TY - JOUR T1 - Unravelling the Antiproliferative Activity of 1,2,5-oxadiazole Derivatives JF - Anticancer Research JO - Anticancer Res SP - 3453 LP - 3461 DO - 10.21873/anticanres.13491 VL - 39 IS - 7 AU - DANIEL EHRSAM AU - FABIOLA PORTA AU - MATTEO MORI AU - HENRIETTE E. MEYER ZU SCHWABEDISSEN AU - LISA DALLA VIA AU - AÌDA NELLY GARCIA-ARGAEZ AU - LIVIA BASILE AU - FIORELLA MENEGHETTI AU - STEFANIA VILLA AU - ARIANNA GELAIN Y1 - 2019/07/01 UR - http://ar.iiarjournals.org/content/39/7/3453.abstract N2 - 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 α relaxation activity. ER -