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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...
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.
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Drug Administration and Therapy Phases: Overview01:26

Drug Administration and Therapy Phases: Overview

Drugs, the chemical agents used in diagnosing, treating, or preventing diseases, undergo a four-phase process of development: pharmaceutic, pharmacokinetics, pharmacodynamics, and therapeutic.
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Drug Metabolism: Phase I Reactions01:17

Drug Metabolism: Phase I Reactions

A phase I reaction is a biochemical process that introduces a functionally reactive polar group to a substance. This transformation predominantly occurs in the liver, facilitated by the cytochrome P450 system of hemoproteins situated in the lipophilic endoplasmic reticulum of cells. The metabolite generated through this process can have varying polarities. If it is sufficiently polar, it can be easily excreted in the urine due to its water compatibility. However, if the metabolite is nonpolar,...
Prodrugs01:30

Prodrugs

Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
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Related Experiment Video

Updated: Jul 8, 2026

Solid-phase Synthesis of [4.4] Spirocyclic Oximes
05:15

Solid-phase Synthesis of [4.4] Spirocyclic Oximes

Published on: February 6, 2019

Function-oriented synthesis, step economy, and drug design.

Paul A Wender1, Vishal A Verma, Thomas J Paxton

  • 1Department of Chemistry, Stanford University, Stanford, California 94305-5080, USA.

Accounts of Chemical Research
|December 28, 2007
PubMed
Summary
This summary is machine-generated.

Function-oriented synthesis (FOS) creates simplified, effective therapeutic leads from complex natural products. This approach enhances drug properties and enables practical, step-economical synthesis for novel treatments.

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Last Updated: Jul 8, 2026

Solid-phase Synthesis of [4.4] Spirocyclic Oximes
05:15

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Published on: February 6, 2019

Discovery and Synthesis Optimization of Isoreticular Al(III) Phosphonate-Based Metal-Organic Framework Compounds Using High-Throughput Methods
07:20

Discovery and Synthesis Optimization of Isoreticular Al(III) Phosphonate-Based Metal-Organic Framework Compounds Using High-Throughput Methods

Published on: October 6, 2023

Area of Science:

  • Medicinal Chemistry
  • Synthetic Organic Chemistry
  • Drug Discovery

Background:

  • Natural product leads offer therapeutic promise but often face challenges in sourcing, synthesis complexity, and suboptimal drug properties.
  • Existing natural products may be scarce, difficult to synthesize at scale, or not ideally suited for human therapeutic applications.

Purpose of the Study:

  • To provide an overview of function-oriented synthesis (FOS) and its application in developing simplified, therapeutically relevant analogs of natural products.
  • To highlight how FOS facilitates synthetic innovation and the creation of novel drug candidates with improved functions.

Main Methods:

  • Application of FOS principles to redesign complex natural product scaffolds into simpler, synthetically accessible structures.
  • Design and synthesis of analogs for natural products like bryostatin and laulimalide, focusing on improved therapeutic efficacy and practicality.
  • Development of novel drug delivery systems using FOS to enhance cellular and tissue uptake.

Main Results:

  • Simplified bryostatin analogs demonstrated superior anticancer activity and improved cognition/memory effects compared to the natural product.
  • Synthesized laulimalide analogs addressed availability and stability issues, retaining efficacy against multidrug-resistant cancer cell lines.
  • Developed advanced drug transporters via FOS, outperforming natural cell-penetrating peptides in delivery efficiency and synthetic accessibility.

Conclusions:

  • FOS enables the translation of complex natural product leads into simplified analogs with enhanced therapeutic functions and improved synthetic feasibility.
  • This strategy allows for the development of synthetically innovative approaches to novel, therapeutically valuable molecules.
  • FOS provides a practical pathway for creating next-generation therapeutics with superior performance and manufacturability.