Premium
Synthesis, Telomerase Evaluation and Anti‐Proliferative Studies on Various Series of Diaminoanthraquinone‐Linked Aminoacyl Residue Derivatives
Author(s) -
Huang FongChun,
Huang KuoFeng,
Chen RueyHui,
Wu JiaEr,
Chen TsungChih,
Chen ChunLiang,
Lee ChiaChung,
Chen JinYang,
Lin JingJer,
Huang HsuShan
Publication year - 2012
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201100122
Subject(s) - telomerase , moiety , chemistry , telomerase reverse transcriptase , stereochemistry , residue (chemistry) , anthraquinones , psychological repression , structure–activity relationship , biochemistry , biology , in vitro , gene expression , botany , gene
Four series of compounds containing an anthraquinone‐linked moiety and symmetrical or asymmetrical aminoacyl residues in side chains at positions 1,4‐, 1,5‐, 2,6‐, and 2,7‐ were synthesized and evaluated for their inhibitory effects toward telomerase and hTERT expression. Of these, only compound B11 showed selective inhibition of telomerase activity. Although it is not as competent as several of the anthraquinones we identified previously, nevertheless, the result is consistent with that the general structure moiety at the 1,5‐position of diaminoanthraquinone‐linked compound is important for the telomerase inhibitory activity. Interestingly, compounds A6 , A8 , C8 , and D8 exhibited selective repressing activities toward hTERT expression and showed less effect toward proliferation of the treated cancer cells. Although it is not apparent which structure moiety is responsible for the telomerase repression effects of these compounds, they could be further developed as potential anti‐tumor agents.