In our attempt to develop potential new drug candidates with promising antimicrobial, antioxidant, and anticancer activities, a series of novel pyrazolothiazole derivatives (PTDs) were synthesized via conventional heating and microwave irradiation as a green technique. The synthesized compounds were characterized through different spectroscopic methods and elemental analyses. Moreover, these compounds were tested for their antimicrobial activity, antioxidant potency, and in‐ silico cancer prevention potential by inhibiting the wingless (Wnt)/β‐catenin signaling pathway, a potent method for cancer cell death. Our results showed that all compounds exhibited antimicrobial impact against E. coli, S. aureus, P. aeuroginosa, B. subtilis, A. flavus, and C. Albicans as well as antioxidant scavenging activity. In addition, the in‐ vitro cytotoxic evaluation of each compound was performed on a panel of cancer cell lines and they agreed with the molecular docking simulation results. Our findings showed that the newly synthesized pyrazolothiazole derivatives offer great potential as antimicrobial and anticancer agents.