SUBSTITUTED HETEROCYCLES AS c-MYC TARGETING AGENTS

A compound—

• (a) having a formula II:
• wherein
• Y is C or N;
• R1 is hydrogen or an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R1 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• n is 0, 1, or 2;
• p is 0 or 1;
• X is O or NH, or R1(CH2)n(X)p— is N-piperazinyl optionally N-substituted with alkyl;
• m is 0 or 1;
• R2 is hydrogen or halo, or R2 is an alkyl group, an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R2 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• R3 is hydrogen, alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, benzyl, hydroxyl, halo, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• R4 is not present, or R4 is hydrogen, amino, alkyl, aryl, or benzyl;
• R4 optionally is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, alkoxycarbonyl, aryloxy, and alkylaryloxy;
• R5 is alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, and halo;
• R6 is not present, or R6 is hydrogen, amino, alkyl, aryl, or benzyl;
• R6 optionally is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, alkoxycarbonyl, aryloxy, and alkylaryloxy;
• and
• R7 is hydrogen or halo, or R7 is an alkyl group, an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R7 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• with the proviso that at least one of R4 and R6 is present;
• (b) having a formula III:
• wherein:
• R1 is hydrogen or an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R1 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• n is 0, 1, or 2;
• p is 0 or 1;
• X is O or NH, or R1(CH2)n (X)p— is N-piperazinyl optionally N-substituted with alkyl;
• m is 0 or 1;
• R2 is hydrogen or halo, or R2 is an alkyl group, an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R2 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• R4 is hydrogen, amino, alkyl, aryl, or benzyl;
• R4 optionally is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, alkoxycarbonyl, aryloxy, and alkylaryloxy;
• R5 is alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, and halo;
• and
• R7 is hydrogen or halo, or R7 is an alkyl group, an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R7 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• (c) having a formula IV:
• wherein:
• R1 is hydrogen or an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R1 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• n is 0, 1, or 2;
• p is 0 or 1;
• X is O or NH, or R1(CH2)n (X)p— is N-piperazinyl optionally N-substituted with alkyl;
• Y is CH or N;
• Z is C or N;
• m is 0 or 1;
• R2 is hydrogen or halo, or R2 is an alkyl group, an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R2 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• R4 is hydrogen, amino, alkyl, aryl, or benzyl;
• R4 optionally is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, alkoxycarbonyl, aryloxy, and alkylaryloxy;
• R5 is alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, amino, hydroxyalkyl, —C(O)H, and halo;
• and
• R7 is hydrogen or halo, or R7 is an alkyl group, an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R7 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• or
• (d) having a formula V:
• wherein:
• R1 is hydrogen or an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R1 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• n is 0, 1, or 2;
• p is 0 or 1;
• X is O or NH, or R1(CH2)n (X)p— is N-piperazinyl optionally N-substituted with alkyl;
• m is 0 or 1;
• R2 is hydrogen or halo, or R2 is an alkyl group, an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R2 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• R5 is alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, benzyloxy, and halo;
• and
• R7 is hydrogen or halo, or R7 is an alkyl group, an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R7 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl
• having a formula II:
• wherein
• Y is C or N;
• R1 is hydrogen or an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R1 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• n is 0, 1, or 2;
• p is 0 or 1;
• X is O or NH, or R1(CH2)n (X)p— is N-piperazinyl optionally N-substituted with alkyl;
• m is 0 or 1;
• R2 is hydrogen or halo, or R2 is an alkyl group, an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R2 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• R3 is hydrogen, alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, benzyl, hydroxyl, halo, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• R4 is not present, or R4 is hydrogen, amino, alkyl, aryl, or benzyl;
• R4 optionally is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, alkoxycarbonyl, aryloxy, and alkylaryloxy;
• R5 is alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, and halo;
• R6 is not present, or R6 is hydrogen, amino, alkyl, aryl, or benzyl;
• R6 optionally is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, alkoxycarbonyl, aryloxy, and alkylaryloxy;
• and
• R7 is hydrogen or halo, or R7 is an alkyl group, an aryl group, a benzyl group, a heteroaryl group, a cycloalkyl group, or a cycloheteroalkyl group, optionally R7 is substituted at one or more positions with one or more of alkyl, alkoxy, haloalkyl, haloalkoxy, hydroxyl, halo, cyano, amido, hydrazonyl, carbonyl, carboxyl, and alkoxycarbonyl;
• with the proviso that at least one of R4 and R6 is present.