KMID : 0043320120350060987
|
|
Archives of Pharmacal Research 2012 Volume.35 No. 6 p.987 ~ p.994
|
|
Anticancer activity of novel indenopyridine derivatives
|
|
Ghorab Mostafa M.
Al Said Mansour S.
|
|
Abstract
|
|
|
Eighteen new 4-[2-amino-3-cyano-5-oxo-4-substitutedaryl-4H-indeno[1,2-b]pyridin-1-(5H)-yl]benzenesulfonamide derivatives 6a?q were synthesized via a reaction of aromatic aldehydes, enaminone 3 and malononitrile in one-pot reaction. Also, compounds 6a?q were obtained, via another route by reaction of enaminone 3 with arylidenemalononitriles 4a?q. The structure of the synthesized compounds was characterized by microanalysis, IR, 1H-NMR, 13C-NMR and mass spectral data. All the target compounds were subjected to in vitro anticancer activity against breast cancer cell line (MCF7). Compound 6d showed a higher potency with IC50 value (4.34 ¥ìM) than that of the Doxorubicin (5.40 ¥ìM), as the reference drug, while compound 6n with IC50 value (6.84 ¥ìM) is nearly as active as Doxorubicin. Also, compounds 6a?c, 6e, 6f, 6h and 6p exhibited a moderate activity, while compounds 3, 6g, 6i?m, 6o and 6q showed weak activity.
|
|
KEYWORD
|
|
Indenopyridines, Sulfonamides, Anti-breast cancer activity
|
|
FullTexts / Linksout information
|
|
|
|
Listed journal information
|
|
|
|