Stilbene derivatives as anticancer agents
First Claim
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1. A compound of the formula:
- ##STR27## and pharmaceutically acceptable salts thereof wherein X is a cis ethylene radical of the formula;
space="preserve" listing-type="equation">--(Y.sub.1)C═
C(Z.sub.1);
Y1 and Z1 are both hydrogen;
R1, R5, R6 and R8 are independently H, halo, amino, lower alkylamino, diloweralkylamino, mercapto, lower alkylthio, amino lower alkyl, lower alkanoyl, nitro, CF3, amino lower alkoxy, lower alkylamino lower alkoxy, diloweralkylamino lower alkoxy,R2, R3 and R4 are lower alkoxy;
R7 is lower alkoxy, amino, lower alkylamino, alkyl of 1-3 carbon atoms, diloweralkylamino, mercapto, lower alkylthio, amino lower alkyl, lower alkanoyl, nitro, CF3, amino lower alkoxy, lower alkylamino lower alkoxy, and diloweralkylamino lower alkoxy.
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Abstract
The present invention relates to stilbene derivatives which possess utility as anti-cancer agents. The compounds can be used to treat cancers which are susceptible to treatment therewith, and can be utilized in a method of treating such cancers. Pharmaceutical compositions containing the compounds are disclosed. Three preferred compounds among those disclosed are (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene, (Z)-1-(4-methylphenyl)-2-(3,4,5-trimethoxyphenyl)ethene, and 4-methyl-3'"'"',4'"'"',5'"'"'-trimethoxybenzylaniline hydrochloride.
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Citations
34 Claims
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1. A compound of the formula:
- ##STR27## and pharmaceutically acceptable salts thereof wherein X is a cis ethylene radical of the formula;
space="preserve" listing-type="equation">--(Y.sub.1)C═
C(Z.sub.1);Y1 and Z1 are both hydrogen;
R1, R5, R6 and R8 are independently H, halo, amino, lower alkylamino, diloweralkylamino, mercapto, lower alkylthio, amino lower alkyl, lower alkanoyl, nitro, CF3, amino lower alkoxy, lower alkylamino lower alkoxy, diloweralkylamino lower alkoxy,R2, R3 and R4 are lower alkoxy; R7 is lower alkoxy, amino, lower alkylamino, alkyl of 1-3 carbon atoms, diloweralkylamino, mercapto, lower alkylthio, amino lower alkyl, lower alkanoyl, nitro, CF3, amino lower alkoxy, lower alkylamino lower alkoxy, and diloweralkylamino lower alkoxy. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16)
- ##STR27## and pharmaceutically acceptable salts thereof wherein X is a cis ethylene radical of the formula;
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17. (E)-1-(4-N,N-dimethylamino)-2-(3,4,5-trimethoxyphenyl)ethene.
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18. A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of the formula:
- ##STR29## and pharmaceutically acceptable salts thereof wherein X is a cis ethylene radical of the formula;
space="preserve" listing-type="equation">--(Y.sub.1)C═
C(Z.sub.1);Y1 and Z1 are both hydrogen;
R1, R5, R6 and R8 are independently H, halo, amino, lower alkylamino, diloweralkylamino, mercapto, lower alkylthio, amino lower alkyl, lower alkanoyl, nitro, CF3, amino lower alkoxy, lower alkylamino lower alkoxy, diloweralkylamino lower alkoxy,R2, R3 and R4 are lower alkoxy; R7 is lower alkoxy, amino, lower alkylamino, alkyl of 1-3 carbon atoms, diloweralkylamino, mercapto, lower alkylthio, amino lower alkyl, lower alkanoyl, nitro, CF3, amino lower alkoxy, lower alkylamino lower alkoxy, and diloweralkylamino lower alkoxy; and
a pharmaceutical carrier therefor. - View Dependent Claims (19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33)
- ##STR29## and pharmaceutically acceptable salts thereof wherein X is a cis ethylene radical of the formula;
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34. A pharmaceutical composition comprising a pharmaceutically effective amount of a (E)-1-(4-N,N-dimethylamino)-2-(3,4,5-trimethoxyphenyl)ethene and a pharmaceutical carrier therefor.
Specification