Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Physical Properties of Amines01:26

Physical Properties of Amines

4.4K
Amines with low molecular weight are usually gaseous at room temperature, while those with high molecular weight are liquid or solids in nature. Usually, low molecular weight amines have a rotten fish-like smell. Diamines typically have a pungent smell. For instance, cadaverine and putrescine, depicted in Figure 1, are two molecules responsible for decaying tissue.
4.4K
Nomenclature of Aryl and Heterocyclic Amines01:10

Nomenclature of Aryl and Heterocyclic Amines

3.3K
The simplest aromatic amine is phenylamine, which contains an –NH2 functionality directly attached to an aromatic ring. The name aniline is designated for this skeleton. As shown in Figure 1, the common names of the functionalized anilines involve prefixes ortho-, meta-, and para- to indicate the substitution position. Different functionalized aniline derivatives also have notable trivial names.
3.3K
Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

4.1K
Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
4.1K
Basicity of Heterocyclic Aromatic Amines01:25

Basicity of Heterocyclic Aromatic Amines

7.1K
Heterocyclic amines, where the N atom is a part of an alicyclic system, are similar in basicity to alkylamines. Interestingly, the heterocyclic amine having a nitrogen atom as part of an aromatic ring has much less basicity than its corresponding alicyclic counterpart. For this reason, as presented in Figure 1, piperidine (pKb = 2.8) is significantly more basic than pyridine (pKb = 8.8).
7.1K
Antifungal Agents01:15

Antifungal Agents

20
Amphotericin B is a broad-spectrum antifungal agent that exploits structural differences between fungal and mammalian cell membranes. Its amphipathic structure—featuring a hydrophobic polyene-lactone ring and a hydrophilic region containing mycosamine and carboxylic acid groups—enables selective binding to ergosterol, a sterol predominantly found in fungal plasma membranes. This selective interaction underlies the drug’s antifungal activity, although weak binding to...
20
Structure of Amines01:19

Structure of Amines

3.4K
The hybridized nitrogen atom in amines possesses a lone pair of electrons and is bound to three substituents with a bond angle of around 108°, which is less than the tetrahedral angle of 109.5°. However, the C–N–H bond angle is slightly larger at 112°, with a carbon–nitrogen bond length of 147 pm. This carbon–nitrogen bond length of of amines is longer than the carbon–oxygen bond of alcohols (143 pm) but shorter than alkanes’ carbon–carbon bond (154 pm). These aspects are...
3.4K

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Machine Learning-Based Models to Predict Drug-Induced Liver Injury (DILI) to Assist Medicinal Chemistry.

Journal of medicinal chemistry·2026
Same author

Corrigendum to "Synthesis and biological evaluation of mixed aryl-alkyl succinates as modulators of autophagy and apoptosis in gastric carcinoma" [Bioorg. Chem. 179 (2026) 109997].

Bioorganic chemistry·2026
Same author

Where do we go from here? Current state of drug-target binding kinetics and a roadmap to their establishment in drug discovery campaigns.

Drug discovery today·2026
Same author

Combinatorial histone modifications direct ATP-dependent chromatin remodeling by NURF to promoter-proximal nucleosomes.

Nucleic acids research·2026
Same author

Synthesis and biological evaluation of mixed aryl-alkyl succinates as modulators of autophagy and apoptosis in gastric carcinoma.

Bioorganic chemistry·2026
Same author

Targeting RAD51-BRCA2 Interaction to Enhance Synthetic Lethality with Olaparib in Pancreatic Cancer: Development of a Novel Phenyl Furan-Quinoline-Carboxylic Acid Series.

ACS medicinal chemistry letters·2026
Same journal

LncRNA signature associated with amino acid metabolism: A novel prognostic tool for Clear Cell Renal Cell Carcinoma.

Current medicinal chemistry·2026
Same journal

HRI Kinase Modulation by BTdCPU as a Therapeutic Strategy for Bortezomib Resistance in Prostate Cancer.

