A Review of the Structure-Activity Relationship of Natural and Synthetic Antimetastatic Compounds.

Liew Liew,Arshad Arshad,Nagoor Nagoor,Malagobadan Malagobadan

doi:10.3390/biom10010138

Abstract

There are innumerable anticancer compounds derived from either natural or synthetic origins. Many of these compounds have been further developed through structural modifications to not only inhibit cancer cell growth but also to exert an antimetastatic effect. This is achieved by attaching different substituents to generate different structure—activity relationships. This review highlights the effectiveness of different functional groups known to have antimigration and antiproliferation activities, such as fluoro, methoxy, methyl, amino, hydroxy, nitro, bromo, chloro, methylamino, ethoxy, carbonyl, iodo, and trifluoromethyl groups. Additionally, the positioning of these functional groups plays an important role in their anticancer activities, which was evident in one of our studies comparing analogues of a natural compound. Thus, this review suggests future recommendations for the design and development of improved anticancer drugs with higher efficacy.

Highlights

Cancer, a chronic disease, ranks in the top three leading cause of death worldwide [1]
An important hallmark of cancer progression, metastasis is a complex cascade of events that involves separation of cancer cells from the primary tumour followed by intravasation, extravasation and the eventual formation of secondary tumours [7]
Due to the high mortality rate in cancer caused by metastasis [8], the development of antimetastatic drugs has become a new aim in modern cancer therapy

Summary

Introduction

A chronic disease, ranks in the top three leading cause of death worldwide [1]. In the development of cancer treatment, natural and synthetic compounds have both been explored for their cytotoxicity [2]. More natural compounds have been discovered and reported for their anticancer activity, such as the epipodophyllotoxin derivatives, maytansine, bruceantin, thalicarpine, camptothecin, and lapachol [6]. Modification of these compounds has proven to be more effective in minimising side effects and targeting other oncogenic phenotypes, such as metastasis. Due to the high mortality rate in cancer caused by metastasis [8], the development of antimetastatic drugs has become a new aim in modern cancer therapy

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Results

Conclusion