β-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.
Keywords: anticancer; synthesis; tubulin; β‐Carboline.
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