Synthesis of tricyclic pyrazolopyrimidine arylidene ester derivatives and their cytotoxic and molecular docking evaluations

Abstract

Our research team has synthesized 33 tricyclic pyrazolopyrimidine arylidene ester derivatives using the lead compound CAM551 as a starting point. This was achieved by a designed five‐step synthesis strategy. The synthesized compounds' inhibitory activities against HT‐116 human colorectal adenocarcinoma cell line and HGC27 human gastric cancer cells were assessed through traditional MTT assays. The designed and synthesized compounds demonstrated superior inhibition against both types of cancer cells. Additionally, compound 7b, which contains a long‐chain substituent, exhibited improved inhibition against hepatocellular carcinoma cells and a greater safety profile. These findings indicate that compound 7b has the potential as an antitumor lead compound for future research.