99282-18-5Relevant academic research and scientific papers
Synthesis and biological activity of a photoaffinity etoposide probe
Hasinoff, Brian B.,Chee, Gaik-Lean,Day, Billy W.,Avor, Kwasi S.,Barnabé, Norman,Thampatty, Padmakumari,Yalowich, Jack C.
, p. 1765 - 1771 (2007/10/03)
The epipodophyllotoxin etoposide is a potent and widely used anticancer drug that targets DNA topoisomerase II. The synthesis, photochemical, and biological testing of a photoactivatable aromatic azido analogue of etoposide also containing and iodo group is described. This azido analogue should prove useful for identifying the etoposide interaction site on topoisomerase II. Irradiation of the azido analogue and an aldehyde-containing azido precursor with UV light produced changes in their UV-visible spectra that were consistent with photoactivation. The azido analogue strongly inhibited topoisomerase II and inhibited the growth of Chinese Hamster Ovary cells. Azido analogue-induced topoisomerase II-DNA covalent complexes were significantly increased of Chinese Hamster Ovary cells. Azido analogue-induced topoisomerase II-DNA covalent complexes were significantly increased subsequent to UV irradiation of drug-treated human leukemia K562 cells as compared to etoposide-treated cells. These results suggest that the photoactivated form of etoposide is a more effective topoisomerase II poison either by interacting directly with the enzyme or with DNA subsequent to topoisomerase II-mediated strand cleavage. Copyright
Synthesis and biological activity of iodinated and photosensitive derivatives of tetrabenazine
Aranda,Beaucourt,Ponchant,Isambert,Henry
, p. 369 - 374 (2007/10/02)
The synthesis of a photosensitive iodinated derivative of tetrabenazine, which should be able to lead to the identification of the vesicular catecholamine transporter of adrenal medulla by photoaffinity, is described in detail. The biological activity of this iodinated ligand was found to be significantly lower than that of non iodinated ligands.
IODINATION OF PHENOLS USING CHLORAMINE T AND SODIUM IODIDE
Kometani, Tadashi,Watt, David S.,Ji, Tae
, p. 2043 - 2046 (2007/10/02)
A convenient procedure for the iodination of many substituted phenols uses chloramine T and sodium iodide in DMF, DMSO, or acetonitrile.
