COMBRETASTATIN

作品数:51被引量:69H指数:5
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Recent clinical trials and optical control as a potential strategy to develop microtubule-targeting drugs in colorectal cancer management被引量:1
《World Journal of Gastroenterology》2024年第13期1780-1790,共11页Katsuhiro Kita Allen Burdowski 
Colorectal cancer(CRC)has remained the second and the third leading cause of cancer-related death worldwide and in the United States,respectively.Although significant improvement in overall survival has been achieved,...
关键词:Colorectal cancer CHEMOTHERAPY MICROTUBULE COMBRETASTATIN Photopharmacology 
Introducing urea into tirapazamine derivatives to enhance anticancer therapy
《National Science Review》2024年第4期239-247,共9页Yajun Xu Jianlin Lv Chaoying Kong Ya Liu Kun Wang Zhaohui Tang Xuesi Chen 
This work was supported by the Ministry of Science and Technology of China(2022YFE0110200);the National Natural Science Foundation of China(52025035);the Jilin Provincial International Cooperation Key Laboratory of Biomedical Polymers Grant(20210504001GH).
Tirapazamine(TPZ)has been approved for multiple clinical trials relying on its excellent anticancer potential.However,as a typical hypoxia-activated prodrug(HAP),TPZ did not exhibit survival advantages in Phase III cl...
关键词:TIRAPAZAMINE vascular disrupting agent hypoxia-activated prodrug combretastatin A4 UREA 
Combretastatin A-4衍生物的设计、合成及抗乳腺肿瘤活性初探被引量:3
《合成化学》2023年第10期749-760,共12页高祎婷 丁茂鹏 马腾 周昊天 刘晓航 孙晓飞 马成 
新疆维吾尔自治区自然科学基金地州科学基金资助项目(2021D01F40);新疆第二医学院科研基金面上项目(MS202301)。
Combretastatin A-4(CA-4)是一个天然的秋水仙碱结合位点的微管蛋白抑制剂,具有抗肿瘤活性。PI3K信号通路是细胞内重要的信号转导通路之一,也是癌细胞中常见的异常表达信号通路。微管蛋白抑制剂和信号通路激酶抑制剂均为抗肿瘤药物研发...
关键词:CA-4 秋水仙碱 微管蛋白 PI3K 构效关系 分子对接 合成 
A mild phenoxysilyl linker for self-immolative release of antibody-drug conjugates
《Chinese Chemical Letters》2023年第5期494-498,共5页Ding Wei Yurong Mao Huihui Wang Siqi Qu Jiakang Chen Jiusheng Li Biao Jiang Hongli Chen 
supported by Shanghai Frontiers Science Center for Biomacromolecules and Precision Medicine at Shanghai Tech University。
Self-immolative linkers have been widely used to construct prodrugs to improve their efficacy and safety.In this study,we report the use of phenoxysilyl linker as a self-immolative unit to prepare antibody-drug conjug...
关键词:Antibody-drug conjugates Self-immolative release Phenoxysilyl linker Combretastatin A4(CA4) 
Transcatheter Arterial Embolization Combined with Anti-vascular Agent Combretastatin A4 Phosphate Inhibits Growth and Vascularization of Liver Tumor in an Animal Model被引量:2
《Current Medical Science》2022年第6期1240-1247,共8页Hui ZHAO Zhen-zhong WU Quan REN Jing-jing WU Ying WANG Jun-wei FENG Min RAO Qing DENG Hong-yao HU 
supported in part by the Fundamental Research Funds for the Central Universities(No.2042015kf0104);in part by the Hubei Provincial Natural Science Foundation of China(No.2015CFB343).
Objective This study aimed to investigate the effect of combretastatin A4 phosphate(CA4P)on proliferation,migration,and capillary tube formation of human umbilical vein endothelial cells(HUVECs)and the efficacy of tra...
