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.jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117 J+Enzyme+Inhib+Med+Chem
2017 ; 32
(1
): 1012-1028
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New sulfurated derivatives of cinnamic acids and rosmaricine as inhibitors of
STAT3 and NF-?B transcription factors
#MMPMID28738705
Gabriele E
; Brambilla D
; Ricci C
; Regazzoni L
; Taguchi K
; Ferri N
; Asai A
; Sparatore A
J Enzyme Inhib Med Chem
2017[Dec]; 32
(1
): 1012-1028
PMID28738705
show ga
A set of new sulfurated drug hybrids, mainly derived from caffeic and ferulic
acids and rosmaricine, has been synthesized and their ability to inhibit both
STAT3 and NF-?B transcription factors have been evaluated. Results showed that
most of the new hybrid compounds were able to strongly and selectively bind to
STAT3, whereas the parent drugs were devoid of this ability at the tested
concentrations. Some of them were also able to inhibit the NF-?B transcriptional
activity in HCT-116 cell line and inhibited HCT-116 cell proliferation in vitro
with IC(50) in micromolar range, thus suggesting a potential anticancer activity.
Taken together, our study described the identification of new derivatives with
dual STAT3/NF-?B inhibitory activity, which may represent hit compounds for
developing multi-target anticancer agents.