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Z. Naturforsch. 2014,
69b, 811 – 816
doi:10.5560/ZNB.2014-4062
Synthesis and Antitumor Activity of Some N2-(Thien-3-yl)amidrazones
1 College of Pharmacy, Taibah University, Al Madinah Almonawarrah, 41477, Saudia Arabia
2 Chemistry Department, Faculty of Science, The University of Jordan, Amman 11942, Jordan
3 Department of Pharmacology, Faculty of Medicine, The University of Jordan, Amman 11942, Jordan
4 Interfakultäres Institut für Biochemie, Universität Tübingen, Hoppe-Seyler-Straße 4, 72076 Tübingen, Germany
Reprint requests to Prof. Dr. W. Voelter. E-mail:
wolfgang.voelter@uni-tuebingen.de or M. M. El-Abadelah.
mustelab@ju.edu.jo
Received March 12, 2014 / published online July 8, 2014
A set of new N2-(thien-3-yl)amidrazones (6a–h) incorporating N-piperazines and related congeners has been synthesized by reacting the hydrazonoyl chloride 4 (derived from 3-amino-thiophene-2-carboxylate) with the appropriate sec-cyclic amine. The antitumor activity of these compounds was evaluated on breast cancer (MCF-7) and leukemic (K562) cell lines by a cell viability assay utilizing the tetrazolium dye (MTT). The amidrazone 6d encompassing the N-piperazine moiety, was the most active against MCF-7 and K562 with IC50 of 7.28 and 9.91 μm, respectively.
Key words: 3-Aminothiophene-2-carboxylic Ester, N2-(Thien-3-yl)nitrile Imine, Piperazines, N2-(Thien-3-yl)amidrazones, Antitumor Activity