Novel LAT1-targeted Chlorambucil Conjugates

Just published article reports synthesis and evaluation of novel LAT1-tareted amino acid conjugates of a known anti-cancer agent, chlorambucil. Two conjugates were synthetized by coupling chlorambucil with the aromatic ring of phenylalanine via amide and ester bond. Compounds were evaluated for their affinity to LAT1 and their uptake in vitro using a human breast canver cell linen MCF-7.The cellular uptake of conjugates were significantly higher tahan uptake of chlorabucil, and the conjugates showed higher cytotoxicity than the parent drug.

Research was carried out in collaboration with the Prodrug research group at University of Eastern Finland and the Division of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Khon Kaen University.

The research was published in The International Journal of Molecular Sciences.

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