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

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship01:29

Cholinergic Antagonists: Chemistry and Structure-Activity Relationship

2.9K
Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic...
2.9K
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

2.3K
Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...
2.3K
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

1.1K
Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
1.1K
Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

1.9K
Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
1.9K
Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

4.0K
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...
4.0K
Prochirality02:05

Prochirality

5.2K
The concept of prochirality leads to the nomenclature of the individual faces of a molecule and plays a crucial role in the enantioselective reaction. It is a concept where two or more achiral molecules react to produce chiral products. A typical process is the reaction of an achiral ketone to generate a chiral alcohol. Here, the achiral reactant reacts with an achiral reducing agent, sodium borohydride, to generate an equimolar mixture of the chiral enantiomers of the product. For example, an...
5.2K

You might also read

Related Articles

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

Sort by
Same author

Response to: "A critical appraisal of principal component analysis of antiseizure medication-induced hostility/aggression and factor analysis of levetiracetam".

Epilepsy research·2026
Same author

Poly(vinyl alcohol) enhancing therapeutic effects of 4-l-boronophenylalanine on thoracic tumors in neutron capture therapy.

International journal of pharmaceutics·2025
Same author

Principal component analysis of antiseizure medication-induced hostility/aggression and factor analysis of levetiracetam using the food and drug administration adverse event reporting system.

Epilepsy research·2025
Same author

The Association between Molecular Initiating Events and Drug-Induced Hiccups.

Pharmaceuticals (Basel, Switzerland)·2024
Same author

[The New Generation of Particle Therapy Focused on Boron Element (Boron Neutron Capture Therapy; BNCT) -The World's First Approved BNCT Drug].

Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·2022
Same author

Elucidation of anti-HIV mechanism of sulfated cellobiose-polylysine dendrimers.

Carbohydrate research·2020

Related Experiment Video

Updated: Mar 6, 2026

Perturbing Endothelial Biomechanics via Connexin 43 Structural Disruption
09:20

Perturbing Endothelial Biomechanics via Connexin 43 Structural Disruption

Published on: October 4, 2019

6.0K

Quantitative Structure-Cytotoxicity Relationship of Chalcones.

Hiroshi Sakagami1,2, Yoshiko Masuda2, Mineko Tomomura2

  • 1Division of Pharmacology, Meikai University School of Dentistry, Sakado, Japan sakagami@dent.meikai.ac.jp.

Anticancer Research
|March 19, 2017
PubMed
Summary

Quantitative structure-activity relationship (QSAR) analysis identified a chalcone derivative with high tumor specificity, showing potential for new anticancer drug design. Further chemical modification of this lead compound is recommended.

Keywords:
ChalconesQSAR analysisanti-HIV activityapoptosis inductioncytotoxicitytumor selectivity

More Related Videos

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
05:17

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Published on: February 9, 2021

2.1K
In Silico Modeling Method for Computational Aquatic Toxicology of Endocrine Disruptors: A Software-Based Approach Using QSAR Toolbox
05:47

In Silico Modeling Method for Computational Aquatic Toxicology of Endocrine Disruptors: A Software-Based Approach Using QSAR Toolbox

Published on: August 28, 2019

14.7K

Related Experiment Videos

Last Updated: Mar 6, 2026

Perturbing Endothelial Biomechanics via Connexin 43 Structural Disruption
09:20

Perturbing Endothelial Biomechanics via Connexin 43 Structural Disruption

Published on: October 4, 2019

6.0K
Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
05:17

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay

Published on: February 9, 2021

2.1K
In Silico Modeling Method for Computational Aquatic Toxicology of Endocrine Disruptors: A Software-Based Approach Using QSAR Toolbox
05:47

In Silico Modeling Method for Computational Aquatic Toxicology of Endocrine Disruptors: A Software-Based Approach Using QSAR Toolbox

Published on: August 28, 2019

14.7K

Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Computational Chemistry

Background:

  • Chalcones are a class of compounds being investigated for biological activities.
  • Understanding structure-activity relationships is crucial for developing targeted therapies.

Purpose of the Study:

  • To perform quantitative structure-activity relationship (QSAR) analysis on fifteen chalcone derivatives.
  • To identify novel biological activities, specifically focusing on cytotoxicity and tumor specificity.

Main Methods:

  • Cytotoxicity was assessed using the MTT assay against oral cancer cell lines and normal oral cells.
  • Tumor specificity (TS) and potency-selectivity expression (PSE) were calculated.
  • Apoptosis markers were analyzed via western blot, and physicochemical parameters were computed.

Main Results:

  • One chalcone derivative exhibited high TS and PSE values, comparable to established anticancer drugs.
  • This compound induced apoptosis by stimulating poly(ADP-ribose) polymerase and caspase-3 cleavage.
  • Tumor specificity correlated with molecular shape and polarization, not substituent groups.

Conclusions:

  • The identified chalcone derivative shows promise as a lead compound for anticancer drug development.
  • Chemical modification of this lead compound could yield novel anticancer agents.
  • No anti-HIV activity was observed for the tested chalcones.