Thioquinazolinones are utilized in chemical synthesis of physiological significance and pharmacological utility. Thioquinazolinones are a large class of active chemical compounds exhibiting a broad spectrum of biological activities in animals as well as in humans. Research studies on thioquinazolinones reveals that the derivatives can be used in series of biological activities such as anti HIV, anticancer, antifungal, antibacterial, antimutagenic, anticoccidial, anticonvulsant, antiinflammatory, CNS depressant, antimalarial, antioxidant, antileukemic activity, antileishmanial activity. This review focused on the various biological activities of thioquinazolinones. The heterocyclic fused rings thioquinazoline have drawn a huge consideration owing to their expanded applications in the field of pharmaceutical chemistry. Thioquinazolinone are reported for their diversified biological activities and compounds with different substitutions bring together to knowledge of a target with understanding of the molecule types that might interact with the target receptors. Thioquinazolinones are an important chemical for the synthesis of various physiological significance and pharmacological utilized molecules. Thioquinazolinone are a large class of biologically active compounds that exhibited broad spectrum of biological activities such as anti-HIV, anticancer, antifungal, antibacterial, antimutagenic, anticoccidial, anticonvulsant, anti-inflammatory, antidepressant, antimalarial, antioxidant, antileukemic, and antileishmanial activities and other activities. Thioquinazolinone used as advantaged scaffold, the alteration is made with different substituent.