Controlling the growth of certain tumor tissue with chalcone derivatives
AssigneeMerrell Dow Pharmaceuticals Inc.
InventorsSai P. Sunkara, Michael L. Edwards, David M. Stemerick
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Abstract
Certain chalcone derivatives are reported to inhibit the polymerization of tubulin to form microtubules and are therefore antimitotic agents which can be used to control the growth of tumor tissue and can be used as antigout agents.
Claims21
A method of inhibiting the polymerization of tubulin to form microtubules which comprises administering to a patient in need thereof an effective amount of a chalcone derivative of the structure ##STR4## wherein Ar is a 2,5-dimethoxyphenyl, 2,3,4-trimethoxyphenyl, or 3,4,5-trimethoxyphenyl substituent;
- R.sub.1 is a hydrogen, (C.sub.1 -C.sub.4)alkyl, chloro, or bromo substituent;
- and
- R.sub.2 is a --N(R).sub.2 or NHCOR wherein R is a (C.sub.1 -C.sub.4)alkyl substituent
- or a pharmaceutically acceptable salt thereof.
A method for controlling the growth of tumor tissues sensitive to treatment with the chalcone derivative as defined below which comprises administering to a patient in need thereof an effective amount of a chalcone derivative of the structure ##STR5## wherein Ar is a 2,5-dimethoxyphenyl, 2,3,4-trimethoxyphenyl, or 3,4,5-trimethoxyphenyl substituent;
- R.sub.1 is a hydrogen, (C.sub.1 -C.sub.4)alkyl, chloro, or bromo substituent;
- and
- R.sub.2 is a --N(R).sub.2 or NHCOR wherein R is a (C.sub.1 -C.sub.4)alkyl substituent or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.