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Chinese Chemical Letters 2010年第5期21卷 554-557页

作者： bao liu,qi dong you,zhi yu li department of medicinal chemistry,china pharmaceutical university,nanjing 210009,china department of medicinal chemistry China Pharmaceutical University Nanjing 210009 China

A series of new 6,7-disubstituted-4-(benzothiazol-6-ylamino)quinoline-3-carbonitrile derivatives(12a-l) were *** cytotoxicity of 12 new compounds was evaluated in AGS,HepG2 and HT-29 cell *** results showed that compounds 12g, 12h,12i,12k and 12l displayed more potent cytotoxic activities than Bosutinib,compound 12l exhibited the most potent antitumor activity among the tested compounds.

关键词： 3-Quinolinecarbonitrile derivatives Synthesis Antitumor

Syntheses of 2- or 6-Substituted Chromones and Chromone Ring-opening Reaction in Polyphosphoric Acid

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Chemical Research in Chinese Universities 2004年第3期20卷 299-304页

作者： HE Xun-gui you qi-dong li zhi-yu department of medicinal chemistry School of PharmacyChina Pharmaceutical UniversityNanjing 210009P.R.China Shanghai Institute of Materia Medica Chinese Academy of SciencesShanghai 201203P.R.China

In an attempt to find new antitumor agents,a novel class of chromone compounds with a benzimidazole or a benzoxazole ring in positions 2 or 6 were synthesized via condensation in polyphosphoric acid(PPA) by using chromone acids as the starting materials. During the preparation process,it was found that PPA could cleave the chromone ring to produce a ring-opening compound(6). The molar ratio of the chromone compound(5) to the ring-opening compound(6) varied with the change of reaction temperature and time. Based on MTT protocol,the antitumor activity of each of the compounds obtained was evaluated against three human cancer cell lines: KB(oral epidermal),A2780(ovary) and Bel7402(liver). The IC_ 50 varied from 54.7 μmol/L to more than 180 μmol/L.

关键词： 2-or 6-Substituted chromone Antitumor agent Polyphosphoric acid Ring-opening reaction

Design,synthesis and antitumor activity of 3-substituted quinolone derivatives (Ⅰ)

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Chinese Chemical Letters 2008年第12期19卷 1395-1397页

作者： Hua Wang qi dong you zhi yu li Yi Quan Zou department of medicinal chemistry China Pharmaceutical University Nanjing 210009 China

A series of quinolone derivatives containing benzimidazole, benzoxazole or benzothiazole ring were synthesized. The cytotoxicity of 12 new compounds was evaluated in KB, Be17402, A2780 and HT-29 cell lines. Most of synthesized compounds showed moderate inhibitory activity against cancer cells. The inhibitory activities of 6k, against KB and A2780 tumor ceils are comparable to that of topotecan, one of topoisomerase I inhibitors.

关键词： Quinolone derivatives Synthesis Antitumor

Advantages of Rho-associated kinases and their inhibitor fasudil for the treatment of neurodegenerative diseases

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Neural Regeneration Research 2022年第12期17卷 2623-2631页

作者： qing Wang li-Juan Song zhi-Bin Ding zhi Chai Jie-Zhong yu bao-Guo Xiao Cun-Gen Ma Research Center of Neurobiology The Key Research Laboratory of Benefiting Qi for Acting Blood Circulation Method to Treat Multiple Sclerosis of State Administration of Traditional Chinese MedicineShanxi University of Chinese MedicineJinzhongShanxi ProvinceChina department of Physiology Shanxi Medical UniversityTaiyuanShanxi ProvinceChina Institute of Brain Science Shanxi Key Laboratory of Inflammatory Neurodegenerative DiseasesShanxi Datong UniversityDatongShanxi ProvinceChina department of Neurology Datong Fifth People’s HospitalDatongShanxi ProvinceChina Institute of Neurology Huashan HospitalInstitutes of Brain Science and State Key Laboratory of Medical NeurobiologyFudan UniversityShanghaiChina

