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Synthesis of honokiol analogues and evaluation of their modulating action on VEGF protein secretion and telomerase‐related gene expressions
Author(s) -
SánchezPeris María,
Murga Juan,
Falomir Eva,
Carda Miguel,
Marco Juan Alberto
Publication year - 2017
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12880
Subject(s) - honokiol , telomerase , telomerase reverse transcriptase , chemistry , secretion , downregulation and upregulation , gene expression , gene , microbiology and biotechnology , mode of action , biochemistry , biology
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 IC 50 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.