Global ETD Search
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Showing 1 to 2 of 2 for “"Indole-based analogues."”.
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Design and synthesis of indole-based analogues of OXi8006 as inhibitors of tubulin polymerization and their incorporation as payloads in drug-linker constructs.
… and two-atom bridging functionalities. Among the analogues synthesized, compounds bearing a sulfide bridge (KGP555) and a methylene bridge (KGP608) demonstrated potent biological activity, including a strong inhibition of tubulin polymerization, a high affinity for the colchicine site, and …
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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.
… between structure and activity, we generated analogues that incorporated indole modifications and separately incorporated a piperazine motif. A number of compounds from these focused libraries showed robust inhibition of tubulin polymerization and potent cytotoxic effects against human cancer …