Inolines have be significant compounds because of their diversity of applications in synthetic organic chemistry, pharmaceutical, industrial chemistry as well as they are present in several biologically active compounds in both natural and synthetic origins. In recent years there are high expectations that they exhibit interesting applications in selective potentiate the activity of β-lactam antibiotics in MRSA as well as other pharmacological arena, such as anticancer, anti-inflammatory, antioxidant, anticoagulant agents, etc. Furthermore, they are considered as substantial compounds due to their widespread use as building blocks and as chiral support in asymmetric synthesis. As a result, the existing events of the indoline-based nucleus in medicinal chemistry studies require to be collected and recognized especially many reports have been suggested that the indoline-based compounds have a very high therapeutic value (in MRSA) and needs to be explored for further studies. So, this review deals with the main innovations regarding indoline-based heterocycle scaffold stressing on their synthesis, reactions and their pharmacological activities.