ArticleChemMedChem2026
Polymethoxylated N-Carboranyl Isoquinolinones: A New Scaffold for ABCG2 Inhibitors.
Article in ChemMedChem, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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Who cites it
2 citing papers in PubMed.
- An Approach Toward Radioiodination and Radiopharmacological Evaluation of a Carborane-Containing Analog of Indomethacin.Molecules (Basel, Switzerland) · 2026Article
- Polymethoxylated N-Carboranyl Isoquinolinones: A New Scaffold for ABCG2 Inhibitors.ChemMedChem · 2026Article
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Authors and funding
6 authors.
Funding
Abstract
ABCG2-mediated multidrug resistance (MDR) is a major challenge among chemotherapeutic treatments of colon, pancreatic, and breast cancer, as well as leukemia. Clinical oncology seeks new adjuvant therapeutics to overcome MDR by developing potent but nontoxic ABCG2 inhibitors. Aided by computational docking analyses, based on known substrate and inhibitor structural motifs, a new isoquinolinone framework and several (poly)methoxylated derivatives were designed and synthesized. The novel carborane-containing N-carboranyl isoquinolinones were evaluated for cytotoxicity, ABCG2 inhibition, and reversal of MDR in combination with mitoxantrone (MXN) in an ABCG2-expressing Madin-Darby canine kidney II cell model. While the parental compound IC-1 showed strong ABCG2 inhibition, its 4-methoxyphenyl, 3,4-dimethoxyphenyl, and 3,4,5-trimethoxyphenyl derivatives (IC-4, IC-5, and IC-6) exhibited improved ABCG2 affinity. Nonsubstituted isoquinolinones IC-1 to IC-6 displayed higher solubility, lower toxicity, and similar ABCG2 inhibition and reversal of MXN resistance than 6,7-dimethoxy-isoquinolinone derivatives IC-7 to IC-11. Especially, the 4-methoxyphenyl- and 3,4-dimethoxyphenyl-substituted isoquinolinones (IC-10, IC-11) caused the strongest left shift of the MXN IC
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Registered trials
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