Data di Pubblicazione:
2019
Citazione:
Unravelling the Antiproliferative Activity of 1,2,5-oxadiazole Derivatives / D. Ehrsam, F. Porta, M. Mori, H.E.M.Z. Schwabedissen, L. Dalla Via, A.N. Garcia-Argaez, L. Basile, F. Meneghetti, S. Villa, A. Gelain. - In: ANTICANCER RESEARCH. - ISSN 0250-7005. - 39:7(2019 Jul), pp. 3453-3461. [10.21873/anticanres.13491]
Abstract:
Aim: To develop several new derivatives aimed to complete the studies concerning the antiproliferative profile of the oxadiazole derivative MD77. Materials and Methods: The substitution pattern around the phenyl rings of this compound was analyzed through the synthesis of positional isomers and of analogues bearing different substituents at the para positions (2-12). Results: The results of the antiproliferative activity of these derivatives versus HCT-116 and HeLa cancer cell lines shed light on the effects of the presence, nature and position of such substituents. Notably, derivative 4, a regioisomer of 1 in which the substituents at the para positions of the phenyl rings were inverted, showed the best antiproliferative profile, exhibiting a significant activity also against MCF7 and MDA-MB 468 cancer cell lines. Conclusion: Preliminary results showed the ability of compound 4 to reduce the viability of cancer cells by counteracting human recombinant topoisomerase II a relaxation activity.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Furazane; HCT-116; HeLa; MCF-7; MDA-MB 468; cytotoxicity; topoisomerase II
Elenco autori:
D. Ehrsam, F. Porta, M. Mori, H.E.M.Z. Schwabedissen, L. Dalla Via, A.N. Garcia-Argaez, L. Basile, F. Meneghetti, S. Villa, A. Gelain
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