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• W2904256380 abstract "Uncialamycin analogs were evaluated as potential cytotoxic agents in an antibody-drug conjugate (ADC) approach to treating human cancer. These analogs were synthesized using Hauser annulations of substituted phthalides as a key step. A highly potent uncialamycin analog 3c with a valine-citrulline dipeptide linker was conjugated to an anti-mesothelin monoclonal antibody (mAb) through lysines to generate a meso-13 conjugate. This conjugate demonstrated subnanomolar potency (IC50 = 0.88 nM, H226 cell line) in in vitro cytotoxicity experiments with good immunological specificity to mesothelin-positive lung cancer cell lines. The potency and mechanism of action of this uncialamycin class of enediyne antitumor antibiotics make them attractive payloads in ADC-based cancer therapy." @default.
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• W2904256380 date "2019-02-01" @default.
• W2904256380 modified "2023-10-04" @default.
• W2904256380 title "Uncialamycin as a novel payload for antibody drug conjugate (ADC) based targeted cancer therapy" @default.
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• W2904256380 doi "https://doi.org/10.1016/j.bmcl.2018.12.021" @default.
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