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Related Concept Videos

Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
Pharmacogenomics: Identification of New Drug Targets01:29

Pharmacogenomics: Identification of New Drug Targets

Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

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 its...
Chronopharmacokinetics: Time-Dependent Pharmacokinetics01:20

Chronopharmacokinetics: Time-Dependent Pharmacokinetics

Chronopharmacokinetics studies the temporal change in drug absorption and elimination. These changes can be cyclical or non-cyclical. Cyclical changes occur over a regular interval, while non-cyclical changes occur over a longer, irregular period.
Time-dependent pharmacokinetics refers to non-cyclical changes in drug rate processes over a period of time. It can lead to nonlinear pharmacokinetics, where the relationship between drug concentration and time is not proportional. Non-cyclical...
Clinical Trials: Overview01:11

Clinical Trials: Overview

Clinical development focuses on how the drug will interact with the human body and encompasses four key phases of clinical trials, each serving a specific purpose in assessing the safety and effectiveness of new drugs. These phases overlap and build upon one another. Phase I involves a small group of healthy volunteers (typically 20-80 individuals) or, in cases where significant toxicity is expected, patients with the targeted disease, such as cancer or AIDS. The volunteers are tested for...
Preclinical Development: Overview01:28

Preclinical Development: Overview

Preclinical development consists of a series of tests that ensure the safety and efficacy of a new therapeutic compound before it is tested in humans. There are four main phases to this process. First, safety pharmacology tests are conducted to ensure the drug does not produce any acutely harmful effects. These tests examine parameters such as bronchoconstriction, cardiac dysrhythmias, blood pressure changes, and ataxia. Next, preliminary toxicological testing is performed to determine the...

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Related Experiment Video

Updated: May 19, 2026

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System
05:10

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System

Published on: December 11, 2016

Macrocycles in new drug discovery.

Jamie Mallinson1, Ian Collins

  • 1Cancer Research UK Cancer Therapeutics Unit, Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey, UK.

Future Medicinal Chemistry
|August 4, 2012
PubMed
Summary

Drug-like macrocycles offer improved drug properties, enhancing potency and selectivity for challenging targets. This review explores macrocyclization

Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Organic Chemistry

Background:

  • Macrocycles, including natural products and synthetic derivatives, have a history of clinical utility.
  • There is growing interest in utilizing macrocyclic scaffolds in drug discovery for difficult targets.
  • Macrocyclization can address 'molecular obesity' by generating ligand-efficient molecules.

Purpose of the Study:

  • To review the impact of macrocyclization on drug potency, selectivity, and physicochemical properties.
  • To highlight recent advancements in macrocycle synthesis.
  • To provide an outlook on the future applications of macrocyclic scaffolds in medicinal chemistry.

Main Methods:

  • Literature review focusing on recent case histories in oncology drug discovery.

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Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
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Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery

Published on: May 16, 2021

Related Experiment Videos

Last Updated: May 19, 2026

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System
05:10

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System

Published on: December 11, 2016

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
06:26

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery

Published on: May 16, 2021

  • Analysis of the effects of macrocyclization on key drug properties.
  • Discussion of synthetic methodologies for macrocycle construction.

    • Main Results:

    • Macrocyclization can lead to favorable changes in biological and physicochemical properties.
    • Functionalized macrocyclic scaffolds can yield ligand-efficient molecules.
    • Recent case studies demonstrate the utility of macrocycles in oncology drug discovery.

    Conclusions:

    • Macrocyclic scaffolds represent a promising strategy for developing novel therapeutics.
    • Advances in synthesis are expanding the accessibility of macrocyclic compounds.
    • Macrocycles are poised for broader application in medicinal chemistry for challenging targets.