Related Experiment Video
Updated: May 9, 2026

Facile Preparation and Photoactivation of Prodrug-Dye Nanoassemblies
Published on: February 17, 2023
Recent advances in small molecule prodrugs for cancer therapy
1School of Biological Science & Medical Engineering, Southeast University, Nanjing 210096, P.R. China. jimin@seu.edu.cn.
Abstract:
Chemotherapy has been performed to treat metastatic cancers but with varying degrees of success. The optimal potential of chemotherapy has not been achieved yet. Numerous compounds cannot be further developed to produce potent drugs because these compounds exhibit poor druggability. To resolve this issue, researchers developed prodrugs in drug discovery because these drugs can be efficiently used. Many small-molecule prodrugs have been designed and synthesized as anticancer agents for several years, and great progress has been achieved. In this study, recently developed, efficient anticancer prodrugs were reviewed, particularly small molecule prodrugs. Moreover, small molecule anticancer prodrugs were summarized according to different types of chemical structures and properties.
Insights
Researchers reviewed efficient anticancer prodrugs, focusing on small molecules. These prodrugs improve drug delivery and efficacy for metastatic cancers, overcoming poor druggability challenges in chemotherapy.
Area of Science:
- Oncology
- Medicinal Chemistry
- Drug Discovery
Background:
- Chemotherapy is a primary treatment for metastatic cancers, but its effectiveness is limited by poor drug druggability.
- Developing potent anticancer drugs is challenging due to the inability of numerous compounds to be effectively formulated or delivered.
- Prodrug strategies offer a solution by enhancing the delivery and efficacy of therapeutic agents.
Purpose of the Study:
- To review recently developed, efficient anticancer prodrugs.
- To focus on small-molecule prodrugs as a key area of advancement.
- To categorize and summarize these prodrugs based on chemical structure and properties.
Main Methods:
- Literature review of recent advancements in anticancer prodrug research.
- Identification and selection of efficient small-molecule anticancer prodrugs.
- Classification of prodrugs based on chemical structures and properties.
Main Results:
- Significant progress has been made in the design and synthesis of small-molecule prodrugs for cancer therapy.
- Various chemical structures and properties of efficient anticancer prodrugs have been identified and summarized.
- The review highlights the potential of prodrugs to overcome limitations of conventional chemotherapy.
Conclusions:
- Small-molecule prodrugs represent a promising strategy to enhance anticancer chemotherapy efficacy.
- Further development and application of these prodrugs can improve treatment outcomes for metastatic cancers.
- Understanding prodrugs' chemical diversity is crucial for future drug discovery efforts.
Related Concept Videos
Prodrugs
Prodrugs help overcome...
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Site-Targeted Drug Delivery Systems: Polymeric Carriers
Cancer Therapies
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
Combination Therapies and Personalized Medicine
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...