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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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Chemical approaches to challenging drug delivery problems:from gasotransmitters to antibody-drug conjugates

Chemical approaches to challenging drug delivery problems:fr...

引用

第11届世界华人药物化学研讨会（iscmc 2018）

作者： Binghe Wang Department of Chemistry and Center for Diagnostics and Therapeutics Georgia State University

Prodrug approaches are often used to solve drug delivery *** doing so,the chemistry needed to bioreversibly derivatize the drug molecule is the *** this line,bioreversible derivatization of gasotransmitters such as nitric oxide,hydrogen sulfide and carbon monoxide are especially ***,the chemistry used to prepare antibody-drug conjugates also has much room for *** presentation will discuss some unique chemistry developed for the preparation of prodrugs of carbon monoxide and hydrogen sulfide as well as a new approach to prodrug activation through enrichment.

关键词： gasotransmitter antibody-drug conjugates carbon monoxide hydrogen sulfide

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Discovery of novel guinazoline-derived JAK inhibitors

Discovery of novel guinazoline-derived JAK inhibitors

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xu Bai The Center for Combinatorial Chemistry and Drug Discovery The School of Pharmaceutical SciencesJilin University

The first-generation JAK inhibitors Tofacitinib and Ruxolitinib are considered as promising therapeutics for the treatment of RA or ***,their side effects such as anemia limited their use possibly due to low selectivity of the drugs（dose-limiting） .Selective inhibition of JAK kinases within the JAK family may lead to maximum efficacy with minimized undesired off-target effects and to understanding the role of individual JAK isoforms in disease. We have discovered a class of novel,quinazoline derivatives as potent and selective JAK *** of SAR studies and profiling will be discussed in details.

关键词： JAK inhibitor Quinazoline Derivatives SAR

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Rapid advances of nonsmall cell lung cancer treatment:perspectives from 2018

Rapid advances of nonsmall cell lung cancer treatment:perspe...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： James Chihhsin Yang Graduate Institute of Oncology Taiwan University College of Medicine Department of OncologyTaiwan University

Most lung cancer patients were diagnosed at advanced stage,therefore,local treatment for cure is often *** treatment is the mainstay for advanced stage nonsmall cell lung cancer ***-based chemotherapy has become standard treatment *** new chemotherapy were designed and improved treatment outcome for *** year 2000,small molecules act as targeted therapy has changed the treatment paradigm

关键词： NSCLC Rapid advances of nonsmall cell lung cancer treatment:perspectives from 2018

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Gossypol schiff bases with hydrophobic effects providing enhanced anti-tumor activities

Gossypol schiff bases with hydrophobic effects providing enh...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Wei Wang Yuzhi Lu Haibing Zhou Wuhan University School of Pharmaceutical Sciences

A series of novel gossypol Schiff bases were identified much potent(10-100 fold) than the gossypol and its known Schiff base derivatives for the anticancer activity.[1]This is the first example for Gossypol Schiff bases with the increased activity.[2]The investigation of the Schiff base side chain of gossypol revealed the unique anticancer effect was achieved by the introduced hydrophobic ester *** molecular modeling analysis demonstrated the possible binding mode of these compounds with the Bcl-2,which could explain the good binding affinity of these novel gossypol Schiff bases with the proteins.

关键词： gossypol anticancer Schiff bases

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A fluorescent HDAC6 Selective inhibitor capable of imaging aggresome

A fluorescent HDAC6 Selective inhibitor capable of imaging a...

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第11届世界华人药物化学研讨会（iscmc2018）

作者： Yingjie Zhang Jin Yan Tsopang Yao Department of Medicinal Chemistry School of Pharmaceutical of ScienceShandong University Department of Pharmacology and Cancer Biology Duke University

There is increasing interest in discovering HDAC6 selective inhibitors as chemical probes to elucidate the biological functions of HDAC6 and ultimately as new therapeutic ***-molecular fluorescent probes are widely used to detect target protein location and function,identify protein complex composition in biological processes of *** the present study,structural modification of the previously reported compound 4 MS leads to two novel fluorescent HDAC inhibitors,6 a and 6 b(Figure 1 A).Determination of IC values against the panel of Zn dependent HDACs(HDACl-11) reveals that 6 b is a HDAC6 selective inhibitor,which can induce hyperacetylation of tubulin but not histone ***,fluorescent and immunofluorescent analyses of cells treated with the proteasome inhibitor MG132 demonstrates that 6 b can selectively target and image HDAC6 within the inclusion body,the aggresome(Figure IB).These results identify 6 b not only as a HDAC6 selective inhibitor but also as a fluorescent probe for imaging HDAC6 and investigating the roles of HDAC6 in various physiological and pathological contexts.

