Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters
3 years ago

Macrocyclic pyrrolobenzodiazepine dimers as antibody-drug conjugate payloads

Macrocyclic pyrrolobenzodiazepine dimers as antibody-drug conjugate payloads
Macrocyclic pyrrolobenzodiazepine dimers were designed and evaluated for use as antibody-drug conjugate payloads. Initial structure–activity exploration established that macrocyclization could increase the potency of PBD dimers compared with non-macrocyclic analogs. Further optimization overcame activity-limiting solubility issues, leading to compounds with highly potent (picomolar) activity against several cancer cell lines. High levels of in vitro potency and specificity were demonstrated with an anti-mesothelin conjugate.

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X17310132

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