Phytochemicals play crucial role in inhibiting key enzymes involved in HIV-1 replication. Repurposing of phytochemical based anti-HIV drug discovery through cross screening approaches and modern techniques is essential to provide better leads. Anti-HIV leads translated through phytochemicals could overcome current challenges of HIV therapy. Considering the immense potential of phytochemicals, this article summarizes the present status of the research carried out on their anti-HIV activities, with its limitations and future directions to foster drug discovery.