Beta-carboline is an indole alkaloid which has been identified as a valuable heterocyclic nucleus in the field of medicinal chemistry. It has different biological activities like antibacterial, anticancer, antifungal, antimalarial, antileishmanial, anti-HIV, anti-trypanosomal, and anti-toxoplosmal respectively in various medicinal compounds. The study of various potent beta-carboline derivatives and their synthetic aspects helps to design other potent derivatives for the effective treatment of multiple diseases like leishmaniasis, malaria, cancer, AIDS, tuberculosis, and bacterial and fungal infections. Incorporation of beta-carboline nucleus improves physiochemical and pharmacological properties. This review is mainly focused on various potential pharmacological active beta-carboline derivatives developed in the last twenty years with their synthetic aspects and structure activity relationship. It is helpful to synthetic chemists, drug designers, and medicinal chemists to design target-based new beta-carboline derivatives with good pharmacological activities in the future. © 2022 The Authors