Discovery of an indole-substituted furanone with tubulin polymerization inhibition activity.

Autor: Mowery P; Department of Biology, Hobart and William Smith Colleges, Geneva, NY 14456, USA. Electronic address: mowery@hws.edu., Filkorn MM; Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA., Hurysz B; Department of Biology, Hobart and William Smith Colleges, Geneva, NY 14456, USA., Kwansare DO; Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA., Lafferty MM; Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA., McFadden MA; Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA., Neerukonda ND; Department of Biology, Hobart and William Smith Colleges, Geneva, NY 14456, USA., Patel RR; Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA., Pierce K; Department of Biology, Hobart and William Smith Colleges, Geneva, NY 14456, USA., Sockett KA; Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA., Truax NJ; Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA., Webster NR; Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA., Pelkey ET; Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA. Electronic address: pelkey@hws.edu.
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2021 Jun 01; Vol. 41, pp. 127991. Date of Electronic Publication: 2021 Mar 26.
DOI: 10.1016/j.bmcl.2021.127991
Abstrakt: Analogs of diarylpyrrolinone lead compound 1 were prepared and tested for anti-proliferative activity in U-937 cancer cells. Alterations of 1 focused on modifying the two nitrogen atoms: a) the pyrrolinone nitrogen atom was substituted with a propyl group or replaced with an oxygen atom (furanone), and b) the substituents on the indole nitrogen were varied. These changes led to the discovery of a furanone analog 3b with sub-micromolar anti-cancer potency and tubulin polymerization inhibition activity.
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Databáze: MEDLINE
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