Key Heterocyclic Cores for Smart Anticancer Drug–Design Part II

Understanding Promising Anticancer Targets for Heterocyclic Leads: An Introduction

Author(s): Shweta Sharma, Mymoona Akhter and Rajesh Kumar Singh * .

Pp: 1-34 (34)

DOI: 10.2174/9789815040043122020004

* (Excluding Mailing and Handling)


With the second-highest cause of mortality in the world, cancer becomes a major threat around the globe. In the last few decades, heterocyclic compounds, obtained naturally or synthetically, have been developed as a potential scaffold for developing many anticancer drugs. Heterocyclic compounds due to heteroatoms such as oxygen, nitrogen and sulphur can be employed as hydrogen bond donors as well as acceptors. Thus, they can bind suitably to pharmacological targets and receptors via intermolecular H-bonds more effectively, giving pharmacological effects. They can also alter liposolubility, hence the aqueous solubility of drug molecules to achieve remarkable pharmacotherapeutic properties. These heterocyclic leads exert the anticancer activity by a distinctive mechanism such as inhibiting Bcl-2, Mcl-1 proteins (induce apoptosis), inhibiting PIM proteins (hinder the cellular process and signal transduction in cells), inhibiting DNA topoisomerase, inhibiting aromatase (inhibit replication and transcription), modulating epigenetic mechanisms (inhibit histone deacetylase/HDAC) and inhibiting cellular mitosis (tubulin inhibitors).The current chapter aims to describe these promising anticancer targets. The novel targets are also illustrated with a pictorial presentation to understand heterocyclic drugs action on various cancer targets. This chapter will facilitate researchers, pharmacologists, and medicinal chemists in the understanding mechanism of heterocyclic drugs, which can help develop new anticancer agents.

Keywords: Anticancer, Apoptosis, Aromatase inhibitors, HDAC, Mitosis, Topoisomerase inhibitors, Tubulin inhibitors.

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