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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81-90 订阅

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Bioactivity of novel dihydroartemisinin-coumarin hybrids

Bioactivity of novel dihydroartemisinin-coumarin hybrids

引用

第11届世界华人药物化学研讨会（iscmc 2018）

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

In order to develop novel agents with potent anticancer activities,we designed dihydro-artemisinin-coumarin hydrids（DCH） in our previous *** found that those compounds had moderate anticancer activity against three cancer cell lines（HCT-116,MDA-MB-231 and HT-29）.The mechanism of the anticancer activity of DCH also be *** could inhibited proliferation of HT-29 cell lines,arrested HT-29 G/G phase and induce both apoptosis and ferroptosis of HT-29 cell ***,DCH had been found to be a potential anti-Alzheimer's *** compound A could induced N9 cell death and the inhibition ratio could even up to 31.25%（10μM）.

关键词： anticancer neuroinflammation artemisnin coumarin hybrid

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Caged siRNAs with single folic acid modification for photoregulation of exogenous and endogenous gene expression in cells

Caged siRNAs with single folic acid modification for photore...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Lijia Yu Nannan Jing Xinjing Tang State key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking University

Manually controlling siRNA activity is an essentially important way to spatiotemporally investigate gene evaluation and *** to the easy operation and precise manipulation,light could be used to regulate siRNAs induced gene silencing in controllable ***,we developed a series of caged siRNAs with folic acid modification at 5' terminus of antisense strand of siRNA through a photolabile *** attachment of folic acid temporally masked the siRNA activity. Upon light illumination,the caged siRNAs were activated,and siRNA gene silencing activity was *** on this strategy,we successfully photomodulated gene expression of both exogeneous gene（green fluorescence protein,GFP）and endogenous gene（mototic kinesin-5,EgS） in cells.

关键词： photoregulation caged oligonucleotides siRNAs gene expression folic acid modification

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Synthesis and biological evaluation of H2S releasing hybrids based on natural oridonin

Synthesis and biological evaluation of H2S releasing hybrids...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xiang Gao Xu Hu Huiming Hua Dahong Li Key Laboratory of Structure-Based Drug Design & Discovery Ministry of Educationand School of Traditional Chinese Materia MedicaShenyang Pharmaceutical University

Hydrogen sulfide（H S）,an important gasotransmitter,mediated several physiological conditions including cardiovascular problems and anticancer *** various pathway and underlining mechanism which exerted by H S donors remained the interest of ***,a series of novel H S releasing hybrids based on natural product oridonin were designed and synthesized for H S releasing ability and antitumor activity *** therapeutic efficacy and selectivity were observed,while further mechanism studies concerning H S mediated antiproliferative pathway were *** results warranted future exploration of H S donor molecules coupled with known structures of natural occurring compounds to harness the full potential of these hybrid compounds.

关键词： H2S donor anticancer natural product oridonin

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Synthesis and broad-spectrum antiviral activity of some novel (5-oxazolyl)-phenylthiourea derivatives

Synthesis and broad-spectrum antiviral activity of some nove...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Zhaojin Zhong Guoling Xing Yuhuan Li Zhihui Zheng Limin Zuo Rongmei Gao Zhuorong Li Institute of Medicinal Biotechnology Chinese Academy of Medical Sciences & Peking Union Medical College

A series of novel（5-oxazolyl）-phenylthiourea derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral *** biological results showed that most of our synthesized compounds exhibited potent broad-spectrum antiviral ***,compounds 6 a(IC = 0.11-1.74 μM) and 6 b(IC = 1.26-3.28 μM) showed potent activity towards both RNA viruses（influenza A virus and coxsackievirus B3） and DNA viruses（HSV-1 and HBV） at low micromolar *** SAR study showed that for most synthesized compounds,the thiourea group was attached to the（5-oxazolyl）-phenyl group,which was favored for antiviral ***,they were IMPDH inhibitors.

关键词： (5-oxazolyl)-phenylthiourea synthesis antiviral activity IMPDH SAR

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Design,synthesis and biological evaluation of natural product guaiane-type sesquiterpenoids derivatives

Design,synthesis and biological evaluation of natural produc...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xiangwei Meng Jing Zhou Xingxian Zhang College of Pharmaceutical Sciences Zhejiang University of Technology

Guaiane-type sesquiterpenes occur widely in nature and have been isolated and identified in many different *** natural products are known for their potent bioactivities,such as anti-inflammatory,antiviral,antimicrobial,anti-tumor,antioxidant and antiprotozoal properties.A convenient method for synthesizing guaiane-type sesquiterpenes compound 2 by using compound 1 with rhodium catalyst resulted in carbonyl ylide formation from the cyclization of the carbonyl group with the electrophilic rhodium ***,we have successfully finished compound *** we will wish to design and synthesize a novel series of guaiane-type sesquiterpenes derivatives from compound *** newly synthesized compounds will be tested in vitro and the inhibition of HepG-2 cells compared to untreated control cells was *** effects of the prepared compounds on HCC cell apoptosis will be further evaluated in our lab.