关键词： HDAC6 Fluorescent probe Inhibitor Aggresomes

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Synthesis and biological evaluation of chromone derivatives

Synthesis and biological evaluation of chromone derivatives

引用

第11届世界华人药物化学研讨会（iscmc 2018）

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

Chromones,which universally exist in nature,exhibit various pharmacological activities,such as antitumor,anti-inflammatory,antioxidant,cardioprotective,anti-HIV and antimicrobial *** were also favored due to low mammalian toxicity,which attracted many researchers' interest for structural modification of *** oxide has great potential in inhibiting carcinogenesis and tumor ***,due to its instability and short half-life,it is not really *** predicament inspired us to design and synthesize a series of chromones derivatives bearing nitric oxide *** biological activities of this series of compounds are under evaluation.

关键词： Chromones Nitric oxide Antitumor

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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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Synthesis and anticoagulation studies of fucosylated chondroitin sulfate oligosaccharides

Synthesis and anticoagulation studies of fucosylated chondro...

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第11届世界华人药物化学研讨会（iscmc2018）

作者： Xiao Zhang Huiying Liu Wang Yao Mingyi Wu Zhongjun Li State Key Laboratory of Natural and Biomimetic Drugs Department of Chemical BiologySchool of Pharmaceutical SciencesPeking University State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of BotanyChinese Academy of Sciences

Thrombotic disease is one of the most serious threats to human ***,available antithrombotic drugs have a common side effect:the risk of bleeding during *** show that selective inhibition of the intrinsic coagulation pathway may distinguish thrombosis from hemostasis ,offering promise *** development of safer anticoagulants without serious bleeding *** chondroitin sulfate(FuCS) is a structurally distinct glycosaminoglycan with excellent anticoagulant *** studies showed that FuCS and its depolymerized fragments selectively inhibited the intrinsic coagulation pathway,and nonasacchande was the minimum structural unit that retained the potent activity .To achieve a large-scale preparation and explore further optimization,here we report a facile method for the synthesis of structurally homogeneous FuCS hexa-and nonasacchande for the first time over 12 linear steps from commercially available chondroitin *** studies showed that the synthetic nonasacchande displayed promising APTT activity and strong FXase inhibition activity,which may promote the discovery of novel anticoagulant candidates.

关键词： fucosylated chondroitin sulfate anticoagulant drug discovery

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Boron-containing compounds in drug discovery and chemical biology

Boron-containing compounds in drug discovery and chemical bi...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Jiong Zhang Jinyi Zhang Long Ye Dazhong Ding Huchen Zhou School of Pharmacy Shanghai Jiao Tong University

An interesting class of cyclic boron-containing compounds,benzoxaboroles,were first synthesized in 1957 while its medicinal usage had remained unknown for fifty years until tavaborole（Kerydin） was approved in 2014 for the treatment of fungal infection of the toenails. To date,benzoxaboroles have been investigated for their antifungal,antibacterial,anti-parasite,antiviral,and anti-inflammatory properties. However,an investigation of their anticancer activity has been *** this talk,I will discuss our recent work on the anticancer activity and mechanism of action study of a series of interesting benzoxaboroles.

关键词： Boron drug discovery anticancer

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Synthesis of glycosidic switch cytotoxic drugs for nanoliposomal delivery to cancer cells

Synthesis of glycosidic switch cytotoxic drugs for nanolipos...

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第11届世界华人药物化学研讨会（iscmc2018）

作者： Pierrealain Burnouf Yulin Leu Yucheng Su Kenneth Wu Weichi Lin Steve Roffler Department of Pharmacy Chia Nan University of Pharmacy ＆ Science

Liposomes provide stable encapsulation and local tumor-specific release for cancer therapy based on enhanced permeability and retention effects to increase therapy outcome and reduce side effect of antitumor ***,the encapsulation efficiency and stable retention of drugs in liposomes is drug dependent Many potent antitumor drags are difficult to encapsulate and retain in liposomes,thus causing side effect and decreasing the dose of drugs at tumor ***,we propose a glycosidic switch technology to adjust lipid/water solubility of drugs to increase drug loading and stability within *** strategy is to conjugate drugs with a methyl glucuronide via a self—immolative linker to generate a lipid soluble methyl drug glucoronate（Drug-GL） that can directly pass through the lipid bilayer of *** Drug-GL then is converted to water-soluble drug glucuronide（Drug-Gw） via spontaneous saponification within liposomes that increase drug retention and *** extend this concept to create highly potent anticancer agents,we synthesis of the glycosidic switch analog of *** is suitable for an extensive range of drugs and provides a new method to improve the loading and retention of drugs in liposome to increase accumulation of anticancer drugs at target cancer cells and produce greater cytotoxicity for improved therapeutic outcome.

关键词： Liposomes glucuronide

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