Exploration of the carmaphycins as payloads in antibody drug conjugate anticancer agents

Antibody–drug conjugates (ADCs) represent a new dimension of anticancer chemotherapeutics, with warheads to date generally involving either antitubulin or DNA-directed agents to achieve low-to sub-nanomolar potency. However, other potent cytotoxins working by different pharmacological mechanisms are...

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Veröffentlicht in:	European journal of medicinal chemistry 2019-01, Vol.161, p.416-432
Hauptverfasser:	Almaliti, Jehad, Miller, Bailey, Pietraszkiewicz, Halina, Glukhov, Evgenia, Naman, C. Benjamin, Kline, Toni, Hanson, Jeffrey, Li, Xiaofan, Zhou, Sihong, Valeriote, Frederick A., Gerwick, William H.
Format:	Artikel
Sprache:	eng
Schlagworte:	4-Sulfonylaniline Amine basicity optimization Amines - chemistry Amines - pharmacology Aniline Compounds - chemistry Aniline Compounds - pharmacology Antibodies, Monoclonal - chemistry Antibodies, Monoclonal - pharmacology Antibody-drug conjugate Anticancer drugs Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Carmaphycins Cell Line, Tumor Cell Proliferation - drug effects Cell Survival - drug effects Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Humans Molecular Structure Oligopeptides - chemical synthesis Oligopeptides - chemistry Oligopeptides - pharmacology Proteasome Endopeptidase Complex - metabolism Proteasome inhibitors Proteasome Inhibitors - chemical synthesis Proteasome Inhibitors - chemistry Proteasome Inhibitors - pharmacology Structure-Activity Relationship
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