Indole-3-carbinol (I3C) derivatives and methods
First Claim
1. A pharmaceutical compostition comprising a compound of any of Tables VI-IX and, or a pharmaceutically acceptable salt or ester thereof, wherein said compound inhibits tumor cell growth, is other than indole-3-carbinol (I3C), 3,3′
- -diinodolylmethane (DIM) and indole[3,2-b]carbazole (ICZ); and
a pharmaceutically acceptable excipient.
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Abstract
The invention provides methods and compositions relating to novel bioactive derivatives of indole-3-carbinol (I3C), including pharmaceuticals comprising a pharmaceutically acceptable excipient and a compound of the general formula:
which inhibits tumor cell growth. Methods of inhibiting targeted cell growth include contacting a target cell with a disclosed compound under conditions whereby the growth the target cell is inhibited, and methods for evaluating the growth inhibitory activity of the compounds include contacting a cell with an effective amount of the compound and measuring the CDK6 expression in the cell, wherein a reduction in CDK6 expression correlates with the growth inhibitory activity of the compound.
44 Citations
21 Claims
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1. A pharmaceutical compostition comprising a compound of any of Tables VI-IX and, or a pharmaceutically acceptable salt or ester thereof, wherein said compound inhibits tumor cell growth, is other than indole-3-carbinol (I3C), 3,3′
- -diinodolylmethane (DIM) and indole[3,2-b]carbazole (ICZ); and
a pharmaceutically acceptable excipient. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17)
- -diinodolylmethane (DIM) and indole[3,2-b]carbazole (ICZ); and
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18. A method of inhibiting cell growth comprising contacting a target cell with a compound of the general formula:
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or a pharmaceutically acceptable salt or ester thereof, wherein; R1-5 are independently selected from the group consisting of substituted or unsubstituted alkyl, alkenyl, alkynyl, and aryl; and
wherein said compound inhibits tumor cell growth and said compound is other than indole-3-carbinol (I3C), 3,3′
-diinodolylmethane (DIM) and indole[3,2-b]carbazole (ICZ), under conditions whereby the growth said target cell is inhibited.- View Dependent Claims (19)
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20. A method for evaluating the growth inhibitory activity of an I3C derivative, said method comprising the steps of:
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treating cultured MCF7 human breast cancer cells with an effective amount of an I3C derivative; and
measuring the CDK6 expression in said cells;
wherein a reduction in CDK6 expression in said cells as compared with otherwise comparable but untreated cells is indicative of growth inhibitory activity of said derivative. - View Dependent Claims (21)
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Specification