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Showing 1 to 4 of 4 for “"OXi8006."”.

  1. Design and synthesis of indole-based analogues of OXi8006 as inhibitors of tubulin polymerization and their incorporation as payloads in drug-linker constructs.

    OXi8006, originally designed and synthesized by the Pinney Research Group at Baylor University, exhibited potent inhibition of tubulin polymerization and strong cytotoxicity against human various cancer cell lines. In previous studies, OXi8007, the phosphate prodrug of OXi8006, demonstrated …

    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.

    … tubulin polymerization and cancer cell growth, 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 …

    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. Inhibitors of tubulin, nitric oxide synthase, and HIF-1 alpha; synthesis, biological, and biochemical evaluation.

    … that are similar to the CA analogues and Oxi8006 were also prepared. The VDAs were tested for cancer cytotoxicity and their ability to inhibit tubulin polymerization. The 3′-amino stilbene 15 was the most effective of the fluoro-nitro stilbenes synthesized, having a tubulin IC50 of 2.9 µM, …

    baylor Repository record for Inhibitors of tubulin, nitric oxide synthase, and HIF-1 alpha; synthesis, biological, and biochemical evaluation. (opens in a new tab)

  4. Design, synthesis, and biological evaluation of dihydronaphthalene and chalcone-based anticancer agents inspired by the natural product combretastatin A-4.

    … hypoxia. Lead compounds KGP03, KGP18, and OXi8006 were evaluated as BAPCs, which incorporate bioreductive nitro-aryl triggers through an ether-linkage. The development of a scalable synthesis to KGP03 facilitated the expansion of our BAPC-library to include an additional nitrofuran series. …

    baylor Repository record for Design, synthesis, and biological evaluation of dihydronaphthalene and chalcone-based anticancer agents inspired by the natural product combretastatin A-4. (opens in a new tab)