Prompted by the aforementioned findings related to indeno[1,2-c]pyrazoles exerting potent inhibitory effects on TKs (e.g., EGFR) involved in the pathogenesis of cancer, the microwave (MW)-assisted synthesis of new indeno[1,2-c]pyrazoles was performed efficiently, and in vitro studies were carried out to assess their potency as EGFR-targeted anti-NSCLC agents. The gene discussed is EGFR; the disease is cancer.