Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 212, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.113122
Keywords
1,3]thiazolo[4,5-e]isoindoles; Apoptosis; Cell cycle arrest; Tubulin polymerization inhibitors
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Funding
- Ministero dell'Istruzione dell'Universita e della Ricerca (MIUR)
- Developmental Therapeutics Program in the Division of Cancer Treatment and Diagnosis of the National Cancer Institute [HHSN261200800001E]
- Italian Association for Cancer Research (AIRC) research project Small molecule-based targeting of lncRNAs 3D structure: a translational platform for the treatment of multiple myeloma [21588]
- PRIN 2017 research project Novel anticancer agents endowed with multi-targeting mechanism of action [201744BN5T]
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A series of [1,3]thiazolo[4,5-e]isoindoles have been synthesized with high antiproliferative activity, with compound 11g showing the highest potency to induce cell cycle arrest and apoptosis. This compound could serve as a lead compound for new antimitotic drug discovery.
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. (C) 2020 Elsevier Masson SAS. All rights reserved.
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