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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）"

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Synthesis,crystal structure and antitumor activity of with ferrocene-amine hybrids and its rare earth complexes

Synthesis,crystal structure and antitumor activity of with f...

引用

第11届世界华人药物化学研讨会（iscmc 2018）

作者： Han Cheng Zhenfeng Chen Lanshan Liao Zuyu Mo Qiyuan Yang Delin Lai State Key Laboratory Cultivation Base for the Chemistry and Molecular Engineering of Medicinal Resources School of Chemistry & Pharmacy of Guangxi Normal University

Ferrocenyl Schiff bases were synthesized with ferrocenecarboxaldehyde and reducted to secondary amines as *** earth complexes synthesized with these ligands have been characterized by ESI-MS,single-crystal X-ray dif&action *** cellular level,antitumor activity of the ligands and its complexes has been examined by MTT assay and flow *** molecular level,the interaction of complexes with DNA were investigated by UV-vis,fluorescence,CD spectroscopy,viscosity and agraose gel electrophoresis.

关键词： Ferrocene Antitumor Activity Rare Earth Complexes

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Discovery of novel endothelial lipase inhibitors by virtual screening

Discovery of novel endothelial lipase inhibitors by virtual ...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Qirui Chen Lan Jiang Zhenming Liu Liangren Zhang State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking University

Endothelial lipase（EL） plays a central role in the negative regulation of high-density lipoprotein（HDL） particles,which makes it a potential target for raising plasma HDLc in the treatment of atherosclerosis.. Due to the lack of EL crystal *** group constructed its structure by homology modeling previously. Then,we conducted docking-based virtual screening combined with structure-based pharmacophore models to identify novel scaffolds of EL *** hits were identified in the enzyme assay and the most active compound,N35,showed an IC equal to 6 μ***,two-dimensional similarity search was performed to find their derivatives,which would be useful for further optimization of these drug candidates.

关键词： Endothelial Lipase High-Density Lipoprotein(HDL) Cholesterol Atherosclerosis Virtual Screening

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Discovery of bioactive molecules via a privileged scaffold repositioning approach

Discovery of bioactive molecules via a privileged scaffold r...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Peng Zhan Dongwei Kang Ping Gao Lin Sun Xinyong Liu Department of Medicinal Chemistry Key Laboratory of Chemical BiologyMinistry of EducationSchool of Pharmaceutical SciencesShandong University

The "privileged structure"-guided scaffold repositioning is a primary strategy to identify structurally novel chemotypes by modifying the central core structure and the side-chain of the existing active compounds,or to exploit undescribed bioactivites by making full use of readily derivatized motifs with well-established synthetic ***,we report the discovery of antiviral agents(targeting HTV-1 reverse transcriptase-associated ribonuclease H and integrase) and anti-gout agents via'privileged scaffold' repositioning *** also discuss the basic tricks of exploiting privileged structures for scaffold repositioning.

关键词： Drug design Privileged structure Antiviral agents Anti-gout agents Scaffold repositioning

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Synthesis of imidazolephenanthrolinederivates as potential inhibitor against the proliferation of HepG2 cells through inhibiting the formation of neovascularization and inducing apoptosis via DNA-damage

Synthesis of imidazolephenanthrolinederivates as potential i...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Jieqiong Cao Li Li Bowen Lian Qiong Wu Wenjie Zheng Wenjie Mei College of pharmacy Jinan University

A series of phenanthroimidazolederivates have been synthesized under microwave irradiationgive yields>90%.Compound 2 exhibit promising activityagainst the growth of HepG2 with the IC of 0.68.μ*** further studies show that 2 can decrease the mitochondrial membrane potential,DNA damage and ***,it's also discovered that 2 can inhibit the formation of neovascularization through zebrafishand tube formation ***,in vivo distribution and metabolism studies show that 2 can rapidly distributed in whole body and accumulated in tumor tissue of balb/c mice.

关键词： phenanthroimidazolederivates anti-angiogenesis DNA damage apoptosis

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Design and synthesis of 15β,16β-methylene steroid-2-benzylidene-4,6-diene-3,17-dione derivatives

Design and synthesis of 15β,16β-methylene steroid-2-benzyl...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Li Zhu Xue An Peipei Gao Lihong Shan Hongmin Liu School of Pharmaceutical Sciences Zhengzhou University

Steroids heterocyclic compounds formed by the fusion of A rings or D rings with heterocycles usually have good biological activities,and they have received extensive attention from pharmaceutical *** dehydroepiandrosterone as the staring material,we have synthesized a series of 15β,16β-methylene steroid-2-benzylidene-4,6-diene-3,17-dione *** reaction process is shown in Scheme *** the final structures are first reported and identified by NMR spectroscopys,and the yields of these products are moderate to good and the reaction conditions are *** in vitro cytotoxicity of this novel derivatives are undergoing.

关键词： Dehydroepiandrosterone Fusarium oxysporum Microbial transformation Claisen-Schmidt

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

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

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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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Cholesterol-modified caged sirnas for photoregulating exogenous and endogenous gene expression

Cholesterol-modified caged sirnas for photoregulating exogen...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Changmai Chen Jiali Yang Xinjing Tang State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking University

siRNA has been widely applied in research and drug development due to its sequence-specific gene silencing ***,how to spatiotemporally control its function is still one of its ***,a fast and noninvasive trigger,is a promising tool for spatiotemporal control of gene ***,we designed and synthesized a new series of caged siKNAs modified with single cholesterol at the 5' terminal of antisense strand RNA through a photolabile linker（Chol-PL-siRNAs）.We demonstrated that these caged siRNAs were successfully used to photochemically regulate both exogenous（firefly luciferase and GFP）and endogenous gene expression（mitotic kinesin-5,Eg5） in cells.

关键词： caged siRNA cholesterol-modification photoregulation gene expression

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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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Function-oriented synthesis of phosphatidylserine targeting drug conjugate via click chemistry

Function-oriented synthesis of phosphatidylserine targeting ...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Kuanhsun Huang Chiayu Hsu Taiyu Chiu Yuwei Liu Yunyu Chen Tengkuang Yeh Jiingjyh Jan Yuchen Huang Chenlung Huang Mingyu Fang Tsuan Hsu Chiungtong Chen Lun K.Tsou Institute of Biotechnology and Pharmaceutical Health Research Institute

Spurred by the encouraging clinical treatment of cancers with antibody drug conjugates(ADC),an emerging strategy with the use of small molecule drug conjugates(SMDC)manifests several advantageous properties,such as better in vitro and in vivo stability,lower antigenicity,facile conjugation chemistry,lower manufacturing costs,and enhanced ability to

关键词： Function-oriented synthesis of phosphatidylserine targeting drug conjugate via click chemistry

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