Related Experiment Video

Updated: Jun 24, 2025

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

14.0K

Discovery of the Next-Generation Platinum-Based Anticancer Agents for Combating Oxaliplatin-Induced Drug Resistance

Ziru Sun1, Jianbin Han2, Jun Xu1

  • 1School of Pharmaceutical Science and Technology, Institute of Molecular Plus, Frontiers Science Center for Synthetic Biology (Ministry of Education of China), Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, Tianjin University, 92 Weijin Road, Nankai District, Tianjin 300072, P. R. China.

Journal of Medicinal Chemistry
|June 7, 2024
PubMed

Insights

Researchers developed new platinum(II)-complexes to overcome oxaliplatin resistance in colorectal cancer. Chiral Pt(II)-malonatoglycoconjugates effectively counteracted drug resistance, showing potent anticancer activity in vitro and in vivo.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Drug Discovery

Background:

  • Oxaliplatin is a key chemotherapy for advanced colorectal cancer.
  • Clinical resistance to oxaliplatin is a significant challenge, limiting treatment efficacy.
  • There is an unmet need for novel anticancer agents to overcome this resistance.

Purpose of the Study:

  • To develop a new generation of platinum(II)-based anticancer agents.
  • To address challenges posed by oxaliplatin-induced drug resistance.
  • To identify novel Pt(II)-complexes with superior antiresistance properties.

Main Methods:

  • Systematic screening of novel Pt(II)-complexes.
  • Quantitative structure-activity relationship (QSAR) study.
  • Evaluation of antiresistance activity against oxaliplatin-resistant colon cancer cells.

Main Results:

  • Ligand structure and chirality significantly influence antiresistance properties of Pt(II)-complexes.
  • Identified chiral R-binaphthyldiamine-ligated Pt(II)-malonatoglycoconjugates.
  • These novel conjugates demonstrated complete counteraction of oxaliplatin resistance.

Conclusions:

  • Chiral Pt(II)-malonatoglycoconjugates represent a promising new class of anticancer agents.
  • These compounds exhibit potent in vitro and in vivo efficacy against resistant colorectal cancer.
  • The findings offer a potential solution to overcome oxaliplatin resistance in cancer therapy.

More Related Videos

Author Spotlight: Unveiling the Role of TMOD3 in Platinum Resistance and Immune Infiltration in Ovarian Cancer09:40

Author Spotlight: Unveiling the Role of TMOD3 in Platinum Resistance and Immune Infiltration in Ovarian Cancer

Published on: August 2, 2024

2.6K
Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms08:46

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms

Published on: December 9, 2015

10.6K

Related Concept Videos

Treatment Resistant Cancers02:56

Treatment Resistant Cancers

Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...
3.3K
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
4.9K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
7.5K