期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 10, 页码 2704-2706出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.03.135
关键词
Thiosemicarbazone; Crystal structure; Cytotoxic activity
资金
- Natural Science Foundation of Henan Province [0611011900]
- Foundation of Educational Department of Henan Province [2007150012]
A series of thiosemicarbazone ligands, HL1 (2-acetylpyrazine thiosemicarbazone), HL2 (2-acetylpyrazine N(4)-methylthiosemicarbazone), HL3 (2-benzoylpyridine thiosemicarbazone) and HL4 (2-benzoylpyridine N(4)-methylthiosemicarbazone), have been synthesized. The crystal structure of HL1 has been determined by single-crystal X-ray diffraction. Hydrogen bonds link the different components to stabilize the crystal structure. The antitumor activity of the four ligands were tested against K562 leucocythemia and BEL7402 liver cancer cell lines. All the thiosemicarbazones showed significant antitumor activity. Different substituents on the ligands show different levels of antitumor activity. By comparison with the other thiosemicarbazone species studied, HL4 with substitution at N(4) position in thiosemicarbazone along with 2-benzoylpyridine is the most active thiosemicarbazone ligand with IC50 = 0.002 mu m in the K562 leucocythemia cell line and 0.138 mu m in the BEL7402 liver cancer cell line, respectively. (C) 2009 Elsevier Ltd. All rights reserved.
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