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.
Results
Showing 1 to 3 of 3 for “"Drug-linker constructs."”.
-
Design and synthesis of indole-based analogues of OXi8006 as inhibitors of tubulin polymerization and their incorporation as payloads in drug-linker constructs.
… In previous studies, OXi8007, the phosphate prodrug of OXi8006, demonstrated vascular disrupting activity within 2 hours of administration by targeting tumor vasculature. OXi8006 binds to the colchicine site on α,β-tubulin heterodimers, inducing a conformation shift from a straight to a curved …
-
Synthesis and biological evaluation of structurally diverse indole-based analogues as inhibitors of tubulin polymerization and synthesis of drug-linker constructs cleavable by enzymes present in the tumor microenvironment.
… OXi8006, and its water-soluble phosphate prodrug salt, OXi8007, which functioned as a promising VDA in mouse models of cancer. To expand our understanding of the relationship between structure and activity, we generated analogues that incorporated indole modifications and separately …
-
Design and synthesis of benzosuberene and tetracyclic-based molecules inspired by natural products as inhibitors of tubulin polymerization and preparation of drug-linker constructs to facilitate tumor selective targeted delivery.
… improving selectivity of active compounds via prodrug and drug-linker strategies. A series of benzosuberene and tetracyclic analogues were designed and synthesized, structurally inspired by related molecules discovered and developed by the Pinney Laboratory as promising anti-cancer agents. These …