||Lung cancer is well known as the second most common malignancy and the leading cause of cancer related deaths in the US for both men and women. 1 Colon cancer is the third most common type of cancer and the second leading cause of cancer related deaths in the US. 2, 3 There is a constant quest for an optimal therapeutic drug for not only these but all cancers. This research has focused on screening novel compounds which include, but are not limited to, pyrido-mimetics and purino-mimetics in an attempt to delineate a new family of cancer fighting drugs. The A549 epithelial lung and LS180 colon cancer cell lines were used to determine the growth inhibitory concentration of the drugs. These studies revealed two lead compounds that were highly effective against both cancers. The lowest IC50 values were noted in the micromolar range similar to cisplatin, which is a widely used chemotherapeutic agent. Compounds 4 and 8 were most effective against the A-549 cells with IC-50 values of 59.15μM and 109.75μM respectively, and compounds 5 and 6 were most effective against the LS-180 cells with IC-50 values of 175.4μM and 98.2 μM respectively. The most effective compounds were tested to determine the mode of action of both the A-549 and LS-180 cell lines. These studies revealed that cell death primarily resulted from damage or inhibition of the DNA, however the DNA itself was unfragmented, which implies that these compounds affect transcription or translation.