发明名称 Anti-tumor agents comprising pyridyl-substituted metal-diphosphine complex
摘要 A method of treatment or inhibition of tumors including the steps of: (i) exchanging one or more of the eight phenyl substituents in the compound [M(dppe)2]+ where M is selected from Au(I), Ag(I) and Cu(I) by 2, 3, or 4 pyridyl substituents to provide a compound having anti-tumor activity and an octanol/water partition coefficient between 0.01 and 25.5; and (ii) administering said compound to a subject requiring treatment which compound has selective toxicity to cancer cells including cisplatin resistant human carcinoma cell lines. The invention also includes within its scope compounds of formula (I)wherein R1, R2, R3, R4, R5, R6, R7 and R8 are the same or different and may be selected from phenyl, 4-pyridyl, 3-pyridyl, 2-pyridyl wherein each of the 4-pyridyl, 3-pyridyl and 2-pyridyl may optionally be substituted; A is selected from -(CH2)- wherein n is 2 or 3 or cis -CH=CH- or (a) where R9 represents carboxylate and in such case R1, R2, R3, R4, R5, R6, R7 and R8, may be all phenyl; M is Au(I), Ag(I) or Cu(I); X is monovalent anion such as nitrate or bromide, chloride, iodine or any other non-toxic anion; with the following provisos: (i) R1 through R8 cannot be all phenyl; (ii) when R1 through R8 is 2-pyridyl, and A is -(CH2)2-, M cannot be Au(I); or (iii) when R1 through R8 is the same and is 4-pyridyl, X is Cl and A is -(CH2)2-, M cannot be Au(I).
申请公布号 US6218378(B1) 申请公布日期 2001.04.17
申请号 US19970860518 申请日期 1997.08.22
申请人 GRIFFITH UNIVERSITY 发明人 BERNERS-PRICE SUSAN JANE;BOWEN RICHARD JOHN;PARSONS PETER GORDON
分类号 A61K31/695;A61K31/675;A61P35/00;C07F9/50;C07F9/58;(IPC1-7):A01N55/02;A61K31/555;C07F1/10;C07F1/12 主分类号 A61K31/695
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