hybrids expected to become potential chemotherapeutic agents for tumor.

关键词： enmein-type diterpenoid antitumor apoptosis

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A facile method for synthesis of 3-substituted-1-indanones via Cu-catalyzed intramolecular annulation reactions

A facile method for synthesis of 3-substituted-1-indanones v...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Guoxue He Yu Zhou Chenglin Wu Jianhui Zhou Qiaolan Yang Chunmei Zhang Huabei Zhang Hong Liu Key Laboratory of Radiopharmaceuticals of Ministry of Education College of ChemistryBeijing Normal University State key Laboratory of Drug Research and Key Laboratory of Receptor Research Shanghai Institute of Materia MedicaChinese Academy of Sciences

We report a facile method access to 1-indanones and a series of derivatives were synthesized,Cu-catalyzed intramolecular annuiation reactions starting from the corresponding 2-ethynylbenzaldehyde for the first *** protocols provided a direct,convenient and atom-economical synthetic approach to afford 1-indanones derivatives under mild conditions in good to excellent *** addition to,to form the 2-benzylidene-1 H-indenel,3(2 H)-dione by a two-step,which showed a antibacterial,antifungal,anti-inflammatory activity.

关键词： 2-ethynylbenzaldehyde Cu-catalyzed 1-indanones

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The design,synthesis and antitumor activity of novel tetrazolo[5,1-a]phthalazine derivatives

The design,synthesis and antitumor activity of novel tetrazo...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Jingchao Xin Na Li Erdong Li Yaqi,Meng Jiaxin,Zheng Qiurong Zhang Hongmin Liu Zhengzhou University School of Pharmaceutical Sciences Collaborative Innovation Center of New Drug Research and Safety Evaluation

Among a large variety of nitrogen-containing heterocyclic compounds,heterocyclic containing hydrazine has received considerable attention because of their pharmacological properties and clinical *** ring was an important bioactive core found in many agents of biological as anti-convulsive,anti-inflammatory,anti-tumor and vascular endothelial growth factor receptor（VEGFR-2） *** base fragments are also frequently used in the synthesis of anti-tumor small *** this paper,phthalic anhydride as a starting material,through cyclization,chlorination,substitution and condensation reactions to get a series of target compounds were designed and *** the compounds have been confirmed by H-NMR、C-NMR and ***,the anti-tumor activity of these compounds are being tested.

关键词： synthesis phthalazine anti-tumor

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Synthesis,crystal structure,cytotoxicity and DNA binding of Pt(Ⅱ) complex of 9-PMAH

Synthesis,crystal structure,cytotoxicity and DNA binding of ...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Ruixue Liu Delin Lai Mengxin Yu Yingshu Wu Yancheng Liu Hong Liang State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources School of Chemistry & Pharmaceutical SciencesGuangxi Normal University

A new Pt(II) complex of 9-PMAH was synthesized and fully characterized by IR,elemental analysis,ESI-MS and single-crystal X-ray diffraction *** bioactivity experiment was demonstrated by DNA binding and anticancer activity,*** DNA binding study showed that the Pt(II) complex interacted with ct-DNA mainly via an intercalative binding mode,which was confirmed by the fluorescence spectral analysis and agarose gel *** in vitro cytotoxicity of the Pt(II) complex was higher than 9-PMAH,but some lower than cisplatin against most tumor cell lines,in which MGC-803 was the most sensitive tumor cell line,with IC50 value of 9.15 0.83 uM.

关键词： anthrahydrazone metal complex antitumor activity DNA binding

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Therapeutic challenges and opportunities on molecular-targeted drug discovery

Therapeutic challenges and opportunities on molecular-target...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Wenshan Li Institute of Chemistry “Academia Sinica” Doctoral Degree Program in Marine Biotechnology Sun Yat-Sen University Biotechnology Research and Development Taipei Medical University Department of Medicinal and Applied Chemistry Kaohsiung Medical University

Human diseases involve an abnormal condition of a part,organ,or system of an organism resulting from various causes,such as tropical infection,chemoresistance,or cancers,and characterized by an identifiable group of signs and *** the present study,we describe the discovery and synthesis of potent inhibitors of SjGST capable of occupying the active site of the enzyme by a structure-based drug design *** is one of the most frequent and lethal diseases that terribly threaten human's *** mortality of the majority cancer patients（> 90%） is due to the occurrence of metastasis rather than their primary ***,the development of therapeutic agents that inhibit tumor metastasis is highly *** of effective antimetastatic agents for clinical use based on the ST inhibitor design is addressed in this investigation.

关键词： Cancer Chemoresistance Metastasis Molecular-targeted drug discovery Tropical infection

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