140647-01-4Relevant articles and documents
VISUAL DETECTION OF PBD INDUCED DNA CROSSLINKS
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, (2021/04/23)
The present invention relates to the field of oncology, laboratory tools and methods, and especially anti-tumor DNA crosslinking agents. Most patients with advanced solid tumors develop resistance to chemotherapy due to the ability of cancer cells to repair or tolerate sustained DNA damages. The inventors showed that the compounds according to the present invention allow the detection and visualization of alkylated DNA damages induced by PBDs without altering their DNA crosslinking ability. This enables the study of the effect and properties of PBDs. In particular, the present invention relates new derivates of PBD molecules and their synthesis. The present invention also relates to a method for visualizing DNA crosslinking; to a method for assessing the resistance of a tumor to a crosslinking agent and to a method for identifying a molecule or treatment for improving the efficiency of a crosslinking agent.
FUSED HETEROCYCLIC BENZODIAZEPINE DERIVATIVES AND USES THEREOF
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, (2020/05/29)
The present disclosure provides compounds and compositions capable of extending lifespan, and methods of use thereof.
New approaches to pyrrolo[2,1-c][1,4]benzodiazepines: Synthesis, DNA-binding and cytotoxicity of DC-81
Bose, D. Subhas,Jones, Gary B.,Thurston, David E.
, p. 751 - 758 (2007/10/02)
Two routes to the naturally occuring DNA-binding antitumor antibiotic DC-81 are described, one of which involves a novel cyclization process based on acid resin. The second route involves the synthesis of a new compound, 6-nitrovanillic acid, a key A-ring component of many naturally occuring PBDs. These routes have provided a sufficient quantity of DC-81 to allow complete characterization and evaluation in DNA-binding and in vitro cytoxicity studies.
