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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Wenjie Zhai Jiangfeng Du Yahong Wu Yuanming Qi Wenshan Zhao Yanfeng Gao School of Life Sciences Zhengzhou University

Cancer immunotherapy is considered as the most promising strategy to conquer ***,we have focused on immune checkpoint blockade targeting programmed cell death 1 protein(PD-1) and other molecules,and tumor vaccines based on *** using the technology of phage display,we developed the first hydrolysis-resistant D-peptide inhibitor targeting PD-1/PD-L1,and novel peptide inhibitors targeting other checkpoint molecules as *** develop personalized tumor vaccines based on neoantigen,we constructed an antigenic peptide library to develop an algorithm for neoantigen prediction which could help the immune checkpoint *** these would serve as novel candidates and tools for cancer immunotherapy.

关键词： Cancer immunotherapy Peptide Immune checkpoint Tumor vaccine

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Synthesis of novel 3-amino substituted-andrographolide derivative

Synthesis of novel 3-amino substituted-andrographolide deriv...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Chunyang Zou Yao Wang Jie Lv Department of Pharmacy Liaoning Vocational College of Medicine

14-Deoxyandrographolide is an analogue of andrographolide and it displays certain anti-influenza virus activity in previous ***,the further structure modifications were carried out in our *** far,3-hydroxyl group of andrographolide is never deeply ***,in view that basic amino group is contributive to biological activity,we plan to substitute 3-hydroxyl group with amino *** from andrographolide,14-deoxyandrographolide 1 was prepared by Srinivas Nanduri's method.19-Hydroxyl group was selectively protected by *** 3-hydroxyl was oxidized by ***,3-carbonyl group was transformed into *** to our developed method,the isoxazole ring was constructed by use of 4-toluene sulfonyl *** the last step,the 3-amino group was released by use of *** structure was confirmed by H NMR,C NMR and HR-MS.

关键词： 3-amino substituted-andrographolide structure modification synthesis

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Structure-based discovery and optimization of new potent and selective BET inhibitors for potential treatment of heart failure

Structure-based discovery and optimization of new potent and...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Maksim Semenov Yuan Shuo Lingyu Li Bin Yu Hongmin Liu Wen Zhao Key Laboratory of Advanced Pharmaceutical Technology Ministry of Education of China Co-innovation Center of Henan Province for New drug R & D and Preclinical Safety School of Pharmaceutical Sciences Zhengzhou University

Bromodomain protein 4(BRD4) is a member of the bromodomain and extra-terminal domain(BET) protein *** binds to acetylated histone tails via its tandem bromodomains BD1 and *** essential role of BRD4 in cell proliferation and cancer growth has been reported in several recent *** studies showed that the strongest interactions took place with di-

关键词： BET Structure-based discovery and optimization of new potent and selective BET inhibitors for potential treatment of heart failure

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From AI to knowledge-based drug design:Case studies

From AI to knowledge-based drug design:Case studies

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Guosheng Wu Computational Drug Discovery Pharmaron

For over half a century,AI has been widely applied in predicting physical properties and biological activities for drug-like ***,due to the complexity for molecular especially biological systems,there are many kinds of limitations in all current computational methods,so that one could not simply utilize the results from *** order to take advantage of the high efficiency for computational methods,we will discuss how to select appropriate methods to solve specific issues such as potency,selectivity,structural novelty,solubility,metabolic stability,and so on,while also utilize available knowledge or data from different sources,such as organic synthesis,medicinal chemistry,3 D structure for target protein and SAR for small molecules from internal study or from *** goal is to help the project team identify the next a few key molecules for synthesis so that the project could be moved to the next stage quickly.

关键词： Drug design AI molecular modeling molecular structure

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第五届世界华人药物化学研讨会

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药学进展 2006年第3期30卷 F0003-F0003页

世界华人药物化学研讨会（International Symposium for Chinese Medicinal Chemists，iscmc）是面向全球从事药物化学相关工作华人的一个专业性学术活动，是全球华人在药学领域中的盛会，并已成功举办四届。活动得到了祖国两岸三地医... 详细信息

世界华人药物化学研讨会（International Symposium for Chinese Medicinal Chemists，iscmc）是面向全球从事药物化学相关工作华人的一个专业性学术活动，是全球华人在药学领域中的盛会，并已成功举办四届。活动得到了祖国两岸三地医药学领域著名学者的广泛参与，也吸引了众多来自欧美及世界各地的医药学华人专家的积极参与和支持，其规模也是逐届增大。为使全球药物化学工作者及时把握国际药物化学研发新趋势，获取国内外药物化学研发新信息，给国内外从事药物化学研发的华人专家构筑学术展示的平台和沟通的渠道，促进国际交流与合作，推动药物化学学科和医药工业的快速发展，中国药学会定于2006年11月2日至7日在古城南京举行第五届世界华人药物化学研讨会。

