RT Journal Article
SR Electronic
T1 Unravelling the Antiproliferative Activity of 1,2,5-oxadiazole Derivatives
JF Anticancer Research
JO Anticancer Res
FD International Institute of Anticancer Research
SP 3453
OP 3461
DO 10.21873/anticanres.13491
VO 39
IS 7
A1 DANIEL EHRSAM
A1 FABIOLA PORTA
A1 MATTEO MORI
A1 HENRIETTE E. MEYER ZU SCHWABEDISSEN
A1 LISA DALLA VIA
A1 AÌDA NELLY GARCIA-ARGAEZ
A1 LIVIA BASILE
A1 FIORELLA MENEGHETTI
A1 STEFANIA VILLA
A1 ARIANNA GELAIN
YR 2019
UL http://ar.iiarjournals.org/content/39/7/3453.abstract
AB 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.