Synthesis and Antitumor Activities of Some New N1-(Flavon-6-yl)amidrazone Derivatives
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 compound...
Saved in:
Published in | Archiv der Pharmazie (Weinheim) Vol. 347; no. 6; pp. 415 - 422 |
---|---|
Main Authors | , , , , |
Format | Journal Article |
Language | English German |
Published |
WEINHEIM
Blackwell Publishing Ltd
01.06.2014
Wiley Wiley Subscription Services, Inc |
Subjects | |
Online Access | Get full text |
Cover
Loading…
Summary: | 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.
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 N‐morpholine derivative was the most active against two cancer cell lines. Docking studies revealed that this derivative fits and blocks the oncogenic tyrosine kinases bcr/abl and EGFR similar to the anticancer agent imatinib. |
---|---|
Bibliography: | ArticleID:ARDP201300326 ark:/67375/WNG-SB19ZS4J-B Deanship of Scientific Research at the University of Jordan, Amman, Jordan istex:4001FD9A35B37CF9828BB538C919B08A9B1271B1 ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0365-6233 1521-4184 |
DOI: | 10.1002/ardp.201300326 |