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US 6,162,930 AGranted
Anti-mitotic agents which inhibit tubulin polymerization
AssigneeBaylor University
InventorsKevin G. Pinney, George R. Pettit, Vani P. Mocharla, Maria del Pilar Mejia, Anupama Shirali
Life of this patent
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Abstract
Methoxy and ethoxy substituted 3-aroyl-2-arylbenzo[b]thiophenes and benzo[b]thiophene analogues are described for use in inhibiting tubulin polymerization. The compounds' use for treating tumor cells is also described.
Claims13
A compound of the structure:
- ##STR9## wherein X is S,
- R.sub.1 -R.sub.4 are independently chosen from the group consisting of H, OH and C.sub.1 -C.sub.5 alkoxy,
- Z is chosen from the group consisting of C.dbd.O, CH.sub.2, C.sub.2 H.sub.2, CHOH, and CHOCH.sub.3,
- Y is chosen from the group consisting of a covalent bond, CH.sub.2, and CH.sub.2 CH.sub.2,
- and Ar and Ar' are aryl moieties chosen from the group consisting of phenyl and napthyl, further substituted with at least one C.sub.1 -C.sub.5, alkoxy group, at least one of which has at least two C.sub.1 -C.sub.5 alkoxy groups,
- wherein when Ar is 3,4,5-trimethoxyphenyl, Z is C.dbd.O, Y is a covalent bond, R.sub.3 is methoxy, R.sub.1, R.sub.2 and R.sub.4 are H, and Ar is substituted with a methoxy group.
3 more elements
A compound of the structure:
- ##STR10## wherein R.sub.1 -R.sub.4 are independently chosen from the group consisting of H, OH and C.sub.1 -C.sub.5 alkoxy,
- Z is C.dbd.O,
- Y is chosen from the group consisting of a covalent bond, CH.sub.2, and CH.sub.2 CH.sub.2,
- Ar is a phenyl group with at least one C.sub.1 -C.sub.5 alkoxy group and Ar' is a phenyl group with at least two C.sub.1 -C.sub.5 alkoxy groups, wherein when Ar' is 3,4,5-trimethoxyphenyl Z is C.dbd.O, Y is a covalent bond, R.sub.3 is methoxy and R.sub.1, R.sub.2 and R.sub.4 are H, and Ar is substituted with a methoxy group.
1 more element
A compound of the structure ##STR11## where R.sub.1 is H or CH.sub.3 O;
- R.sub.2 is H, CH.sub.3 O or C.sub.2 H.sub.5 O;
- R.sub.3 is CH.sub.3 O of C.sub.2 H.sub.5 O;
- R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are independently H, CH.sub.3 O, C.sub.2 H.sub.5 O, or F;
- R.sub.6 is H, CH.sub.3 O, C.sub.2 H.sub.5 O, OH, F or N(CH.sub.3).sub.2 ;
- wherein at least one of R.sub.4, R.sub.5, R.sub.6, R.sub.7 or R.sub.8 is F or N(CH.sub.3).sub.2 ;
- and X is ##STR12##
3 more elements
A compound of the structure where X is S or S.dbd.O.
A compound of the structure ##STR13## where X is CHOH or C.dbd.O.
Dependencies are inferred from the claim text.