Synthesis and evaluation of biphenyl derivatives as potential downregulators of VEGF protein secretion and telomerase-related gene expressions.
A group of 47 biphenyl functionalized compounds, prepared by means of Suzuki couplings, has been investigated for their cytotoxicity on two tumoral cell lines (HT-29 and MCF-7) and one non tumoral cell line (HEK-293). 29 selected compounds have been investigated for their ability to inhibit the production of the vascular endothelial growth factor (VEGF). Subsequently, the capacity of the compounds to downregulate the expression of the VEGF, h-TERT and c-Myc genes, the two latter involved in the control of the activation of telomerase, has also been determined.
Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.
María
M
Sánchez-Peris
Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.
Eva
E
Falomir
Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain. Electronic address: jmurga@uji.es.
Juan
J
Murga
Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.
Miguel
M
Carda
Depart. de Q. Orgánica, Univ. de Valencia, E-46100 Burjassot, Valencia, Spain.
J Alberto
JA
Marco
D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015536:Down-Regulation / Q000187:drug effects*; D016259:Genes, myc; D057809:HEK293 Cells; D019073:HT29 Cells; D006801:Humans; D061986:MCF-7 Cells; D013329:Structure-Activity Relationship; D019098:Telomerase / Q000235:genetics*; D042461:Vascular Endothelial Growth Factor A / Q000235:genetics / Q000378:metabolism*
D001713:Biphenyl Compounds; D019098:Telomerase; D042461:Vascular Endothelial Growth Factor A; C010574:biphenyl
Antiangiogenesis; Biphenyl derivatives; Telomerase; VEGF; hTERT