Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 11 of 11 for “"Duocarmycin"”.
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Identification of determinants of sensitivity to duocarmycin analogues: A class of potent anti-cancer drugs
Duocarmycin analogues are currently in pre-clinical development as hypoxia-activated prodrugs and as so-called payloads for antibody-drug conjugates for the treatment of cancer. Although the mechanism of action (MOA) of duocarmycins has been elucidated as DNA minor groove alkylation, not much is …
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The utilisation of Fmoc solid phase chemistry as a novel approach to the generation of duocarmycin analogues
… the conception and multi-gram synthesis of a duocarmycin SA alkylation subunit suitably substituted to serve as a building block for Fmoc based solid phase synthesis and initial investigations into its application. Chapter two describes the pilot and subsequent large scale racemic synthesis of …
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Design of smart linkers and their applications in controlled-release drug delivery systems
… linkers featuring coumarin as fluorophore and a duocarmycin analogue as an example of cytotoxic drug. Markedly, it represents the first example a duocarmycin analogue is protected with an acid cleavable moiety. Kinetic studies were performed on these linkers and showed that they are stable in …
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Epiregulin as a Novel Target for Antibody-Drug Conjugate Development for the Treatment of Colorectal Cancer
… a novel tripeptide linker attached to a modified duocarmycin payload. H231 EGC-qDuoDM gluc demonstrated minimal toxicity and significant antitumor efficacy in preclinical models of CRC. Future studies include further optimization of EREG-targeted ADCs or testing in combination with other therapies …