Abstract: Novel 5-Aminosalicylate-4-thiazolinone derivatives for therapeutic formulations and methods for treating cancer. There are provided novel compounds as development of new anti-cancer agents with multicellular targets and with higher selectivity to cancer cells to enhance the outcome of cancer therapy. In a preferred aspect, there is provided a pharmaceutical composition, including a therapeutically effective amount of compound I.A, or a pharmaceutically acceptable salt thereof, and one or more pharmaceutical excipients.