Derivados de etoxi-difeniletano, procesos de preparación y usos del mismo

• Main Authors: XIAO, FANHUA, WU, FANHONG, ZHOU, WEIGUO, XU, FANGMING
• Format: Patent
• Language: Spanish
• Published: 09.09.2014
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Un derivado de etoxi-difeniletano que se caracteriza porque su estructura se muestra como la fórmula (KI): donde R es hidroxi, amino, fosfato, sulfato, fosfato de colina o una cadena lateral de aminoácidos y sales de amonio solubles en agua de los mismos. 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' thereof is simultaneously modified to water soluble prodrug such as phosphate, and similarly, amino acid side chain is introduced to amino at position 3' 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.