In order to obtain less toxic antitumoral compounds we have looked for novel compounds with anticancer activity based on proapoptotic mechanisms. The compounds studied in this work are derivatives of bicyclic aromatic systems like pyrido[2,3-d]pyrimidines. The potential antitumoral activity of the compounds was evaluated in vitro by examining their cytotoxic effects against human breast, colon, and bladder cancer lines (MD-MBA-231, HT-29, and T-24). The data indicate that HC-6 is a potent anticancer drug showing dose-dependent cytostatic and proapoptotic effects through activation of two different signaling pathways namely a pathway leading to cell cycle arrest and a transcription-independent route leading to rapid apoptosis.