Ras homolog(Rho)-associated kinases(ROCKs)belong to the serine-threonine kinase family,which plays a pivotal role in regulating the damage,survival,axon guidance,and regeneration of *** are also involved in the biological effects of immune cells and glial cells,as well as the development of neurodegenerative disorders such as Alzheimer’s disease,Parkinson’s disease,and multiple *** studies by us and others confirmed that ROCKs inhibitors attenuated the symptoms and progression of experimental models of the abovementioned neurodegenerative diseases by inhibiting neuroinflammation,regulating immune imbalance,repairing the blood-brain barrier,and promoting nerve repair and myelin ***,the first ROCKs inhibitor to be used clinically,has a good therapeutic effect on neurodegenerative *** increases the activity of neural stem cells and mesenchymal stem cells,thus optimizing cell *** review will systematically describe,for the first time,the effects of abnormal activation of ROCKs on T cells,B cells,microglia,astrocytes,oligodendrocytes,and pericytes in neurodegenerative diseases of the central nervous system,summarize the therapeutic potential of fasudil in several experimental models of neurodegenerative diseases,and clarify the possible cellular and molecular mechanisms of ROCKs *** review also proposes that fasudil is a novel potential treatment,especially in combination with cell-based *** from this review add support for further investigation of ROCKs and its inhibitor fasudil for the treatment of neurodegenerative diseases.

关键词： Alzheimer’s disease cell-based therapy central nervous system cells fasudil immunocytes multiple sclerosis Parkinson’s disease pericytes Rho kinase inhibitor Rho-associated kinases

新思路·新技术——中药复方新药研发相关重大科学和技术问题

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中国药理学与毒理学杂志 2020年第4期34卷 241-260页

作者：蒋宁杜保民杜冠华段大跃方坚松高兴华高秀梅顾金辉郭彦飞侯悦黄晏李琦林志彬刘建勋陆茵吕圭源聂红庞晓斌齐晓甜秦雪梅任巧任远任周新茹祥斌申竹芳石京山孙建宁孙蓉孙晓波王陈王梅王同兴吴春福谢宗杰徐惠波薛云丽杨宝学杨奎余林中张丹参张兰张林张永鹤张永祥赵勤实周玉枝朱焰周文霞军事科学院军事医学研究院毒物药物研究所北京100850 北京北大维信生物科技有限公司北京100094 中国医学科学院北京协和医学院药物研究所北京100050 西南医科大学附属中医医院中医药表型组学中心四川泸州646000 广州中医药大学科技创新中心广东广州510006 中国药科大学江苏南京210009 天津中医药大学天津301617 国家卫生健康委员会科技教育司重大专项处北京100044 东北大学辽宁沈阳110819 中国中医科学院中药研究所北京100700 北京大学基础医学院北京100191 中国中医科学院西苑医院北京100091 南京中医药大学药学院江苏南京210023 浙江中医药大学现代中药与健康产品研究所浙江杭州310053 广东省药效物质基础和创新药物研究重点实验室广东广州510632 河南大学药学院河南开封475004 山东大学高等医学研究院山东济南250012 山西大学中医药现代研究中心山西太原030006 甘肃中医药大学甘肃兰州730000 河南中医药大学河南郑州450046 遵义医科大学贵州遵义563003 北京中医药大学北京100029 中国医学科学院药用植物研究所北京100193 莱顿大学-欧洲中医药和天然化合物中心荷兰莱顿天士力国际基因网络药物创新中心有限公司天津300410 沈阳药科大学辽宁沈阳110016 吉林省中医药科学院吉林长春130012 山东绿叶制药有限公司山东烟台264003 成都中医药大学四川成都611137 南方医科大学广东广州510515 河北科技大学河北石家庄050018 首都医科大学宣武医院北京100053 中国科学院昆明植物研究所云南昆明650201 复旦大学上海200433

"第十二届全国中药与天然药物药理学术会议"于2019年10月11-13日在天津市社会山国际会议中心酒店举行。会议期间,中国药理学会中药与天然药物药理专业委员会召开了"中药复方新药研发相关重大科学和技术问题"专题研讨会。研讨会分为主题... 详细信息

"第十二届全国中药与天然药物药理学术会议"于2019年10月11-13日在天津市社会山国际会议中心酒店举行。会议期间,中国药理学会中药与天然药物药理专业委员会召开了"中药复方新药研发相关重大科学和技术问题"专题研讨会。研讨会分为主题报告和综合讨论2部分。主题报告由中国药理学会中药与天然药物药理专业委员会副主任委员吴春福教授主持,刘建勋、孙晓波、段大跃和吕圭源教授作主题报告。中国药理学会理事长兼中药与天然药物药理专业委员会主任委员张永祥研究员主持综合讨论,国家卫生健康委员会科技教育司重大专项处顾金辉处长全程参加。与会专家围绕中药复方新药研发相关重大科学和技术问题进行了广泛、深入的讨论。本文整理了专家们的主要观点和建议,希望能为中药复方新药研发提供新思路和新技术,为提高我国中药复方新药的研发水平发挥积极的推动作用。

关键词：中药复方新药研发新思路新技术