130107-96-9Relevant articles and documents
Macrocyclic pyrrolobenzodiazepine dimers as antibody-drug conjugate payloads
Donnell, Andrew F.,Zhang, Yong,Stang, Erik M.,Wei, Donna D.,Tebben, Andrew J.,Perez, Heidi L.,Schroeder, Gretchen M.,Pan, Chin,Rao, Chetana,Borzilleri, Robert M.,Vite, Gregory D.,Gangwar, Sanjeev
, p. 5267 - 5271 (2017)
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.
PYRROLOBENZODIAZEPINE CONJUGATES
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Page/Page column 139; 140, (2018/04/27)
A compound of formula (I) : (I) and its conjugates.
PYRROLOBENZODIAZEPINE CONJUGATES
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Page/Page column 99, (2017/09/05)
A conjugate of formula (I), wherein L is a Ligand unit, D is a Drug Linker unit of formula (II), wherein either: (a) R10 and R11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (b)