6533b871fe1ef96bd12d24e7
RESEARCH PRODUCT
Synthesis of honokiol analogues and evaluation of their modulating action on VEGF protein secretion and telomerase-related gene expressions
Eva FalomirJuan MurgaMaría Sánchez-perisMiguel CardaJuan Alberto Marcosubject
Vascular Endothelial Growth Factor A0301 basic medicineHonokiolTelomeraseAngiogenesishonokiol analoguesGene ExpressionEnzyme-Linked Immunosorbent AssayBiologytelomeraseBiochemistryLignans03 medical and health scienceschemistry.chemical_compoundangiogenesisDownregulation and upregulationDrug DiscoveryHumansSecretionTelomerase reverse transcriptaseTelomerasePharmacologyRegulation of gene expressionBiphenyl CompoundsOrganic ChemistryVEGFHEK293 Cells030104 developmental biologySecretory proteinc-MycchemistryMCF-7 CellsCancer researchMolecular Medicinegene regulationhTERTHT29 Cellsdescription
A group of 36 biphenyl derivatives structurally related to honokiol were synthesized by means of Suzuki coupling reactions. Their cytotoxicities were evaluated and compared to that of honokiol. Some of the compounds were then evaluated for their ability to downregulate the secretion of the VEGF protein and the expression of the VEGF, hTERT, and c-Myc genes; the two latter involved in the activation of telomerase in tumoral cells. Some of the synthetized derivatives showed promising pharmacological features as they exhibited IC50 values in low micromolar range, good therapeutic margins, and a multiple mode of action on tumor cells based on the inhibition of VEGF and, at the same time, of the expression of genes related to the activation of telomerase.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2017-04-01 |