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Recent Progress and Therapeutic Potential of Indole Hybrids Against Colorectal Cancer
Danchen Zhao1, Kesong Zhu1, Jie Mou1
1School of Pharmacy, Xianning Medical College, Hubei University of Science and Technology, Xianning, Hubei, China.
Abstract:
Colorectal cancer (CRC) represents one of the most prevalent and lethal malignancies worldwide, with rapidly increasing global incidence and mortality. Current clinical therapies for CRC are severely compromised by tumor metastasis, intrinsic and acquired drug resistance, and unsatisfactory prognosis for advanced patients, highlighting an urgent demand for novel and effective therapeutic candidates. As privileged multifunctional scaffolds, indole hybrids integrate diverse pharmacophores to achieve simultaneous modulation of multiple CRC-associated oncogenic signaling pathways and mutant proteins, enabling them to overcome the limitations of traditional single-target drugs, reduce systemic toxicity, and optimize pharmacokinetic performance. This review comprehensively summarizes the research progress of novel indole hybrids for anti-CRC therapy reported since 2021, excluding indole-pyrimidine and indole-pyridine hybrids covered in previous studies. Notably, among all summarized subclasses, indole-chalcone/chromene, indole-hydroxamic acid/benzamide, and indole-azole hybrids, show the most prominent and promising therapeutic outcomes. These three dominant hybrid categories display potent antiproliferative activity against both drug-sensitive and drug-resistant CRC cell lines, exert robust in vivo tumor growth inhibition in xenograft models, and possess favorable safety profiles with low cytotoxicity to normal cells. We systematically elaborate their key structure-activity relationships, core anti-CRC molecular mechanisms, including cell cycle arrest, apoptosis induction, and targeted pathway regulation, as well as superior preclinical pharmacological characteristics. Furthermore, the current challenges and future research directions for indole hybrid-based anti-CRC drug development are discussed.
Insights
Novel indole hybrids show significant promise for treating colorectal cancer (CRC), offering improved efficacy against drug-resistant tumors and reduced toxicity. These compounds represent a promising new avenue for CRC therapy development.
Area of Science:
- Medicinal Chemistry
- Oncology
- Pharmacology
Background:
- Colorectal cancer (CRC) is a leading cause of cancer death globally, with current treatments limited by metastasis and drug resistance.
- There is an urgent need for novel therapeutic strategies to improve outcomes for advanced CRC patients.
- Indole hybrids offer a multifunctional approach to target multiple cancer pathways simultaneously.
Purpose of the Study:
- To review recent advancements (since 2021) in indole hybrids for anti-colorectal cancer (CRC) therapy.
- To highlight promising subclasses, including indole-chalcone/chromene, indole-hydroxamic acid/benzamide, and indole-azole hybrids.
- To discuss structure-activity relationships, mechanisms of action, and preclinical pharmacological properties.
Main Methods:
- Comprehensive literature review of studies published since 2021 on indole hybrids for CRC therapy.
- Exclusion of indole-pyrimidine and indole-pyridine hybrids previously reviewed.
- Systematic analysis of structure-activity relationships, molecular mechanisms, and preclinical data.
Main Results:
- Indole-chalcone/chromene, indole-hydroxamic acid/benzamide, and indole-azole hybrids demonstrate potent antiproliferative activity against sensitive and resistant CRC cells.
- These hybrids exhibit significant in vivo tumor growth inhibition in xenograft models with favorable safety profiles.
- Key mechanisms include cell cycle arrest, apoptosis induction, and regulation of oncogenic signaling pathways.
Conclusions:
- Certain indole hybrid subclasses show significant therapeutic potential for colorectal cancer (CRC).
- These compounds offer advantages over traditional single-target drugs, including overcoming resistance and reducing toxicity.
- Further research into indole hybrid-based drug development is warranted, addressing current challenges and future directions.
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