Anticancer Potential of Quinazoline Derivatives Modified with Hydrazones and Triazoles Against MG‐63 Cancer Cell Line

Abstract Antiproliferative potential of quinazoline flanked bis‐hydrazones and quinazoline fused bis‐triazoles against human bone cancer cell line (MG‐63) have been described in the present work. A series of 2,4‐bis(2‐(E)‐arylidenehydrazinyl)quinazolines 5a–5n have been synthesized by refluxing 2,4‐dihydrazinylquinazoline with respective benzaldehyde derivatives. Thereafter, these bis‐hydrazone derivatives 5a–5n have been cyclized to corresponding 3,7‐diarylbis([1,2,4]triazolo)[4,3‐ a ][4′,3′‐ c ]quinazolines 6a–6n by using bis(trifluoroacetoxy)iodobenzene (PIFA) as oxidant. All the synthesized bis‐hydrazones 5a–5n and bis‐triazoles 6a–6n were tested for their in vitro anticancer potential against human bone cancer cell line, i.e., MG‐63. These compounds demonstrated moderate to significant cytotoxic activities against the tested cancer cell line comparable to camptothecin as a standard. However, the bis‐hydrazones, 5i and 5n displayed potent antiproliferative properties with GI 50 values of 114.31 µM and 136.95 µM, respectively and bis‐triazoles, 6i and 6k may be considered as potent antiproliferative agents with their GI 50 values 137.69 µM and 124.26 µM, respectively.