133041-83-5Relevant academic research and scientific papers
F-18 labelled N,N-bis-haloethylamino-phenylsulfoxides - A new class of compounds for the imaging of hypoxic tissue
Falzon, Cheryl L.,Ackermann, Uwe,Spratt, Neil,Tochon-Danguy, Henri J.,White, Jonathon,Howells, David,Scott, Andrew M.
, p. 1089 - 1103 (2007/10/03)
Two N,N-bis-chloroethylamino-phenylsulfoxides have been synthesized and radiolabelled with F-18 via halogen exchange. The radiolabelling of both compounds proceeds smoothly with K[18F]F-kryptofix 2.2.2 complex at 100°C in DMSO. Decay-corrected
Sulfoxide-containing aromatic nitrogen mustards as hypoxia-directed bioreductive cytotoxins
Sun,Botros,Su,Kim,Wang,Baturay,Kwon
, p. 4160 - 4168 (2007/10/03)
A series of diaryl and alkylaryl sulfoxide-containing nitrogen mustards were synthesized and evaluated for their hypoxia-selective cytotoxicity against V-79 cells in vitro as well as for their metabolism profiles with the rat S-9 fractions. In general, th
DNA-Direcred Alkylating Agents. 4. 4-Anilinoquinoline-Based Minor Groove Directed Aniline Mustards
Gravatt, G. Lance,Baguley, Bruce C.,Wilson, William R.,Denny, William A.
, p. 1552 - 1560 (2007/10/02)
A series of 4-anilinoquinoline-linked aniline mustards of widely varying mustard reactivity were prepared and evaluated for their antitumor activity.The compounds were designed as minor groove binding agents, where the aniline mustard ring is itself part of the DNA-binding ligand.While there was a general trend for cytotoxicity to correlate with mustard reactivity, this was much less pronounced than with untargeted mustards.The compounds were much more cytotoxic than the parent diols, and were also at least 10-fold more cytotoxic than the corresponding aniline mustards themselves.Comparative cell line studies suggested that the mechanism of cytotoxicity varied with mustard reactivity.The most reactive mustards cross-linked DNA, while cell killing by the less reactive compounds appeared to be by the formation of bulky monoadducts.The compounds were active but not particularly dose-potent against P388 leukemia in vivo.The modest potency may be related to their poor aqueous solubility, since the more soluble methyl quarternary salts were equally active at much lower doses.
