Other

Shanghai Ecust Biomedicine Co., Ltd.

Zhejiang Wild Wind Pharmaceutical Co. Ltd.

Fanhong Wu

Lei Zhao

Zhikai Zhang

Weiguo Zhou

Fangming Xu

Fanhua Xiao

Zhonglin Ma

Jiujiu Zhou

Xiaodong Yu

Jinwen Huang

Wan Pang

Jianyue Wu

Disclosed is a 5-fluorouracil derivative having the molecular structure shown in general formula VI, in which Ra and Rb groups are an alkoxy group or a fluorine-substituted alkoxy group having 1, 2, 3, or 4 carbon atoms, and are mono-, bis-, tri-, tetra- or penta-substituted on a phenyl group; a linking group L1 is an alkyl or alkenyl group having 1, 2, 3, or 4 carbon atoms, a linking group L2 is oxygen, or an alkyl or alkoxy group having 1, 2, 3, or 4 carbon atoms, or an amino acid, or an alkyl group having 1, 2, 3, or 4 carbon atoms containing an amino moiety, or a furyl group, and an X group is O or &#x2014;NH&#x2014;. Further disclosed is a method for preparing such a derivative and a use of the same in the treatment of cancer, tumor diseases, and diseases caused by abnormal neovascularization in a human or non-human mammal, and a medicament or a composition containing the 5-fluorouracil derivative.

5-fluorouracil derivatives, preparation methods and uses thereof

The invention discloses an ethoxydiphenylethane derivative and a synthetic method and uses thereof 4' position of phenylethane B aromatic ring is chemically modified by ethoxy and hydroxy at position 3&#x2032; thereof is simultaneously modified to water soluble prodrug such as phosphate, and similarly, amino acid side chain is introduced to amino at position 3&#x2032; to form amino acid amide water soluble prodrug having the structure shown as formula (I) the ethoxydiphenylethane derivative and the prodrug thereof include strong tubulin aggregation inhibiting ability and obvious target damage effect for tumor vessels, selectively cause dysfunction and structural damage of tumor vessels and induce apoptosis of vascular endothelial cells in order to play the role of killing tumor cells or inhibiting tumor metastasis in case that the tumor cells are free from the support of nutrition and oxygen.

Ethoxy diphenyl ethane derivatives, preparation processes and uses thereof

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Shanghai, China

Fanhong Wu