6533b7d6fe1ef96bd12670b9
RESEARCH PRODUCT
Insights of Tris(2-pyridylmethyl)amine as anti-tumor agent for osteosarcoma: experimental and in silico studies
Anthuan Ferino PérezAntonio Doménech-carbóIdania Rodeiro GuerraNady Passe-coutrinAlessandra Mendonça Teles De SouzaSuzana Assad KahnMauricio LanznasterJuliana Lima SouzaAmanda Dos Santos CavalcantiMarcos V. Palmeira-melloMarcos V. Palmeira-melloUlises Jáuregui-hazaUlises Jáuregui-hazaGerardo Cebrián-torrejónGerardo Cebrián-torrejónsubject
TrisCisplatin010405 organic chemistryChemistryIn silicoOrganic Chemistry010402 general chemistryTris(2-pyridylmethyl)aminemedicine.disease01 natural sciences0104 chemical sciences3. Good healthAnalytical ChemistryInorganic Chemistrychemistry.chemical_compoundmedicineCancer researchOsteosarcoma[CHIM]Chemical SciencesAmine gas treatingDoxorubicinSpectroscopyDNAmedicine.drugdescription
Abstract Osteosarcoma (OS) is a malignant bone tumor and its occurrence is associated with high levels of microRNAs (miRNAs) and critical protein sinvolved on intracellular signaling pathways. Cisplatin and Doxorubicin are employed on chemotherapy, but their use cause side effects and contributes to multidrug resistance. Since several tripodal amines have been studied as anticancer agents, tris(2-pyridylmethyl)amine (TPA) was investigated against osteosarcoma cells. Here we show that TPA exhibits activity against MG-63 and Saos-2 cells. Cyclic voltammetry results indicate an interaction between TPA and dsDNA, denoted by blocking of the proton-assisted reduction of the 2-pyridylmethyl moiety in the presence of the biomolecule. Molecular docking studies indicate binding modes between TPA and DNA, as well as other crucial biological targets related to OS pathology. In addition, ADMET in silico prediction results suggest a good pharmacokinetic and toxicity profile for TPA.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2021-03-15 |