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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（ISCMC 2018）"

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Exploration of farnesoid X receptor ligands based on a library of oleanolic acid A-and C-ring modifications

Exploration of farnesoid X receptor ligands based on a libra...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Weishuo Fang State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences & Peking Union Medical College

The pentacyclic triterpene oleanolic acid(OA) with known famesoid X receptor(FXR)modulatory activity was modified at A-ring(C-3) and C-ring(C-12) positions to find new FXR-interacting *** agonist-and antagonist-based ligand-FXR binding models were established to assist the design of structural modifications at both sites on A-and *** potent antagonists were found,in addition to a few weak to moderate agonists and compounds with coactivation effects with CDCA,the internal FXR agonist in luciferase-based cell *** vivo PD and PK assessment are in progress.

关键词： farnesoid X receptor FXR triterpene oleanolic acid

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Synthesis,characterization and DNA-binding properties of Ru(Ⅱ) complexes as potential antitumor agents

Synthesis,characterization and DNA-binding properties of Ru(...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xukui Liu Xuanhao Zhao Yumei Li Yin Feng Kangdi Zheng Qiong Wu Wenjie Mei School of Pharmacy Guangdong Pharmaceutical University The First Affiliation Hospital Guangdong Pharmaceutical University Guangdong Province Engineering Technology Centre for Molecular Probe and Biomedicine Imaging

Three ruthenium（Ⅱ） complexes have been synthesized and characterized with electronic absorption and emission spectra. It's found that these complexes can inhibit the growth of human A549 lung cell ***,these three complexes exhibited excellent binding affinities with DNA,as confirmed by spectroscopy,viscosity experiments and agarose gel electrophoresis. Therefore,this result show that the synthesized ruthenium（Ⅱ）complexes have excellent DNA-binding abilities and antitumor properties with potential applications in cancer chemotherapy.

关键词： Ru(Ⅱ) complexes Antitumor DNA-binding

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Cyclization strategy in medicinal chemistry:a way to discovery of potent and selective BTK inhibitors

Cyclization strategy in medicinal chemistry:a way to discove...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Yu Xue Zilan Song Ao Zhang CAS Key Laboratory of Receptor Research and the State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences College of Pharmacy University of Chinese Academy of Sciences School of Life Science and Technology ShanghaiTech University

Rational structural optimization is a key to tailor the druglike properties of a lead compound and come up with a well-balanced developable candidate.A good draggable chemotype is generally surrounded by a larger number of patents,therefore a unique approach is necessary to avoid the reported intellectual property and gain a new patentable *** have used a cyclization strategy to form new ring systems either from the core templates or from the

关键词： BTK Cyclization strategy in medicinal chemistry:a way to discovery of potent and selective BTK inhibitors

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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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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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Small molecule drug conjugates for anti-colorectal cancer

Small molecule drug conjugates for anti-colorectal cancer

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Chunkai Chang Peifang,Chiu Huiyi Yang Pihui Liang School of Pharmacy Taiwan University The Genomics Research Center “Academia Sinica”

Sodium-dependent glucose cotransporterl(SGLT1) and glucose transporter(GLUT) are abnormally expressed in colorectal cancer *** of glucose uptake in cancer cells causes the resistance of genotoxic *** suggests that blocking glucose uptake has the potential to increase the efficacy of anti-cancer *** this study,we focused on the small molecule drug conjugation for colorectal cancer.5-FU is a common requirement for colorectal cancer,through the combination of 5-FU and SGLT1 or GLUT inhibitors via bio-reductive linker,the efficacy of new conjugates were *** study will assess the results of in vitro study before entering animal experiments.

关键词： 5-FU glucose transporter anti-colorectal cancer

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Preparation of crystal polymorphs of tetracaine hydrochloride

Preparation of crystal polymorphs of tetracaine hydrochlorid...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Shasha Li Shanshan Guo Jie Zhao Yuanmin Din Wen Li School of Chemical Engingeering and Energy Zhengzhou University School of Pharmaceutical Sciences Zhengzhou University Key Laboratory of Technology of Drug Preparation(Zhengzhou University) Ministry of EducationCollaborative Innovation Center of New Drug Research and Safety EvaluationHenan Province& Key Laboratory of Henan Province for Drug Quality and Evaluation

Tetracaine hydrochloride(Fig.1) is a local anesthetic drug widely used in epidural blocks,subarachnoid blocks,nerve conduction blocks,and mucosal surface anesthesia.11"21Through experimentation,we found mat tetracaine hydrochloride could exist in three forms at ambient temperature,denoted forms *** I is the commercial crystal form with a melting point range of 413.15-423.15 *** II was obtained by reciystallization from form I in

关键词： Preparation of crystal polymorphs of tetracaine hydrochloride

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Synthesis of Rhodamine B-based pentacyclic triterpene probe for studying the interaction of influenza virus and host cells

Synthesis of Rhodamine B-based pentacyclic triterpene probe ...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Man Li Qianqian Gao Demin Zhou Sulong Xiao State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking University

Pentacyclic triterpene derivatives possess a variety of biological *** recent works on the anti-influenza virus activities of pentacyclic triterpenes together with published reports lead us to further investigate their antiviral *** this study,several fluorescent probes based on Rhodamine B and pentacyclic triterpenes were synthesized and *** showed moderate anti-influenza activity with IC50 values of 3.41-14.27 *** antiviral mechanism was carried out by time of addition,hemagglutination inhibition,surface plasmon resonance,flow cytometry and confocal laser microscopy assays.

关键词： Rhodamine B betulinic acid influenza

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A role of targeting the Skp1-Cullin1-Skp2 complex through regulation of protein neddylation in prostate cancer treatment and prevention

A role of targeting the Skp1-Cullin1-Skp2 complex through re...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xiaolin Zi Departments of Urology and Pharmacology and Chao Family Comprehensive Center University of California

The S-phase kinase-associated protein 2(Skp2) is overexpressed in prostate cancer and associated with tumour stage,disease recurrence,and worse patient *** also have demonstrated that Skp2 overexpression plays a critical role in development and progression of prostate cancer in several prostate cancer models,including PTEN knockout

关键词： A role of targeting the Skp1-Cullin1-Skp2 complex through regulation of protein neddylation in prostate cancer treatment and prevention

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