Use of colchinol derivatives as vascular damaging agents

A compound of the formula

• wherein
• R1, R2, R3 and R6 are each independently H, optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, alkanoyl or PO3H2, provided that at least one of R1, R2, R3 and R6 is PO3H2;
• X is carbonyl (CO), thiocarbonyl (CS), methylene (CH2) or a group CHR4;
• R4 is OH, O-alkyl or NR8R9;
• R5 and R7 are each independently H, alkyl, halogen, hydroxy, alkoxy, nitro or amino;
• R8 is H, optionally substituted alkyl, cycloalkyl, alkanoyl, thioalkanoyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, arylaminocarbonyl, alkylsulphonyl, arylsulphonyl, aminosulphonyl, alkylaminosulphonyl, dialkylaminosulphonyl or arylaminosulphonyl;
• and
• R9 is H, alkyl or cycloalkyl;
• and pharmaceutically acceptable salts, solvates, and hydrates thereof.

A compound of the formula

• wherein
• R1, R2 and R3 are each independently H, optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, alkanoyl, or PO3H2;
• R6 is PO3H2;
• R4 is H or NR8R9;
• R5 and R7 are each independently H, alkyl, halogen, alkoxy, nitro or amino;
• R8 is H, optionally substituted alkyl, cycloalkyl, alkanoyl, thioalkanoyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, arylaminocarbonyl, alkylsulphonyl, arylsulphonyl, aminosulphonyl, alkyaminosulphonyl, dialkylaminosulphonyl or arylaminosulphonyl;
• and
• R9 is H, alkyl or cycloalkyl;
• and pharmaceutically acceptable salts, solvates and hydrates thereof.

A compound of the formula

• wherein
• R1, R2 and R3 are each independently H, optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, alkanoyl or PO3H2;
• R6 is H, optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl or PO3H2;
• R4 is H or NR8R9;
• R5 and R7 are each independently H, alkyl, halogen, nitro or amino;
• R8 is H, optionally substituted alkyl, cycloalkyl, alkanoyl, thioalkanoyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, arylaminocarbonyl, alkylsulphonyl, arylsulphonyl, aminosulphonyl, alkylaminosulphonyl, dialkylaminosulphonyl or arylaminosulphonyl;
• and
• R9 is H, alkyl or cycloalkyl;
• with the proviso that, when R1, R2 and R3 are all methyl groups and R4 is hydrogen, acetylamino, acetylmethylamino, amino, methylamino or dimethylamino then R6 is not hydrogen, methyl, hydroxyethyl, or acetoxyethyl;
• and pharmaceutically acceptable salts, solvates and hydrates thereof.