Synthesis, antitumor evaluation and crystal structure of hydroxyurea derivatives.
A series of hydroxyurea derivatives have been synthesized and elucidated by means of FT-IR, (1)H-, (13)C-NMR and MS. The exact stereostructures of representative compounds have been determined by X-ray crystal structure analysis. In the crystals, inversion dimers linked by pairs of N-H...O hydrogen bonds occurred, and further N-H...O links led to chains of molecules. In vitro antitumor activities against Tca8113 human tongue cancer cells and L1210 murine leukemia cells were evaluated. A total of 8 of the 12 compounds had higher inhibitory activities than hydroxyurea against L1210 cells. Among them, the most promising compounds were 3e, 3d, 3a and 2d.
Mai
Xi
X
State Key Laboratory of Food Science and Technology, Nanchang University, Nanchang, China.
Lu
Xiaosan
X
Xia
Hongying
H
Cao
Yusheng
Y
Liao
Yijing
Y
Lv
Xiaolan
X
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D018360:Crystallography, X-Ray; D006801:Humans; D006918:Hydroxyurea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D007938:Leukemia / Q000188:drug therapy*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D014062:Tongue Neoplasms / Q000188:drug therapy*
D000970:Antineoplastic Agents; D006918:Hydroxyurea