Archiv der Pharmazie (Weinheim) 2014-06-01

Synthesis and antitumor activities of some new N1-(flavon-6-yl)amidrazone derivatives.

Almeqdad Y Habashneh, Mustafa M El-Abadelah, Malek A Zihlif, Amer Imraish, Mutasem O Taha

Index: Arch. Pharm. (Weinheim) 347(6) , 415-22, (2014)

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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. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.