European journal of medicinal chemistry, 2021-02, Vol.212, p.113122, Article 113122
2021
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Details
- Autor(en) / Beteiligte
- Titel
- Insight on [1,3]thiazolo[4,5-e]isoindoles as tubulin polymerization inhibitors
- Ist Teil von
- European journal of medicinal chemistry, 2021-02, Vol.212, p.113122, Article 113122
- Ort / Verlag
- France: Elsevier Masson SAS
- Erscheinungsjahr
- 2021
- Quelle
- Access via ScienceDirect (Elsevier)
- Beschreibungen/Notizen
- A series of [1,3]thiazolo[4,5-e]isoindoles has been synthesized through a versatile and high yielding multistep sequence. Evaluation of the antiproliferative activity of the new compounds on the full NCI human tumor cell line panel highlighted several compounds that are able to inhibit tumor cell proliferation at micromolar-submicromolar concentrations. The most active derivative 11g was found to cause cell cycle arrest at the G2/M phase and induce apoptosis in HeLa cells, following the mitochondrial pathway, making it a lead compound for the discovery of new antimitotic drugs. [Display omitted] •[1,3]Thiazolo[4,5-e]isoindoles were synthesized.•11i and 11g showed growth inhibitory activity at low micromolar concentrations.•11c showed 60% inhibition of colchicine binding to tubulin at 50 μM.•11g induced cell death by apoptosis through the mitochondrial pathway.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0223-5234eISSN: 1768-3254DOI: 10.1016/j.ejmech.2020.113122Titel-ID: cdi_crossref_primary_10_1016_j_ejmech_2020_113122
- Format
- –
- Schlagworte
- 1,3]thiazolo[4,5-e]isoindoles, Apoptosis, Apoptosis - drug effects, Cell cycle arrest, Dose-Response Relationship, Drug, HeLa Cells, Humans, Isoindoles - chemical synthesis, Isoindoles - chemistry, Isoindoles - pharmacology, Models, Molecular, Molecular Structure, Polymerization - drug effects, Structure-Activity Relationship, Tubulin - metabolism, Tubulin Modulators - chemical synthesis, Tubulin Modulators - chemistry, Tubulin Modulators - pharmacology, Tubulin polymerization inhibitors