A series of [1,2]Oxazolo [5,4-e]isoindoles has been synthesized through a versatile and high yielding sequence. All the new structures showed in the 1HNMR spectra, the typical signal in the 8.34–8.47 ppm attributable to the H-3 of the [1,2]oxazole moiety. Among all derivatives, methoxy benzyl substituents at positions 3 and 4 or/and 5 were very effective in reducing the growth of different tumor cell lines, including diffuse malignant peritoneal mesothelioma (DMPM), an uncommon and rapidly malignancy poorly responsive to available therapeutic options. The most active compound 6j was found to impair tubulin polymerization, cause cell cycle arrest at G2/M phase and induce apoptosis in DMPM cells, making it as a new lead for the discovery of new potent antimitotic drugs.
|Numero di pagine||12|
|Rivista||European Journal of Medicinal Chemistry|
|Stato di pubblicazione||Published - 2016|
All Science Journal Classification (ASJC) codes
- Drug Discovery
- Organic Chemistry
Spano', V., Montalbano, A., Barraja, P., Parrino, B., Diana, P., Carbone, A., Cirrincione, G., Lopergolo, A., Cominetti, D., Pennati, M., Zuco, V., & Zaffaroni, N. (2016). [1,2]Oxazolo[5,4-e]isoindoles as promising tubulin polymerization inhibitors. European Journal of Medicinal Chemistry, 124, 840-851.