The rapidly growing interest in the literature about the anticancer activity of 3,5-disubstituted pyrazolines and their promising therapeutic potentials/pharmacological properties, supported by the number of pyrazoline derivatives currently in clinical use or clinical trials, encouraged us to review the antiproliferative effects and biochemical investigations of probable mechanisms of action. Nevertheless, many reported pyrazoline-bearing compounds have anticancer activity without an explored mode of action, which opens new research avenues to examine their biochemical profiles further. Therefore, 3,5-disubstituted pyrazoline is a promising core that can be used to design new derivatives with anticancer activity based on the structure-activity relationship summarized in this review to obtain higher potency and selectivity.

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