Abstract: Chemical agents, such as derivatives of hydroxy benzene moieties, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of enzymes and structural polypeptides present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.

Abstract: Methods for identifying antineoplastic agents by using their ability to modify expression of specific genes or the biological activity of polypeptides encoded by such genes, wherein said genes are located in specific chromosomal regions, called amplicons, or regions of interest, and the presence of such amplified regions within a cancerous cell, are disclosed. Also described are methods for diagnosing cancerous, or potentially cancerous, conditions using these methods. Also encompassed are methods involving determining the modulated expression of the genes in these regions of interest (ROIs), or amplicons, as pharmacodynamic/pharmacogenetic/surrogate markers and/or for patient profiling prior to accrual for clinical trials/treatments based on the identification of these genes as validated gene/drug targets in various cancer tissue types.

Abstract: Compounds of the general structure according to Formula (I) wherein R1 is selected from alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, and heterocycloalkyl; R2 is selected from alkyl, alkenyl, alkyny, heteroalkyl, haloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, and heterocycloalkylalkyl; R3 is selected from aryl, heteroaryl, cycloalkyl, and heterocycloalkyl; W is selected from Ch2, O and S; n is 0 to about 3: X is selected from S or O; Y, if present, is selected from a bond, aryl, NH, NR, O or S, where R3 is selected from hydrogen, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, and heterocycloalkylalkyl; and Z, if present, can represent a bond or is selected from lower alkyl, O or S are disclosed. Also disclosed are uses of such compounds for treating a variety of disease conditions, including cancer.