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Discovery and Development of Macrolides as Anticancer Agents
Rongli Liu1, Yani Hou1, Yijun Gu2
1Medical School, Xi'an Peihua University, Xi'an710125, Shaanxi, China.
Current Topics in Medicinal Chemistry
|July 28, 2021
Summary
Macrolides show promise as novel anticancer drugs, offering potential against drug-sensitive and resistant cancers. Research into their anticancer activity, structure-activity relationships, and mechanisms can lead to new cancer therapies.
Area of Science:
- Oncology
- Medicinal Chemistry
- Pharmacology
Background:
- Cancer incidence is rising due to lifestyle changes, necessitating novel therapeutic strategies.
- Chemotherapy faces challenges including drug resistance, side effects, and toxicity, limiting its efficacy.
- Macrolides, known for antibacterial properties, also exhibit anticancer potential against various cancer types.
Purpose of the Study:
- To review current advancements in macrolides concerning their anticancer activity.
- To explore structure-activity relationships of macrolides for cancer treatment.
- To elucidate the mechanisms of action of macrolides in cancer therapy.
Main Methods:
- Literature review of preclinical and clinical studies on macrolides and cancer.
- Analysis of structure-activity relationships to identify key pharmacophores.
- Examination of molecular targets and signaling pathways modulated by macrolides.
Main Results:
- Macrolides demonstrate efficacy against both drug-sensitive and drug-resistant cancer cell lines.
- Modulation of diverse cellular targets and signaling pathways contributes to macrolides' anticancer effects.
- Structure-activity relationship studies provide insights for rational drug design.
Conclusions:
- Macrolides represent a promising class of compounds for developing novel anticancer agents.
- Further research into macrolide anticancer activity and mechanisms can guide the development of effective cancer therapeutics.
- Rational design of macrolides holds potential for overcoming current chemotherapy limitations.
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