Azoles, viz., pyrazoles and pyrazolines, constitute valuable building blocks in medicinal chemistry.15 Presently, different commercially available pyrazole-containing drugs are used to treat various types of cancers (Fig. 1).59–62 Several studies demonstrated that pyrazole-based compounds exhibit in vitro and in vivo antitumor activity by inhibiting various enzymes such as topoisomerase II, EGFR, MEK, VEGFR, GGT1, microtubule, and HDACs.59–62. Here, KDR is linked to cancer.