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Synthesis and Antitumor Activities of Some New N 1‐(Flavon‐6‐yl)amidrazone Derivatives
Author(s) -
Habashneh Almeqdad Y.,
ElAbadelah Mustafa M.,
Zihlif Malek A.,
Imraish Amer,
Taha Mutasem O.
Publication year - 2014
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.201300326
Subject(s) - morpholine , chemistry , stereochemistry , tyrosine kinase , k562 cells , cell culture , derivative (finance) , chloride , quinazoline , receptor , biochemistry , cell , medicinal chemistry , biology , organic chemistry , genetics , financial economics , economics
A new series of N 1‐(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 IC 50 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.