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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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Discovery of novel 2-amino-pyridine derivatives as potent FGFR/KDR dual inhibitors

Discovery of novel 2-amino-pyridine derivatives as potent FG...

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第11届世界华人药物化学研讨会（iscmc2018）

作者： Li Xing Xia Peng Manman Wei Yang Dai Meiyu Geng Ao Zhang Jing Ai Zilan Song CAS Key Laboratory of Receptor Research and the State Key Laboratory for Drug Research Shanghai Institute of Materia MedicaChinese Academy of Sciences Division of Anti-tumor Pharmacology State Key Laboratory for Drug ResearchShanghai Institute of Materia Medica(SIMM)Chinese Academy of Sciences

VEGF and FGF are major players of tumor angiogenesis and the synergistic effects of FGF and VEGF have been reported in preclinical studies1’*** on this,stating from the molecular docking study of FGFR1 with phase II clinical FGFR inhibitor Lucitanib,a series of novel 2-amino-pyridine derivatives was designed by quinolone ring-opening coupled with introducing flexible chain from *** 55-2 exhibited equally high potency against FGFR 1/2 and KDR with IC less than 5 *** antiproliferative effects against FGFR 1/2 and KDR addictive cancer cells were ***,compound 55-2 showed significant inhibition of tumor growth in a SNU-16 nude mouse xenograft model with14.9%oral *** work may provide a promising basis for the discovery of clinical agents that target FGFR and KDR.

关键词： FGFR KDR inhibitors 2-amino-pyridine derivatives

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Discovery of a second generation FBPase inhibitor,MB07803,with improved oral bioavailability and potential for eliminating DDI with metformin

Discovery of a second generation FBPase inhibitor,MB07803,wi...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Max(Qun) Dang Global BD and External Innovation Qilu Pharmaceutical

MB06322(CS-917,a prodrug of FBPase inhibitor MB05032) significantly lowered fasting plasma glucose levels in patients with type 2 diabetes(T2DM) during two phase 2a clinical *** 2nd-generation program sought to improve a number of properties of MB06322including oral bioavailability and efficient conversion of the prodrug to the active phosphonic

关键词： DDI Discovery of a second generation FBPase inhibitor,MB07803,with improved oral bioavailability and potential for eliminating DDI with metformin

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Formal synthesis of an antitumor antibiotic,fostriecin

Formal synthesis of an antitumor antibiotic,fostriecin

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Moran Sun Hua Yang School of Pharmaceutical Science Zhengzhou University Collaborative Innovation Center of New Drug Research and Safety Evaluation

The Formal synthesis of an antitumor antibiotic,fostriecin,via a highly convergent route is described.A characteristic feature of the present synthesis is that the synthesis was achieved via a coupling procedure of three segments A,B,and *** segment A,a α,β,-unsaturated 8-lactone was constructed via a coupling,iodolactonization and dehydration *** segment B,with chiral tertiary and secondary alcohols,was prepared via[2,3]-Meisenheimer rearrangement,epoxidation and epoxy-ring *** two segments were coupled using the Julia-Kocienski olefination.

关键词： Fostricein [2,3]-Meisenheimer rearrangement Julia-Kocienski olefination

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Regioselective synthesis of pyranone-fused indazoles via reductive cyclization and alkyne insertion

Regioselective synthesis of pyranone-fused indazoles via red...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Tzyi Wu Sandip Dhole Manikandan Selvaraju Chungming Sun Department of Applied Chemistry Chiao-Tung University Department of Medicinal and Applied Chemistry Kaohsiung Medical University

A novel and efficient method for the one-pot synthesis of 2 H-indazole from readily available building blocks is *** reaction of 2-nitrobenzylamines with zinc and ammonium formate underwent partial reduction to nitroso benzylamine followed by an intramolecular cyclization to afford 2 H-indazole via N-N bond *** carboxylic acid moiety of indazole was proceeded to regioselective alkyne insertion under ruthenium catalysis to form pyranone-fused *** regioselectivity is influenced by the weak co-ordination of indazole ring nitrogen to the metal center.