关键词： Guaiane sesquiterpenes total synthesis structural modification bioactivity

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Synthesis and potential antidepressant effects study of solifenacin derivatives

Synthesis and potential antidepressant effects study of soli...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Zhiyang Fu Yuxuan Qi Yanan Xia Liping Guan Food and Pharmacy College Zhejiang Ocean University

Quinolinone compounds are generally used in medicine and in the literature due to their broad biological effects,including antidepressant and anticonvulsant *** research group has been studying with the chemical structure and biological properties of the antidepressant effect of *** found solifenacin including isoquinoline showed antidepressant activity at a dose of 100 mg/*** research attempt to find the new antidepressant and anticonvulsant compounds with improved safety profile and therapeutic potency,a series of derivatives were synthesized and evaluated for their antidepressant *** 1 and2,both with electron-withdrawing substituent o-fluoro and o-chloro for the phenly ring,compounds 3（m-CH） and 4（m-OCH） with electron-donor groups,showed the most antidepressant effects in the forced swimming test（FST）（DID:82%,81%,72.5%and72.8%,respectively） at a dose of 30 mg/kg,which was greater than that or nearly equivalent to that of fluoxetine（79%）.

关键词： Solifenacin Isoquinoline Synthesis Antidepressant

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Recent progress in terpenoid synthesis:total syntheses of caribenol A and caribenol B

Recent progress in terpenoid synthesis:total syntheses of ca...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Hongdong Hao Dirk Trauner Shaanxi Key Laboratory of Natural Products & Chemical Biology College of Chemistry & PharmacyNorthwest A&F University Department of Chemistry and Center for Integrated Protein Science Ludwig-Maximilian University Munich Department of Chemistry New York University

Several diterpenes and norditerpenes with novel carbon skeletons were isolated from the Caribbean sea plume Pseudopterogorgia,such as caribenol A,caribenol B and aberrarone（Figure 1）,they have shown biological activity against Mycobacterium tuberculosis H37 Rv and antiplasmodial *** the sponge-derived isocyanoterpenes exhibit potent antimalarial *** these terpenoid natural products became attractive targets for the synthetic community due to their intriguing biological activities as well as their unique *** program aimed at a unified synthesis of these natural product and here we present our successful approach to caribenol A,caribenol B.

关键词： marine natural product antimalarial total synthesis

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Medicinal chemistry and clinical trial of anti-cancer stem cell drug

Medicinal chemistry and clinical trial of anti-cancer stem c...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Yue Chen College of Pharmacy Nankai University

Many studies suggested that cancer stem cells play a key role in the cancer initiation,development,relapse and drug ***,calling for more anti-CSC compounds and study of their possible target are highly ***,small molecules that can selectively ablate cancer stem cells(CSCs) are very *** identified a series of sesquiterpene lactones(SLs) and APD-cyclic depsipeptides that can selectively eradicate cancer stem *** Michael adduct of MCL(ACT001) has entered Phase I clinical trail in Australia as anti-glioblastoma drug ***001 has been designated as orphan drug candidate by *** outcome of Clinical I has been presented on the ACSO meeting:"At well-tolerated doses,ACT001 showed satisfactory bioavailability and preliminary evidence of anti-tumor activity in a subset of patients."

关键词： synthesis cancer stem cell natural products

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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 and synthesis of novel Wogonin derivatives with potent antitumor activity in vitro

Discovery and synthesis of novel Wogonin derivatives with po...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者：王举波李志裕卞金磊 Department of Medicinal Chemistry China Pharmaceutical University

Phenotypic screening of high quality compound library is one of the most effective strategy to obtain novel bioactive ***,our group have constructed a Wogonin-scaffold library with substituents diversity and successfully obtained a series of potent ***,we reported the synthesis of these compounds and evaluated the in vitro antitumor activity against a panel of human tumor cell *** of them showed good activity with a broad spectrum and preliminary structure-activity relationship for the substitutions were *** biological assays showed that the most potent compounds 18 n and 20 b could significantly enhance the intracellular ROS level and induce the cell apoptosis at low micromole *** similarity searching,CDK9 was identified as the potential target for 20 b,which could be a start point for next structure-based drug design.

关键词： Wogonin SAR antitumor CDK9

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