Abstractβ‐Carboline nucleus is therapeutically valuable in medicinal chemistry for the treatment of varied number of diseases, most importantly cancer. The potent and wide‐ranging activity of β‐carboline has established them as imperative pharmacological scaffolds especially in the cancer treatment. Numerous derivatives such as Tetrahydro β‐carbolines, metal complexed β‐carbolines, mono, di and tri substituted β‐carbolines have been reported to possess dynamic anticancer activity. These different substituted β‐carboline derivatives had shown different mechanism of action and plays important role in anticancer drug discovery and development. The review is an update of the chemistry of β‐carbolines, both synthetic and natural origin acting through various targets against cancerous cells. In addition to this, studies of multitarget molecules designed by coupling β‐carbolines along with other mechanisms for treatment of neoplasm are also summarized.