NOVEL DISUBSTITUTED ADAMANTYL DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PRODUCTION METHOD FOR SAME, AND PHARMACEUTICAL COMPOSITION FOR SUPPRESSING CANCER METASTASIS COMPRISING SAME AS ACTIVE INGREDIENT

摘要

The present invention relates to a novel disubstituted adamantyl derivative or the pharmaceutically acceptable salts thereof, a method for preparing the same, and a pharmaceutical anticancer or antimetastasis composition comprising the same as an active ingredient. The disubstituted adamantyl derivative of the present invention suppressed accumulation of HIF-1α, inhibiting the expression of the metastasis related protein Twist dose-dependently. Thus, the disubstituted adamantyl derivative of the invention is effective in inhibiting the expressions of the metastasis related proteins, β-catenin and RohA, and the EMT related genes such as MMP2 and MMP9, without cytotoxicity. Therefore, the disubstituted adamantyl derivative or the pharmaceutically acceptable salts thereof of the invention can be efficiently used as a pharmaceutical anticancer or antimetastasis composition.

主权项

1. A disubstituted adamantyl derivative represented by formula 1 or a pharmaceutically acceptable salt thereof: wherein R1 is —X—(CH2)n—R3; R2 is H or a C1-C6 straight or branched alkyl; and R3 is unsubstituted or substituted C5-C10 aryl or unsubstituted or substituted heteroaryl, wherein the heteroaryl is 5-membered or 6-membered heteroaryl comprising one or more heteroatoms selected from the group consisting of N, O, and S, the substituted aryl or heteroaryl can be substituted with one or more halogens; C1-C6 straight or branched alkyl; hydroxy; C1-C6 straight or branched alkoxy; nitro; nitrile; unsubstituted amine or amine substituted with one or more C1-C6 straight or branched alkyls; C1-C6 straight or branched alkylcarbonyl or 5-membered or 6-membered heterocycloalkyl comprising heteroatoms selected from the group consisting of N, O, and S; X is NH or O, provided that when R3 is unsubstituted or substituted aryl X is O; and n is an integer of 1-5.