| abstract |
"BENZOCYCLODECAN DERIVATIVES WITH ANTITUMORAL ACTIVITY". The present invention relates to a compound which is a benzocyclodecane of formula I wherein <sym> at positions 8 and 9, and 11-12 independently represent a single bond or double bond, -R ~ 1 ~, is = O, or -OR7, -R7 is H C1-7 alkanoyl, benzoyl, C1 -C10 alkyl, C2 -C10 alkenyl or COCH-CHR8, -R8 is aryl or heterocyclyl; -R 2 and -R 3 are H, = O or -OR 9, -R 9 is H, C 1 -C 7 alkanoyl or benzoyl; when at position 11 -12 there is a single bond then -R 4 represents = O, = CH 2, = CHCOOR 10, R 10 is C 1 -C 10 alkyl or aryl; = CH (OCH 3), -OR 9; -CH 2 OR 11, R 11 is H or a sugar residue, -COR 12, R 12 is H, -OH or -OR 10; or when at position 11-12 there is a double bond, then -R4 is -CH2OR11 or -COR12; -R5 and -R6 are H or, when in position 8-9 there is a single bond, together they form a cyclopropane ring; R13 is H or 1-3 substituents selected from C1-C6 alkyl, C2-C6 alkenyl, phenyl, phenyl C1-C6 alkyl, halogen, hydroxy, C1-C6-alkoxy, aryloxy, cyano, nitro, amino, C1-C10 alkylamino arylamino, C1-C7 alkanoylamino, aroylamino, hydroxycarbonyl, aminocarbonyl, C1-C6-alkylcarbonyl, C1-C6-alkylaminosulfonyl and arylaminosulfonyl group; provided that if R1 and R4 = 0, then one of R2, R3, R5, R6 and R13 is not an H atom; or a pharmaceutically acceptable salt thereof. These benzocyclodecane derivatives are endowed with antitumor activity; Also provided are a process and novel intermediates for their preparation, pharmaceutical compositions containing them, and their use in cancer prevention, control and treatment. |