Anti-tubulin agents are important chemotherapeutics.Combretastatin A-4 (CA-4) emerged as lead compound for the design ofnew tubulin-binding agents. Its analogues 4,5-diarylisoxazoles, containingthe [1,2]oxazole ring as linker of two aryl moieties, displayed higher antitubulinactivity than CA-4. [1,2]oxazolo[5,4-e]isoindoles also gave excellentresults reducing cell growth of NCI-60 tumor cell lines and diffuse malignantperitoneal mesothelioma (DMPM) cells. Selected derivatives showed in vivoantitumor activity at well-tolerated doses in a DMPM xenograft model.[1,2]oxazolo[5,4-e]isoindoles were screened in four lymphoma histotypes:germinal center B-cell and activated diffuse large B cell lymphoma, marginalzone lymphoma and mantle cell lymphoma.
|Numero di pagine||2|
|Stato di pubblicazione||Published - 2020|
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