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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
2018 ; 33
(1
): 434-444
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N-thioalkylcarbazoles derivatives as new anti-proliferative agents: synthesis,
characterisation and molecular mechanism evaluation
#MMPMID29383954
Sinicropi MS
; Iacopetta D
; Rosano C
; Randino R
; Caruso A
; Saturnino C
; Muią N
; Ceramella J
; Puoci F
; Rodriquez M
; Longo P
; Plutino MR
J Enzyme Inhib Med Chem
2018[Dec]; 33
(1
): 434-444
PMID29383954
show ga
Synthetic or natural carbazole derivatives constitute an interesting class of
heterocycles, which showed several pharmaceutical properties and occupied a
promising place as antitumour tools in preclinical studies. They target several
cellular key-points, e.g. DNA and Topoisomerases I and II. The most studied
representative, i.e. Ellipticine, was introduced in the treatment of metastatic
breast cancer. However, because of the onset of dramatic side effects, its use
was almost dismissed. Many efforts were made in order to design and synthesise
new carbazole derivatives with good activity and reduced side effects. The major
goal of the present study was to synthesise a series of new N-thioalkylcarbazole
derivatives with anti-proliferative effects. Two compounds, 5a and 5c, possess an
interesting anti-proliferative activity against breast and uterine cancer cell
lines without affecting non-tumoural cell lines viability. The most active
compound (5c) induces cancer cells death triggering the intrinsic apoptotic
pathway by inhibition of Topoisomerase II.