Antitumor Comparison of Three alpha-N-Heterocyclic Thiosemicarbazone Derivatives' Crystal Structures of Bis(2-acetylpyridine)thiocarbonohydrazone and Bis(imidazole-2-carboxaldehyde)thiocarbonohydrazone

作者：Chen Chun Ling; Chen Dan Yun; Li Ming Xue^*; Niu Jing Yang

来源：Chinese Journal of Structural Chemistry, 2010, 29(9): 1380-1386.

• thiosemicarbazone
• thiocarbonohydrazone
• crystal structure
• cytotoxic activity

A series of ligands, HL(1) (2-acetylpyridine thiosemicarbazone), H(2)L(2) (bis(2-acetylpyridine) thiocarbonohydrazone) and H(2)L(3) (bis(imidazole-2-carboxaldehyde) thiocarbonohydrazone) was synthesized. H(2)L(2) and H(2)L(3) were characterized by elemental analysis, IR spectra and single-crystal X-ray diffraction studies. Hydrogen bonds link different components to stabilize the crystal structure in the two ligands. To comprehend the structure-activity relationship well, the three ligands are all tested against human K562 leucocythemia cell line with IC(50) analysis. Different substituent groups on the ligands show different levels of antitumor activity. By comparison with the other species studied, H(2)L(2) with thiocarbonohydrazone along with 2-acetylpyridine is the most active compound with IC(50) = 2.48 mu m.

• 出版日期2010
• 单位河南大学