Discovery of new tricyclic spiroindole derivatives as potent P-glycoprotein inhibitors for reversing multidrug resistance enabled by a synthetic methodology-based library

Tao Yu; Rong Zeng; Yu Guan; Bin Pan; Hongwei Li; Jing Gu; Peng‐Fei Zheng; Qian Yan; Qin Ouyang

doi:10.1039/d4md00136b

January 1, 2024RSC Medicinal ChemistryOpen Access

Discovery of new tricyclic spiroindole derivatives as potent P-glycoprotein inhibitors for reversing multidrug resistance enabled by a synthetic methodology-based library

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Key Points

To identify novel tricyclic spiroindole derivatives from a methodology-based synthetic library that inhibit P-glycoprotein and reverse multidrug resistance in tumors.
Generated a focused chemical library of tricyclic spiroindole derivatives utilizing a targeted synthetic methodology.
Screened and evaluated the chemical library for inhibitory activity against P-glycoprotein.
Identified novel tricyclic spiroindole scaffolds functioning as potent P-glycoprotein inhibitors.
Provided a structural framework designed to reverse multidrug resistance and advance therapies for drug-resistant tumors.

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Implication

Preclinical study reveals novel tricyclic spiroindoles that inhibit P-glycoprotein in drug-resistant tumors, highlighting strategies to overcome multidrug resistance.

Abstract

P-gp inhibition. In conclusion, this study provides a novel skeleton that inspires the design of new P-gp inhibitors, laying the foundation for the treatment of drug-resistant tumors.

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Cite This Study

Yu et al. (2024) studied this question.

synapsesocial.com/papers/6a7e365c3a6a8ebbaf3991d5 https://doi.org/10.1039/d4md00136b

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Discovery of new tricyclic spiroindole derivatives as potent P-glycoprotein inhibitors for reversing multidrug resistance enabled by a synthetic methodology-based library

Key Points

Ask about this paper

Implication

Abstract

Discussion

Cite This Study

Discovery of new tricyclic spiroindole derivatives as potent P-glycoprotein inhibitors for reversing multidrug resistance enabled by a synthetic methodology-based library

Key Points

Ask about this paper

Implication

Abstract

Discussion

Cite This Study

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