The main objective in this study was the synthesis of new urea, indole, and triazole derivatives of 4-(1,3-benzothiazol-2-yl)-benzoyl-1H-pyrazole as anticancer agents able to inhibit VEGF–VEGFR2 complex formation and to suppress proliferation and survival of endothelial cells, angiogenesis and consequently cancer progression. The gene discussed is KDR; the disease is cancer.