Synthesis and Antitumor Activities of Some New N1‐(Flavon‐6‐yl)amidrazone Derivatives. Issue 6 (24th February 2014)

• Record Type: Journal Article
• Authors: Habashneh, Almeqdad Y.; El‐Abadelah, Mustafa M.; Zihlif, Malek A.; Imraish, Amer; Taha, Mutasem O.
• Is Part Of: Archiv der Pharmazie. Volume 347:Issue 6(2014:Jun.)
• Page Start: 415
• Page End: 422
• Publication Date: 2014-02-24
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201300326
• Languages: English
• ISSNs: 0365-6233

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <sec id="ardp201300326-sec-0001" sec-type="section"> <p>A new series of <italic>N</italic>1‐(flavon‐6‐yl)amidrazones were synthesized by reacting the hydrazonoyl chloride derived from 6‐aminoflavone with the appropriate <italic>sec</italic>‐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 <italic>N</italic>‐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 <italic>N</italic>‐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.</p> </sec> </abstract>