Effects of Systematic Shortening of Noncovalent C8 Side Chain on the Cytotoxicity and NF-κB Inhibitory Capacity of Pyrrolobenzodiazepines (PBDs)

The systematic shortening of the noncovalent element of a C8-linked pyrrolobenzodiazepine (PBD) conjugate (13) led to the synthesis of a 19-member library of C8-PBD monomers. The critical elements of 13, which were required to render the molecule cytotoxic, were elucidated by an annexin V assay. The...

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Veröffentlicht in:	Journal of medicinal chemistry 2019-02, Vol.62 (4), p.2127-2139
Hauptverfasser:	Corcoran, David B, Lewis, Thomas, Nahar, Kazi S, Jamshidi, Shirin, Fegan, Christopher, Pepper, Chris, Thurston, David E, Rahman, Khondaker Miraz
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - metabolism Antineoplastic Agents - pharmacology Benzodiazepines - chemical synthesis Benzodiazepines - metabolism Benzodiazepines - pharmacology Cell Line, Tumor DNA - chemistry DNA - metabolism Drug Screening Assays, Antitumor Humans Molecular Docking Simulation Molecular Structure NF-kappa B - antagonists & inhibitors NF-kappa B - metabolism Pyrroles - chemical synthesis Pyrroles - metabolism Pyrroles - pharmacology Quantitative Structure-Activity Relationship
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