Recent progress in biologically active indole hybrids: a mini review
Esraa Mahmoud1, Alaa M Hayallah2,3, Suzana Kovacic4
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Deraya University, Minia, Egypt.
Pharmacological Reports : PR
|May 20, 2022
Summary
This review explores novel indole-based hybrid compounds, highlighting their diverse biological activities. These synthesized molecules show promise for improved drug discovery and development, offering potential therapeutic benefits.
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
- Pharmacology
Background:
- Indole is a prevalent heterocyclic structure in natural products and biological systems.
- Indole derivatives exhibit a wide range of significant biological activities, including anticancer, antioxidant, and anti-inflammatory properties.
- The development of indole-based hybrids aims to enhance therapeutic efficacy and reduce adverse effects.
Purpose of the Study:
- To review newly synthesized indole-based hybrid compounds.
- To discuss the biological activities associated with these novel hybrids.
- To provide insights for drug discovery and development.
Main Methods:
- Literature review of recent synthetic strategies for indole-based hybrids.
- Compilation and analysis of reported biological activities of these compounds.
- Focus on hybrid structures like indole-coumarin, indole-chalcone, indole-isatin, and indole-pyrimidine.
Main Results:
- Identification of various indole-based hybrids with diverse pharmacological profiles.
- Demonstration of promising anticancer, antioxidant, anti-inflammatory, and antimicrobial activities.
- Highlighting the structure-activity relationships for optimized drug design.
Conclusions:
- Indole-based hybrids represent a valuable scaffold for developing new therapeutic agents.
- The reviewed compounds offer potential for improved drug candidates with enhanced activity and selectivity.
- Further research into these hybrids can accelerate drug discovery and development pipelines.
Related Concept Videos
02:31In-situ Hybridization
9.6K
In situ hybridization (ISH) is a technique used to detect and localize specific DNA or RNA molecules in cells, tissue, or tissue sections using a labeled probe. The technique was first used in 1969 for the investigation of nucleic acids. It is currently an essential tool in scientific research and clinical settings, especially for diagnostic purposes.
Types of probes and labels
A probe is a complementary strand of DNA or RNA that binds to corresponding nucleotide sequences in a cell. Many...
Types of probes and labels
A probe is a complementary strand of DNA or RNA that binds to corresponding nucleotide sequences in a cell. Many...
9.6K
01:29Diels–Alder Reaction Forming Bridged Bicyclic Products: Stereochemistry
4.8K
Diels–Alder reactions between cyclic dienes locked in an s-cis configuration and dienophiles yield bridged bicyclic products.
4.8K
01:27Inductive Effects on Chemical Shift: Overview
1.3K
The protons in unsubstituted alkanes are strongly shielded with chemical shifts below 1.8 ppm. Methine, methylene, and methyl protons appear at approximately 1.7, 1.2 and 0.7 ppm, while the proton signal from methane appears at 0.23 ppm. An electronegative substituent, such as chlorine, withdraws the electron density from the protons, increasing their chemical shift. Progressive substitution of the hydrogens in methane by chlorine shifts the proton signals increasingly downfield, to 3.05 ppm in...
1.3K
01:11Aryldiazonium Salts to Azo Dyes: Diazo Coupling
3.1K
The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the...
3.1K
01:11ortho–para-Directing Activators: –CH3, –OH, –NH2, –OCH3
6.4K
All ortho–para directors, excluding halogens, are activating groups. These groups donate electrons to the ring, making the ring carbons electron-rich. Consequently, the reactivity of the aromatic ring towards electrophilic substitution increases. For instance, the nitration of anisole is about 10,000 times faster than the nitration of benzene. The electron-donating effect of the methoxy group in anisole activates the ortho and para positions on the ring and stabilizes the corresponding...
6.4K
02:07FISH - Fluorescent In-situ Hybridization
21.8K
Fluorescence in situ hybridization, or FISH, was developed in the early 1980s and has quickly become one of the most widely used techniques in cytogenetics. Labeled probes are used to bind complementary DNA or RNA sequences on a chromosome or in a region within a cell. Earlier, the probes could only be obtained by cloning or reverse transcription of a DNA template. Currently, the probe oligonucleotides can be synthesized synthetically. Additionally, with the advancement of optical techniques,...
21.8K