Indole Hybrids With Therapeutic Potential Against Drug-Resistant Cancers: An Update (2021-2025)

Xiaoyu Li1, Feng Wang1, Lin Xie1

  • 1Department of Radiation Oncology, Chongqing University Cancer Hospital, Chongqing, China.

Archiv Der Pharmazie
|November 26, 2025
PubMed

Insights

New indole hybrids show promise for overcoming drug-resistant cancers, offering hope for improved patient outcomes and reduced healthcare burdens. This review covers recent advances in their development and mechanisms of action.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Drug Discovery

Background:

  • Drug-resistant cancer presents a significant challenge in clinical treatment, leading to adverse outcomes and increased healthcare costs.
  • Indole derivatives are recognized as effective anticancer scaffolds due to their multitargeted therapeutic properties.
  • Indole hybrids are particularly effective in combating drug resistance by employing multitargeted strategies.

Purpose of the Study:

  • To review the therapeutic potential of indole hybrids against drug-resistant cancers.
  • To cover literature published on indole hybrids since 2021.
  • To discuss structure-activity relationships and mechanisms of action for future drug design.

Main Methods:

  • Comprehensive literature search for indole hybrids and drug-resistant cancer research published since 2021.
  • Analysis of structure-activity relationships (SAR) of identified indole hybrids.
  • Evaluation of the mechanisms of action (MoA) of promising indole hybrid candidates.

Main Results:

  • Indole hybrids demonstrate significant potential in overcoming various drug resistance mechanisms in cancer.
  • Recent studies highlight novel indole hybrid structures with enhanced efficacy and targeted action.
  • Key structure-activity relationships and mechanisms of action have been elucidated for several indole hybrids.

Conclusions:

  • Indole hybrids represent a promising class of compounds for developing novel chemotherapeutics against resistant cancers.
  • Further research into SAR and MoA will facilitate the rational design of next-generation indole hybrid anticancer agents.
  • The findings support the continued investigation of indole hybrids to address the unmet need for effective cancer treatments.

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