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Catharanthine C16 substituent effects on the biomimetic coupling with vindoline: preparation and evaluation of a key series of vinblastine analogues.

Author: BogerDale L, GotohHiroaki, RobertsonWilliam M, TamAnnie

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Overview

The presence of an electron-withdrawing substituent at the C16 position of catharanthine is essential for its cytotoxic activity. The C16 methyl ester plays a unique role in this activity.
Paper Details　
Original Abstract of the Article :
The examination of the catharanthine C16 substituent effects on the Fe(III)-promoted biomimetic coupling reaction with vindoline is detailed, confirming the importance of the presence of a C16 electron-withdrawing substituent, and establishing an unanticipated unique role (>10-fold) that the C16 met...See full text at original site
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引用元：
https://pubmed.ncbi.nlm.nih.gov/20932748

データ提供：米国国立医学図書館（NLM）

Fine-Tuning Vinblastine Analogues: A Quest for Enhanced Anticancer Activity

The development of effective anticancer drugs is a continuous process of refinement. This study investigates the impact of modifications to the structure of catharanthine, a compound found in the Madagascar periwinkle plant, on its ability to bind to vindoline, another important anticancer compound. The authors explore the potential of these structural changes to create more potent vinblastine analogues, which are promising anticancer agents.

Unlocking the Potential of Vinblastine Analogues

The study demonstrates that subtle modifications to the structure of catharanthine can significantly influence its binding affinity to vindoline and ultimately affect the potency of the resulting vinblastine analogues. The authors identified key structural features that contribute to the effectiveness of these compounds, providing valuable insights for the design of future anticancer agents.

The Promise of Precision Medicine in Cancer Treatment

This research exemplifies the power of precision medicine in cancer treatment. Just as a desert explorer meticulously charts a course to reach a specific destination, researchers are carefully tailoring the structures of anticancer drugs to achieve maximum efficacy while minimizing side effects. This study highlights the importance of precision medicine in the development of more effective and targeted treatments for cancer.

Dr.Camel's Conclusion

This research underscores the significance of structural optimization in the design of anticancer drugs. By understanding the subtle nuances of molecular interactions, researchers can create more potent and specific therapies, offering new hope for cancer patients. This study is a testament to the ongoing efforts in the field of cancer research, where every step closer to understanding the disease brings us closer to effective treatments.
Date :
  1. Date Completed 2011-03-29
  2. Date Revised 2021-10-20
Further Info :

Pubmed ID

20932748

DOI: Digital Object Identifier

NIHMS238175

Related Literature

Article Analysis
・Effects of vinblastine
SNS
PICO Info
in preparation
Languages

English

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