In the present investigation, novel pyrazoles and pyrrolo[3,2-c]pyridines have been designed as potential antiproliferative agents against different types of cancer. Their antiproliferative activities were examined against 61 cancer cell lines of 9 different cancer types. Biological investigation of representative target compounds at molecular level was conducted in order to investigate the possible mechanism(s) of antiproliferative activity of our target compounds. In addition, molecular modeling study was carried out. Some compounds showed broad-spectrum antiproliferative activity, while others demonstrated selectivity over certain types of cancer. Our research led to discovery a selective FMS kinase inhibitor, multiple-kinase inhibitor, ERK kinase inhibitors, and dual ERK/COX-2 inhibitors. This work led to development of novel lead anticancer agents, which can be utilized for future development of potential anticancer agents.