关键词： Indazole Reductive cyclization Ru-catalyst Acid-alkyne insertion

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Design,synthhesis,biological and physicochemical evaluation of selective S1P1 agonists

Design,synthhesis,biological and physicochemical evaluation ...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xiaojian Wang Yonghui Chen Tianqi Liu Qiumu Xi Wenqaing Jia Dali Yin Institute of Materia Medica Peking Union Medical College and Chinese Academy of Medical Sciences

The Spingosine-1-phosphate receptor 1(S1P1) has been proven to be a potential target for autoimmune ***720 the represented 2-aminopropane-1,3-diol agent has been approved for the treatment of relapsing remitting multiple sclerosis(MS).The clinical efficacy of FTY720 and the understanding of what cause its side effects have initiate intensive efforts toward the discovery of

关键词： Design,synthhesis,biological and physicochemical evaluation of selective S1P1 agonists

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Synthesis,cytotoxicity and mechanism of biological action of aza-crown ether-squaramide conjugates as anion/cation symporters

Synthesis,cytotoxicity and mechanism of biological action of...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xiaoqiao Hong Xiongjie Cai Xihui Yu Wenhua Chen School of Pharmaceutical Sciences Southern Medical University

It is reported that transmembrane anion/cation symport can induce cell death by disrupting the ionic homeostasis of cells. Herein,we designed and synthesized aza-crown ether-squaramide conjugates and studied their anion/cation symport properties and anti-tumor activity（Fig.1）.The results indicate that these conjugates exhibit potent liposomal and in vitro anion/cation symport,and are able to trigger cell apoptosis by modifying the intracellular pH,inducing the basification of acidic organelles in live cells and facilitating the influx of chloride and sodium ions into cells.

关键词： anion/cation symport aza-crown ether squaramide anion transport apoptosis

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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...

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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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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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A photochemical avenue to photoluminescent N-dots and their upconversion cell imaging

A photochemical avenue to photoluminescent N-dots and their ...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Qingqing Jin Amu Gubu Xiuxian Chen Xinjing Tang State Key Laboratory of Natural and Biomimetic Drugs the School of Pharmaceutical SciencesPeking University

A photochemical avenue to synthesize nitrogen-rich quantum dots（N-dots） using 2-azido imidazole as the starting material was established for the first time[1,2].A production yield of up to 92.7%was *** N-dots were then fully characterized by elemental analysis,IR,XPS,XRD,AFM and *** the basis of the N production and in situ IR results,the underlying mechanism for the photochemical formation of N-dots was *** N-dots showed promising optical properties including wavelength-dependent upconversion photoluminescence,and were successfully used in upconversion cell imaging[3].

关键词： bioimaging upconversion photoluminescence quantum dots N-dots

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Synthesis of bionic insecticides from brefeldin A and biological evaluation

Synthesis of bionic insecticides from brefeldin A and biolog...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Haoda Lyu Yongnan Xu Dahong Li Key Laboratory of Structure-Based Drug Design & Discovery Ministry of EducationShenyang Pharmaceutical University

Brefeldin A is a macrolide antibiotic synthesized by fungi that inhibits protein transportation from the endoplasmic reticulum to the Golgi apparatus by blocking the formation of COPII envelope *** A displays anti-fungal,anti-viral and anti-mitotic *** is also widely used in bio-signaling *** to unique location,novel structure and non-interaction with other traditional insecticides,the inhibitors of uridin receptors have attracted researchers' *** to the principle of drug combination,we spliced the pharmacophore of the uridin receptor pesticide and the protein transport inhibitor brefeldin A to obtain a series of biomimic insecticides and studied the biological activity,structure-activity relationship and the target of action.

关键词： Brefeldin A Uridin receptors Drug combination Biomimic insecticides

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