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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Review Article

A Medicinal Chemist’s Perspective Towards Structure Activity Relationship of Heterocycle Based Anticancer Agents

Author(s): Bhupender Nehra, Bijo Mathew and Pooja A. Chawla*

Volume 22, Issue 6, 2022

Published on: 11 January, 2022

Page: [493 - 528] Pages: 36

DOI: 10.2174/1568026622666220111142617

Price: $65


Aim: This paper aims to describe the structure activity relationship of heterocyclic derivatives with multi-targeted anticancer activity.

Objectives: With the following goals in mind, this review tries to describe significant recent advances in the medicinal chemistry of heterocycle-based compounds: (1) To shed light on recent literature focused on heterocyclic derivatives' anticancer potential; (2) To discuss recent advances in the medicinal chemistry of heterocyclic derivatives, as well as their biological implications for cancer eradication; (3) To summarise the comprehensive correlation of structure activity relationship (SAR) with pharmacological outcomes in cancer therapy.

Background: Cancer remains one of the major serious health issues in the world today. Cancer is a complex disease in which improperly altered cells proliferate at an uncontrolled, rapid, and severe rate. Variables such as poor dietary habits, high stress, age, and smoking, can all contribute to the development of cancer. Cancer can affect almost any organ or tissue, although the brain, breast, liver, and colon are the most frequently affected organs. For several years, surgical operations and irradiation have been in use along with chemotherapy as a primary treatment of cancer, but still, effective treatment of cancer remains a huge challenge. Chemotherapy is now considered one of the most effective strategies to eradicate cancer, although it has been shown to have a number of cytotoxic and unfavourable effects on normal cells. Despite all of these cancer treatments, there are several other targets for anticancer drugs. Cancer can be effectively eradicated by focusing on these targets, including cell-specific and receptor-specific targets such as tyrosine kinase receptors (TKIs). Heterocyclic scaffolds also have a variety of applications in drug development and are a common moiety in the pharmaceutical, agrochemical, and textile industries.

Methods: The association between structural activity relationship data of many powerful compounds and their anticancer potential in vitro and in vivo has been studied. SAR of powerful heterocyclic compounds can also be generated using molecular docking simulations, as reported in literature.

Conclusion: Heterocycles have a wide range of applications, from natural compounds to synthesised derivatives with powerful anticancer properties. To avoid cytotoxicity or unfavourable effects on normal mammalian cells due to a lack of selectivity towards the target site, as well as to reduce the occurrence of drug resistance, safer anticancer lead compounds with higher potency and lower cytotoxicity are needed. This review emphasizes on design and development of heterocyclic lead compounds with promising anticancer potential.

Keywords: Heterocycles, Anticancer, SAR, Cytotoxicity, Docking studies, Mammalian cells.

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