Unravelling the Antiproliferative Activity of 1,2,5-oxadiazole Derivatives.
- Ehrsam D Biopharmacy, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland.
- Porta F Biopharmacy, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland.
- Mori M Department of Pharmaceutical Sciences, University of Milan, Milan, Italy.
- Schwabedissen HEMZ Biopharmacy, Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland.
- Dalla Via L Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy.
- Garcia-Argaez AN Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua, Italy.
- Basile L Department of Drug Sciences, Section of Medicinal Chemistry, University of Catania, Catania, Italy.
- Meneghetti F Department of Pharmaceutical Sciences, University of Milan, Milan, Italy.
- Villa S Department of Pharmaceutical Sciences, University of Milan, Milan, Italy stefania.villa@unimi.it.
- Gelain A Department of Pharmaceutical Sciences, University of Milan, Milan, Italy.
- 2019-07-03
Published in:
- Anticancer research. - 2019
Furazane
HCT-116
HeLa
MCF-7
MDA-MB 468
cytotoxicity
topoisomerase II
Antineoplastic Agents
Cell Line, Tumor
Cell Proliferation
Humans
Oxadiazoles
English
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.
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.
- Language
-
- English
- Open access status
- green
- Identifiers
-
- DOI 10.21873/anticanres.13491
- PMID 31262869
- Persistent URL
- https://folia.unifr.ch/global/documents/49814
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