Biological evaluation of benzosuberones

ABSTRACT

Introduction: Several natural products containing benzosuberone moiety are clinically reported as anti-tumor agents. Furthermore, several synthetic benzosuberones cited in this review exhibited wide range of theraputic activities such as bacteriostatic, anti-inflammatory, antidepressants and anti-tumor activities. Our recent review provides an overview of the different methods to synthesize the benzosuberones and their extensive biological activities.

Areas covered: Thirty-two patents among 130 references are cited in this review that covered the recent inhibitory activities of the benzosuberone scaffolds and their broad area of biological applications up to the first quarter of 2017. The areas covered included anti-inflammatory, antimicrobial, antitumor, selective estrogen receptor, anti-obesity, beta-amyloid production, enzymes and HCV inhibitors in addition to anti-Alzheimer and anti-tuberculosis activities as well as several receptors antagonists.

Expert opinion: It is important for medical and pharmaceutical researchers to prepare the first intensive review article concerning the highly biologically active benzosuberone derivatives where they are potent anti-inflammatory, immunosuppressive, antitumor activities and inhibitors of several enzymes. They are useful for treating abnormalities such as sleep disorders, eating disorders and reproductive disorders. Some of these compounds have potential as vascular disrupting agents to selectively target microvessels feeding tumors and some were potential leads for the development of promising therapeutic drugs.

KEYWORDS:

• Benzosuberones
• benzosuberan
• anti-inflammatory
• antitumor
• antimicrobial
• enzymes inhibitors

Article highlights

• Some benzosuberone-based natural products are clinically used as anti-tumor drugs.

• A number of synthetic benzosuberone derivatives are under clinical trials and some are potential leads for therapeutic drugs.

• More than 30 patents among 132 references are cited herein, covering broad-spectrum biological applications.

• Most of the covered areas included nanomolar inhibition of inflammations, tumors and enzymes.

• The collected data are of great interest for chemistry, medicinal and pharmaceutical researchers.

• Fusion of some heterocycles with the benzosuberone moiety led to high increase of their biological activities.

This box summarizes key points contained in the article.

Declaration of interest

The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Additional information

Funding

The financial support for this work was provided by the University of Kuwait through the research grant SC06/15.