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Related Concept Videos

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.
Prodrugs help overcome...
Stereoisomerism02:52

Stereoisomerism

Isomerism in Complexes
Isomers are different chemical species that have the same chemical formula.
Transition metal complexes often exist as geometric isomers, in which the same atoms are connected through the same types of bonds but with differences in their orientation in space. Coordination complexes with two different ligands in the cis and trans positions from a ligand of interest form isomers. For example, the octahedral [Co(NH3)4Cl2]+ ion has two isomers (Figure 1) In the cis...
Phase II Reactions: Miscellaneous Conjugation Reactions01:19

Phase II Reactions: Miscellaneous Conjugation Reactions

Phase II biotransformations are detoxification mechanisms that conjugate xenobiotics with endogenous substances, neutralizing their toxicity.
A key example involves the conjugation of cyanide ions, which impair cellular respiration and alter hemoglobin into non-oxygen-carrying cyanmethemoglobin. To neutralize this threat, a sulfur atom from thiosulphate is transferred to the cyanide ion, catalyzed by the enzyme rhodanese, resulting in an inactive compound called thiocyanate. The production of...
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Drug Metabolism: Phase II Reactions01:14

Drug Metabolism: Phase II Reactions

Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
Drug Biotransformation: Overview01:16

Drug Biotransformation: Overview

Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...

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Related Experiment Video

Updated: May 26, 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

Pt(IV) complexes as prodrugs for cisplatin.

Yi Shi1, Shu-An Liu, Deborah J Kerwood

  • 1Department of Chemistry, Syracuse University, 111 College Place, CST, Rm 1-014, Syracuse, New York 13244-4100, USA.

Journal of Inorganic Biochemistry
|December 16, 2011
PubMed
Summary

Platinum(IV) complexes are reduced to platinum(II) to target DNA. Ascorbic acid reduction yields cisplatin, but glutathione reduction produces different platinum(II) products. Carbonate inhibits platinum binding to DNA.

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Last Updated: May 26, 2026

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

  • Inorganic Chemistry
  • Medicinal Chemistry
  • Biochemistry

Background:

  • Platinum(IV) complexes are investigated as prodrugs for cisplatin, relying on biological reduction to active platinum(II) species.
  • The reduction products of platinum(IV) complexes are known to interact with DNA, leading to antitumor effects.

Purpose of the Study:

  • To investigate the reduction products of oxoplatin and its carboxylate-modified analog using ascorbic acid (AsA) or glutathione (GSH).
  • To determine the effect of carbonate on the reduction and subsequent DNA-binding of these platinum complexes.

Main Methods:

  • Utilized pBR322 DNA to capture reduction products of platinum(IV) complexes.
  • Employed ((195))Pt NMR spectroscopy to confirm the formation of cisplatin and characterize platinum(II) products.
  • Investigated the impact of carbonate presence on platinum speciation and DNA binding using ((13))C NMR.

Main Results:

  • Ascorbic acid reduction of both platinum(IV) complexes yielded cisplatin, which bound to and unwound DNA, forming 1,2-intrastrand crosslinks.
  • Glutathione reduction did not produce cisplatin; the resulting platinum(II) products bound to DNA but exhibited different effects on DNA mobility.
  • The presence of physiological carbonate inhibited platinum binding to DNA by forming platinum(II) carbonato complexes.

Conclusions:

  • The choice of reducing agent significantly influences the platinum(II) species formed from platinum(IV) prodrugs.
  • Carbonate ions in biological systems can impede the DNA-binding efficacy of platinum-based anticancer drugs.
  • These findings provide crucial insights into the prodrug potential of platinum(IV) complexes and factors affecting their therapeutic activity.