What question did this study set out to answer?

To explore enzymatic diversification of rapamycin and evaluate its anticancer effects.

February 26, 2026

Enzymatic C42 Diversification of Rapamycin Identifies a Potent Butyryl-Modified Anticancer Derivative

Q: What does this research mean for the field?

Derivative 9 of rapamycin exhibits superior antiproliferative activity with an IC50 of 6.5 μM in ACHN cells, outperforming both rapamycin and temsirolimus. Novelty: ClaimNovelty.NOVEL_FINDING. Consensus alignment: ConsensusAlignment.NEUTRAL.

Key Points

To explore enzymatic diversification of rapamycin and evaluate its anticancer effects.
Used lipase-catalyzed method for regioselective modification of rapamycin at C42 position.
Screened derivatives for biological activity against cancer cell lines (ACHN).
Identified and characterized 10 new rapamycin derivatives.
Derivative 9 demonstrated significant antiproliferative activity (IC50 = 6.5 μM) in ACHN cells.
Derivative 9 outperformed original rapamycin and temsirolimus in biological testing.
Four novel derivatives were created in this study, offering new potential leads.

Abstract

A highly regioselective, one-step lipase-catalyzed method enabled the diversification of rapamycin at its C42 position, producing 10 derivatives (4 novel). Biological screening identified derivative 9 as a potent lead compound with superior antiproliferative activity (IC50 = 6.5 μM in ACHN cells), outperforming both rapamycin and temsirolimus. This work offers a practical enzymatic route for rapamycin remodeling and highlights a promising mTOR-targeted anticancer candidate.

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Cite This Study

Liu et al. (Tue,) studied this question.

synapsesocial.com/papers/699fe3d995ddcd3a253e7d3d https://doi.org/https://doi.org/10.1021/acs.orglett.6c00072

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