Synthesis of isoxazole and isothiazole derivatives enhances carboplatin effectiveness in low doses, indicating potential for low-cytotoxicity cancer therapies.
In this study, the synthesis of a series of alkaloid analogs—isoxazole and isothiazole esters of 2-substituted 3-oxoindoline-4-carboxylic acid was performed. The target derivatives were obtained by the carbodiimide method. It was established that the studied esters have low cytotoxicity and are able to enhance the effect of the anticancer drug carboplatin, taken in low doses (0.5–5 μM), by up to 30%. Quantum chemical modeling of the obtained compounds and their conjugates with carboplatin was carried out to analyze the relationship between various calculated parameters and the observed biological effects.
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Mukusheva et al. (2026) studied this question.
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