关键词：药物化学世界华人医药学领域 Chinese 学术活动国际交流中国药学会化学相关著名学者世界各地

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Design,synthesis and in vitro evaluation of diaryl ether derivatives as Raf/HDAC dual inhibitors

Design,synthesis and in vitro evaluation of diaryl ether der...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Yong Zhu Aixin Geng Hao Cui Hongmei Li Tao Lu Yadong Chen Department of Organic Chemistry School of ScienceChina Pharmaceutical University

Histone deacetylase（HDAC） inhibitors are known to induce multiple epigenetic modifications affecting signaling networks and act syneigistically with Raf inhibitors for the treatment of cancer. Herein we design a generation of dual Raf and HDAC inhibitors with diaryl ether scaffold. The designed compounds were synthesized which showed inhibitory activity against B-Raf and *** representative dual Raf/HDAC inhibitors,compound 7,showed potent antiproliferative activities against tumor cell lines MDA-MB-231 and MV4-11 in cellular *** work may lay the foundation for developing dual Raf/HDAC inhibitors as potential anticancer therapeutics.

关键词： Raf inhibitors HDAC inhibitors synthesis antiproliferative activity dock

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Development of carbon monoxide prodrug and its applications

Development of carbon monoxide prodrug and its applications

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Bowen Ke Binghe Wang Laboratory of Anesthesiology & Critical Care Medicine Translational Neuroscience CenterWest China HospitalSichuan University Department of Chemistry and Center for Diagnostics and Therapeutics Georgia State University

CO is as an endogenous signaling molecule, with a tremendous amount of pharmacological and mechanistic work in demonstrating CO's effect in cytoprotection, anti-inflammation,and anti-cancer. We are interested in developing organic CO-prodrugs for further therapic *** taking advantage of intramolecular Diels-Alder reaction,a prodrug strategy was developed for preparations of organic CO-prodrugs that are stable during synthesis and storage,and yet readily release CO with tunable release rates under near physiological *** effectiveness of the CO-prodrug system in delivering a sufficient quantity of CO for possible therapeutic applications has been studied using cell culture anti-inflammatory assay and animal *** study fully demonstrates the proof of concept,and lays foundation for further clinical applications of CO prodrugs.

关键词： Carbon Monoxide Prodrug Diels-Alder Reaction Therapeutic Effects

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Pharmacological validation of new kinases with small molecules

Pharmacological validation of new kinases with small molecul...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Xianming Deng State-province Joint Engineering Laboratory of Targeted Drugs from Natural Products School of Life SciencesXiamen University

Protein kinases have been a rich source of targets for drug discovery with 37 small molecules as approved ***,most academic and industrial research remains focused on only a small fraction of the kinome for which evidence of therapeutic utility already ***'s an emerging need to explore the untargeted kinome that have received scant attention. Here we presented the new strategies including "pathway-specific" screening and "compound-centric" approach that led to the discovery of first-in-class kinases MST1/2 inhibitor（XMU-MP-1） and breast tumor kinase（BRK/PTK6） inhibitor（XMU-MP-2）with in vivo *** inhibitors will serve as valuable tools to pharmacologically interrogate MST1/2 and BRK biology,and they provide a starting point for medicinal chemistry efforts aimed at developing related targeted therapeutics.

关键词： Untargeted kinome pathway-specific compound-centric first-in-class kinase inhibitors

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Efficient synthesis of novel amide-linked polysaccharides through EDCI-pyridine system

Efficient synthesis of novel amide-linked polysaccharides th...

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第11届世界华人药物化学研讨会（iscmc 2018）

作者： Shuang Hao Zhuang Hou Chuo Guo Key Laboratory of Structure-Based Drugs Design and Discovery(Ministry of Education) School of Pharmaceutical EngineeringShenyang Pharmaceutical University

The field of glycoscience has received considerable attention over the past decade,due in large part to the recognition of the important roles carbohydrates play in biology and medicine. In this study,a series of novel amide-linked polysaccharides were synthesized starting from corresponding glucuronic acid *** that have been developed to synthesis of glucuronic acid derivatives via the efficient and selective removal of a C-6 methyl group in our previous study. Based on the synthetic methodology,this investigation is related to the development of a general strategy for the synthesis of certain amide-linked *** present method proves to be efficient and environmentally friendly in terms of shorter reaction time-and resource-consuming workup and purification steps,simpler synthetic procedures and high yield.

关键词： Amide-Linked Polysaccharides Glucuronic acid Synthetic methodology

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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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