- Synthesis and antitumor activities of some new N1-(flavon-6-yl)amidrazone derivatives.
Synthesis and antitumor activities of some new N1-(flavon-6-yl)amidrazone derivatives.
Archiv der Pharmazie (2014-03-13)
Almeqdad Y Habashneh, Mustafa M El-Abadelah, Malek A Zihlif, Amer Imraish, Mutasem O Taha
PMID24615985
ABSTRACT
A new series of N1-(flavon-6-yl)amidrazones were synthesized by reacting the hydrazonoyl chloride derived from 6-aminoflavone with the appropriate sec-cyclic amines. The antitumor activities of these compounds were evaluated on breast cancer (MCF-7) and leukemic (K562) cell lines. Among the compounds tested, the N-morpholine derivative was the most active against the MCF-7 and K562 cell lines, with IC50 values of 5.18 and 2.89 μM, respectively. Our docking studies showed that the N-morpholino derivative fits and blocks the oncogenic tyrosine kinases bcr/abl and epidermal growth factor receptor (EGFR) in a similar fashion to that of the potent anticancer agent imatinib.
MATERIALS
Product Number
Brand
Product Description
Sigma-Aldrich
Morpholine, polymer-bound, 200-400 mesh, extent of labeling: 2.75-3.25 mmol/g loading, 1 % cross-linked
Cyclizine impurity A, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
StratoSpheres™ PL-MPH resin, 50-100 mesh, extent of labeling: 3.0-4.0 mmol/g loading, 1 % cross-linked