Design, synthesis, and high-throughput anti-cancer evaluation of novel 4-aminopyrazolo[3,4-]pyrimidine derivatives: potential anti-cancer candidates against UO-31 renal cancer cells

A novel series of 20 compounds containing 4-aminopyrazolo[3,4- d ]pyrimidine core were synthesized, characterized and their chemical structures confirmed using spectroscopic techniques such as 1 H NMR, 13 C NMR, IR, and HRMS. The compound's growth inhibitory activities were evaluated against 60 human tumor cell lines from nine panels: leukemia, non-small cell lung cancer (NSCLC), colon, central nervous system (CNS), melanoma, ovarian, renal, prostate, and breast cancer. Among all the compounds, 11 , 12c , 12d , 12f , and 12j are active against different cancer cell lines. Between all the cell lines, compounds 12c , 12d , 12f , 12j , and 11 showed good inhibitory activity against renal cancer cell lines. From the five-dose study, based on IC 50 values, the order of activity of compounds against renal cancer cell lines was found to be 12c > 12f > 12c > 12j > 11 with 12c being the most potent, was better than sunitinib and sorafenib. Having been recognized as initial hits, these substances need additional pharmacological investigation. Twenty novel 4-aminopyrazolo[3,4- d ]pyrimidine core compounds were synthesized, characterized and identified as novel anti-cancer compounds. These compounds showed excellent activity against UO-31 Renal Cancer Cells.