Epothilones as Natural Compounds for Novel Anticancer Drugs Development
Cecilia Villegas1, Iván González-Chavarría2, Viviana Burgos3,4
1Laboratory of Natural Products & Drug Discovery, Center CEBIM, Department of Basic Sciences, Universidad de La Frontera, Temuco 4811230, Chile.
International Journal of Molecular Sciences
|April 13, 2023
Summary
Epothilones are natural compounds effective against cancer, acting similarly to paclitaxel but overcoming resistance. New derivatives show promise for treating refractory tumors, including triple-negative breast cancer.
Area of Science:
- Natural Products Chemistry
- Oncology
- Pharmacology
Background:
- Epothilones are cytotoxic macrolides from *Sorangium cellulosum*.
- They exhibit anti-cancer properties by inducing tubulin polymerization and apoptosis.
- Epothilones demonstrate low susceptibility to tumor resistance mechanisms, unlike paclitaxel.
Purpose of the Study:
- To review epothilone research against cancer from 2010-2022.
- To evaluate preclinical and clinical outcomes of epothilone derivatives.
- To explore novel synthetic strategies for improved epothilone-based therapies.
Main Methods:
- Literature review of preclinical and clinical studies (2010-2022).
- Analysis of epothilone mechanisms of action and resistance profiles.
- Evaluation of synthetic strategies for new epothilone derivatives.
Main Results:
- Epothilones are superior to paclitaxel against many refractory tumors.
- Ixabepilone and utidelone are clinically used, improving triple-negative breast cancer treatment.
- New derivatives show enhanced activity against refractory tumors compared to existing drugs.
Conclusions:
- Epothilones offer a promising therapeutic avenue for refractory cancers.
- Further development of novel epothilone derivatives and delivery systems is warranted.
- Combination therapies involving epothilones show significant clinical benefit, particularly for TNBC.
Keywords:
anticancer agentsclinical trialscytotoxicityepothilone derivatesepothilonesrefractory cancertaxanesMore Related Videos
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