A Facile One‐Pot Synthesis of New Fused Indole Pyrazole Derivatives and Their Anticancer and Antidiabetic Activities

Abstract

Indole‐pyrazole hybrids are intriguing due to their potential for synergistic pharmacological effects, unlike molecules with only one pharmacophore. This study presents a one‐pot synthesis of fused indole‐pyrazole derivatives, bis indole‐pyrazole 4a and chromone indole‐pyrazole 4b using an aldehyde, thiosemicarbizide, and an indole, as potential anticancer and antidiabetic agents. The synthesized compounds were characterized using Fourier transform infrared (FTIR), nuclear magnetic resonance (NMR), and time‐of‐flight mass spectrometry (TOF‐MS). Initially, a mutagenicity test was performed, and the compounds showed no significant increase in revertant colonies against Salmonella typhimurium TA 98 and TA 100 strains. In the MTT assay for cytotoxicity against two human cancer cell lines, A549 and HepG‐2; and one normal cell line, HEK 293. Compound 4b showed high potency against the cancer cell lines, with IC50 values of 18.70 and 50.07 µg/mL, respectively, whereas both compounds showed low inhibition level against HEK 293 at 100 µg/mL. The in vitro inhibition of α‐amylase and α‐glucosidase, compound 4a demonstrated excellent in vitro inhibition of α‐amylase and α‐glucosidase, with the IC50 values of 3.9 µg/mL and 12.1 µg/mL, respectively.