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VIRGINIA SPANO'

Evaluation of [1,2]oxazolo[5,4-e]isoindoles in lymphoma cells

  • Authors: Barreca M.; Spanò Virginia; Raimondi M.V.; Montalbano A.; Bai R.; Gaudio E.; Alcaro S.; Hamel E.; Bertoni Francesco; Barraja P.
  • Publication year: 2020
  • Type: Abstract in atti di convegno pubblicato in rivista
  • OA Link: http://hdl.handle.net/10447/438572

Abstract

Anti-tubulin agents are important chemotherapeutics. Combretastatin A-4 (CA-4) emerged as lead compound for the design of new tubulin-binding agents. Its analogues 4,5-diarylisoxazoles, containing the [1,2]oxazole ring as linker of two aryl moieties, displayed higher antitubulin activity than CA-4. [1,2]oxazolo[5,4-e]isoindoles also gave excellent results reducing cell growth of NCI-60 tumor cell lines and diffuse malignant peritoneal mesothelioma (DMPM) cells. Selected derivatives showed in vivo antitumor 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, marginal zone lymphoma and mantle cell lymphoma.