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Development of indole hybrids for potential lung cancer treatment - part II
Shanshan Huang1, Zhi Xu2, Yafei Zhuang3
1School of Chemistry and Pharmaceutical Engineering, Huanghuai University, Zhumadian, Henan, China.
Abstract:
Lung cancer has become the most prevalent cancer for the past three decades, and the 5-years survival rate of lung cancer is only ~20% nowadays. Chemotherapy is the mainstay of lung cancer therapy, especially for non-small cell lung cancer. However, drug resistance represents a principal cause of therapeutic failure in non-small cell lung cancer leading to therapeutic insensitivity, tumor recurrence, and disease progression. Indole hybrids have the potential to conquer drug resistance, enhance efficacy, reduce adverse events, and improve pharmacokinetic properties due to their capacity to inhibit multiple targets simultaneously. Moreover, indole hybrids osimertinib, mobocertinib, cediranib, and vizimpro are currently applied in clinics for lung cancer therapy, demonstrating that indole hybrids are valuable scaffolds in the treatment and eradication of lung cancer. This review provides a comprehensive overview of the evolving landscape of indole hybrids with the in vitro and in vivo efficacy against lung cancer, and the structure-activity relationships as well as mechanisms of action are also discussed, covering articles published from 2021 onward.
Insights
Indole hybrids show promise in overcoming drug resistance in non-small cell lung cancer (NSCLC) therapy. This review explores their efficacy, structure-activity relationships, and mechanisms for improved lung cancer treatment.
Area of Science:
- Oncology
- Medicinal Chemistry
- Pharmacology
Background:
- Lung cancer remains a leading cause of cancer mortality globally, with poor survival rates.
- Chemotherapy is a primary treatment for non-small cell lung cancer (NSCLC), but drug resistance frequently leads to treatment failure.
- Developing novel therapeutic strategies is crucial to overcome resistance and improve patient outcomes.
Purpose of the Study:
- To provide a comprehensive overview of indole hybrids for lung cancer therapy.
- To discuss the in vitro and in vivo efficacy of indole hybrids against lung cancer.
- To explore structure-activity relationships and mechanisms of action for indole hybrids in lung cancer treatment.
Main Methods:
- Literature review of articles published from 2021 onward.
- Analysis of studies on indole hybrids' efficacy in lung cancer models.
- Examination of structure-activity relationships and mechanisms of action.
Main Results:
- Indole hybrids demonstrate potential in overcoming drug resistance in NSCLC.
- Several indole hybrids, including osimertinib and mobocertinib, are already in clinical use for lung cancer.
- Indole hybrids can inhibit multiple targets, enhancing therapeutic efficacy and potentially reducing adverse events.
Conclusions:
- Indole hybrids represent a valuable scaffold for developing new lung cancer therapies.
- Further research into indole hybrids could lead to improved treatment strategies for drug-resistant lung cancer.
- Understanding structure-activity relationships and mechanisms is key to optimizing indole hybrid-based drugs.
