Benzophenone: a ubiquitous scaffold in medicinal chemistry

Abstract

The benzophenone scaffold represents a ubiquitous structure in medicinal chemistry because it is found in several naturally occurring molecules which exhibit a variety of biological activities, such as anticancer, anti-inflammatory, antimicrobial, and antiviral. In addition, various synthetic benzophenone motifs are present in marketed drugs. They also represent important ingredients in perfumes and can act as photoinitiators. This review will provide an overview of benzophenone moieties with medicinal aspects synthesized in the last 15 years and will cover the most potent molecule in each report. In this review, only benzophenones with substitutions on their aryl rings, i.e. diphenyl ketone analogues, have been covered.

Fig. 1. Representative examples of naturally occurring benzophenones.

Fig. 2. Representative examples of benzophenone drugs.

Fig. 3. Various synthetic strategies for the synthesis of benzophenones.

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Fig. 4. 2,2′-Hydroxybenzophenones and their N-acyl hydrazone derivatives as anti-tumor agents.

Fig. 5. A diamide-coupled benzophenone derivative as a potent anti-cancer agent.

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Fig. 6. Morpholine-conjugated benzophenones as potent anti-cancer agents.

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Fig. 7. Benzophenone and uracil hybrids as potent anti-HIV-1 agents.

Fig. 8. Benzophenone derivatives with amide linkers as potent anti-HIV-1 agents.

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Fig. 9. O-Prenyl derivatives of benzophenone with leishmanicidal activity.

Fig. 10. 2,4-Diaminobenzophenone scaffolds as FTase inhibitors.

Fig. 11. Benzophenone-containing tetraamides as potent antimicrobial agents.

Fig. 12. Benzophenones with a furamide linkage as antihyperlipidemic agents.

Khemchand Surana

Bharatkumar Chaudhary

Monika Diwaker

Satyasheel Sharma