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Showing 1 to 3 of 3 for “"Drug-linker constructs."”.

  1. 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 …

    baylor Repository record for Design and synthesis of indole-based analogues of OXi8006 as inhibitors of tubulin polymerization and their incorporation as payloads in drug-linker constructs. (opens in a new tab)

  2. 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 …

    baylor Repository record for 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. (opens in a new tab)

  3. 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 …

    baylor Repository record for 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. (opens in a new tab)