Novel melphalan and chlorambucil derivatives of 2,2,6,6-tetramethyl-1-piperidinyloxy radicals: synthesis, characterization, and biological evaluation in vitro.
A series of spin-labeled melphalan and chlorambucil derivatives, coupling the alkylating agents with 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO) radicals, were synthesized, characterized, and their biological properties in vitro were evaluated. These compounds showed much higher cytotoxic activity against human leukemia cell line K562 in vitro than their parent compounds.
Zhao
Hongli
H
Key Laboratory for Advanced Materials, and Research Center of Analysis and Test, East China University of Science and Technology, Shanghai 200237, P. R.China.
Meng
Xianjiang
X
Yuan
Huihui
H
Lan
Minbo
M
D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002699:Chlorambucil / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003497:Cyclic N-Oxides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D005609:Free Radicals / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D006868:Hydrolysis; D007700:Kinetics; D008558:Melphalan / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D003497:Cyclic N-Oxides; D005609:Free Radicals; D002699:Chlorambucil; D008558:Melphalan; C003959:TEMPO