关键词:embolization therapeutic vascular disrupting agents combretastatin A4 phosphate liver cancer 
Designing anticancer combretastatin A-4 analogues with aggregation-induced emission characteristics被引量:1
《Science China Chemistry》2022年第4期694-698,共5页Rucheng Zhao Yusheng Wu Yuequn Zhang Jiabao Ling Xinxin Liu Jiaqi Xiang Xiangchao Zeng Tianfeng Chen 
supported by the National Key R&D Programs of China(2017YFC1103603);the National Natural Science Foundation of China(21877049,32171296);Guangdong Natural Science Foundation(2020B1515120043);the Innovation Team Project in Guangdong Colleges and Universities(2019KCXTD008);K.C.Wong Education Foundation。
Herein a series of combretastatin A-4(CA-4)analogues with aggregation-induced emission characteristics(compounds a1-a19)were rationally designed and synthesized.The research results showed that the mechanism of AIE of...
关键词:combretastatin A-4 analogues ANTICANCER AIE CARBAZOLE FLUORENE 
Time-course monitoring of in vitro biotransformation reaction via solid-phase microextraction-ambient mass spectrometry approaches
《Journal of Pharmaceutical Analysis》2022年第1期186-191,共6页Karol Jaroch Janusz Pawliszyn 
supported by Shimadzu Scientific Instruments(Columbia,MD,USA)and Canada’s National Science and Engineering Research Council-Industrial Research Chair(NSERC-IRC)program,grant number IRCPJ 184412-15
The solid-phase microextraction technique quantifies analytes without considerably affecting the sample composition.Herein,a proof-of-concept study was conducted to demonstrate the use of coated probe electrospray ion...
关键词:Solid-phase microextraction Coated probe electrospray ionization Coated blade spray COMBRETASTATIN BIOTRANSFORMATION Prodrug activation 
Hypoxia-induced activity loss of a photo-responsive microtubule inhibitor azobenzene combretastatin A4被引量:1
《Frontiers of Chemical Science and Engineering》2020年第5期880-888,共9页Yang An Chao Chen Jundong Zhu Pankaj Dwivedi Yanjun Zhao Zheng Wang 
The work was financially supported by the National Natural Science Foundation of China(Grant No.21650110447).
The conformation-dependent activity of azo-benzene combretastatin A4(Azo-CA4)provides a unique approach to reduce the side-effects of chemotherapy,due to the light-triggered conformation transition of its azobenzene m...
关键词:HYPOXIA microtubule inhibitor drug delivery azo-combretastatin A4 PHOTO-RESPONSIVE 
新型Combretastatin A-4衍生物的合成及生物活性研究
《化学试剂》2020年第9期1130-1133,共4页杨超 钱玺丞 周斌 陈婷 
民族中兽药分离纯化技术西部地区创新能力建设项目(发改办高技〔2016〕2195号);铜仁市科技局基础科学研究专项基金资助项目(2017TRS32195)。
Combretastatin A-4是一类结构独特的天然产物,具有较好的抗肿瘤活性。为了进一步研究该类化合物的构效关系,以3,4,5-三甲氧基苯甲醛和3-羟基-4-甲氧基苯乙酸为原料,在碱性条件下经缩合、酰化反应合成了5个未见文献报道的Combretastatin...
关键词:3 4 5-三甲氧基苯甲醛 缩合 Combretastatin A-4 合成 抗肿瘤 
微管蛋白秋水仙碱结合位点抑制剂Combretastatin A-4类似物的研究进展被引量:3
《沈阳药科大学学报》2019年第9期844-852,共9页王展 关奇 张晓坚 
国家自然科学青年科学基金资助项目(81602969)
目的综述微管蛋白秋水仙碱结合位点抑制剂Combretastatin A-4(CA-4)类似物的研究进展。方法依据近期国内外公开发表的49篇文献,将CA-4类似物的研究进展分类、归纳并总结。结果微管蛋白秋水仙碱结合位点抑制剂(colchicine binding site i...
关键词:秋水仙碱结合部位抑制剂 抗肿瘤活性 构效关系 结构修饰 
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