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Nucleophilic Aromatic Substitution: Elimination–Addition

Nucleophilic Aromatic Substitution: Elimination–Addition

Simple aryl halides do not react with nucleophiles. However, nucleophilic aromatic substitutions can be forced under certain conditions, such as high temperatures or strong bases. The mechanism of substitution under such conditions involves the highly unstable and reactive benzyne intermediate. Benzyne contains equivalent carbon centers at both ends of the triple bond, each of which is equally susceptible to nucleophilic attack. This 50–50 distribution of products is confirmed through isotopic...

Sedatives and Hypnotics Drugs: Benzodiazepines

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Benzodiazepines have both sedative and hypnotic properties. They include compounds such as diazepam (Valium) and alprazolam (Xanax). Structurally, their cores are similar, consisting of the fusion of a benzene ring and a diazepine ring, but they share a common mechanism of action in the central nervous system (CNS).
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Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
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When more than one substituent is present on the benzene ring, the IUPAC nomenclature depends on the number of substituents present.
For disubstituted benzene derivatives, with two groups attached to the benzene ring, three constitutional isomers are possible. For example, consider dimethyl benzene, often called xylene, where the second methyl group can be substituted at the second, third, or fourth carbon. The relative position of the substituents is represented by prefixes ortho, meta, or...

Anxiolytic Drugs: Benzodiazepines and Buspirone

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Benzodiazepines are a class of anxiolytic drugs known for their rapid efficacy and high therapeutic-to-lethal dose ratio, but with a potential risk of drug dependence. These drugs are lipophilic, allowing for rapid absorption after oral administration, eventually reaching the central nervous system (CNS). Once in the CNS, benzodiazepines bind to the allosteric site of the GABAA receptor. This binding enhances the inhibitory effects of the neurotransmitter GABA. By doing so, they prevent...

Directing and Steric Effects in Disubstituted Benzene Derivatives

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When disubstituted benzenes undergo electrophilic substitution, the product distribution depends on the directing effect of both substituents. When the directing effects of both substituents reinforce each other, a single product is obtained. For example, bromination of p-nitrotoluene occurs ortho to the methyl group and meta to the nitro group, which is the same position, resulting in a single product. However, if the directing effects of the two groups oppose each other, the more strongly...

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Diagonal Method to Measure Synergy Among Any Number of Drugs

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Published on: June 21, 2018

Recent Overview on the Molecular Hybrids Integrated With Benzosuberone/Benzo[7]annulene Derivatives as Multi-Target

Mohamed S Nafie^1,2,3, Kamal M Dawood⁴, Mohamed K Diab⁵

¹Department of Chemistry, College of Sciences, University of Sharjah, Sharjah, UAE.

Archiv Der Pharmazie

|July 16, 2026

Summary

Benzosuberone derivatives show potent anticancer activity against breast, lung, and colon cancers. These compounds also exhibit diverse biological activities, highlighting their therapeutic potential.

Keywords:

benzo[7]annulene benzosuberone kinase inhibition molecular hybrids topoisomerase II inhibitors

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Efficient Synthesis of Polyfunctionalized Benzenes in Water via Persulfate-promoted Benzannulation of α,β-Unsaturated Compounds and Alkynes

Efficient Synthesis of Polyfunctionalized Benzenes in Water via Persulfate-promoted Benzannulation of α,β-Unsaturated Compounds and Alkynes

Published on: December 16, 2019

Area of Science:

Medicinal Chemistry
Pharmacology
Drug Discovery

Background:

Benzosuberone is a scaffold with diverse pharmacological properties.
Significant interest exists in developing benzosuberone derivatives as anticancer agents.

Purpose of the Study:

To review the historical interest, chemical diversity, and medicinal applications of benzosuberone derivatives.
To explore the structure-activity relationships of benzosuberone hybrids for anticancer and other biological activities.

Main Methods:

Investigated molecular hybrids of benzosuberone with various functionalities and heterocycles.
Performed in vitro analyses to assess cytotoxicity against cancer cell lines and normal cells.
Reviewed existing literature on benzosuberone derivatives and their biological activities.

Main Results:

Benzosuberone derivatives demonstrated significant cytotoxicity against breast, lung, and colon cancer cell lines (low micromolar and submicromolar IC50 values).
These derivatives exhibited a broad spectrum of biological activities, including antimicrobial, antiviral, neurological, antiparasitic, anti-diabetic, and antitubercular effects.
Low toxicity profiles were observed in normal cells, indicating a favorable safety margin.

Conclusions:

The benzosuberone scaffold is a privileged structure for developing novel therapeutic agents.
Hybrid molecules, combinatory therapy, and nano-formulations are promising strategies for advancing benzosuberone derivatives towards clinical applications.