Current medicinal chemistry·2026
Same journal

EGFR Dysregulation in Cancer: From Molecular Mechanisms and Key Mutations to Evolving TKI Strategies and Resistance Mitigation.

Current medicinal chemistry·2026
Same journal

DHRS2 as a Novel Thalidomide Target Regulating Mitophagy and Inflammation in Head and Neck Squamous Cell Carcinoma.

Current medicinal chemistry·2026
Same journal

Synthetic AtMP2 from Anabas testudineus: Comprehensive ADMET and In Vivo Toxicity Assessment to Enable Future Therapeutic Development.

Current medicinal chemistry·2026
Same journal

Screening of Medicinal and Edible Homology Substances for Diabetic Kidney Disease Based on GraphBAN.

Current medicinal chemistry·2026
See all related articles

Related Experiment Video

Updated: Mar 22, 2026

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
07:20

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents

Published on: May 28, 2014

14.6K

Diaryl Urea: A Privileged Structure in Anticancer Agents.

Laura Garuti1, Marinella Roberti, Giovanni Bottegoni

  • 1Department of Pharmacy and Biotechnology, University of Bologna, via Belmeloro 6, I-40126 Bologna, Italy. laura.garuti@unibo.it.

Current Medicinal Chemistry
|April 12, 2016
PubMed
Summary
This summary is machine-generated.

Diaryl ureas are key pharmacophores in anticancer drug design, enabling potent antitumor activity through favorable binding interactions. This review details their synthesis and highlights representative agents targeting kinases and signaling pathways.

More Related Videos

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies
08:54

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

Published on: February 17, 2023

1.6K
Regioselective O-Glycosylation of Nucleosides via the Temporary 2',3'-Diol Protection by a Boronic Ester for the Synthesis of Disaccharide Nucleosides
08:46

Regioselective O-Glycosylation of Nucleosides via the Temporary 2',3'-Diol Protection by a Boronic Ester for the Synthesis of Disaccharide Nucleosides

Published on: July 26, 2018

9.3K

Related Experiment Videos

Last Updated: Mar 22, 2026

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
07:20

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents

Published on: May 28, 2014

14.6K
Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies
08:54

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies

Published on: February 17, 2023

1.6K
Regioselective O-Glycosylation of Nucleosides via the Temporary 2',3'-Diol Protection by a Boronic Ester for the Synthesis of Disaccharide Nucleosides
08:46

Regioselective O-Glycosylation of Nucleosides via the Temporary 2',3'-Diol Protection by a Boronic Ester for the Synthesis of Disaccharide Nucleosides

Published on: July 26, 2018

9.3K

Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis
  • Pharmacology

Background:

  • Diaryl ureas are crucial pharmacophores in anticancer drug development, offering excellent hydrogen bonding capabilities.
  • This structural motif is found in successful drugs like sorafenib and various kinase inhibitors.
  • Diaryl ureas also function as ligands for the Hedgehog (Hh) signaling pathway.

Purpose of the Study:

  • To review synthetic methodologies for diaryl ureas.
  • To describe representative anticancer agents containing the diaryl urea moiety.
  • To analyze their receptor binding mechanisms and structure-activity relationships (SAR).

Main Methods:

  • Literature review of synthetic routes for diaryl ureas.
  • Analysis of published data on antitumor agents featuring diaryl ureas.
  • Examination of SAR and mechanism of action studies.

Main Results:

  • Diaryl ureas exhibit versatile binding modes, particularly in type II kinase inhibitors.
  • They are integral to compounds targeting RAF, KDR, and Aurora kinases.
  • Derivatives also show efficacy as Hedgehog pathway inhibitors.

Conclusions:

  • Understanding diaryl urea synthesis and SAR can guide the development of novel anticancer therapeutics.
  • This scaffold holds significant potential for designing more potent and selective antitumor agents.
  • Further research into diaryl urea derivatives may yield next-generation cancer treatments.