82830-18-0Relevant articles and documents
Enantiomers of 7-(2,3-Epoxypropoxy)actinomycin D as Dual-Action DNA-Acting Antitumor Agents
Sengupta, Sisir K.,Rosenbaum, David P.,Sehgal, Raj K.,Almassian, Bijan,Blondin, Joanne
, p. 1540 - 1547 (2007/10/02)
Enantiomeric forms of (+/-)-EPA have been synthesized; these are (R)-(+)- and (S)-(-)-EPA, which are active against a range of actinomycin resistant and marginally resposive tumors.The (R)-(+) enantiomer is unif
Carbon-7 Substituted Actinomycin D Analogues as Improved Antitumor Agents: Synthesis and DNA-Binding and Biological Properties
Sengupta, Sisir K.,Anderson, Jerome E.,Kelley, Christine
, p. 1214 - 1219 (2007/10/02)
7-(2,3-Epoxypropoxy)actinomycin D has been synthesized along with its major companion product, 7-(2,3-dihydroxypropoxy)actinomycin D.They were characterized by UV-visible and CD spectra and by NMR studies.According to UV-visible absorptiometry, circular dichroism, and thermal denaturation studies, they bind to DNA in a manner that is comparable to actinomycin D.The analogues are, like actinomycin D, extremely cytotoxic to human lymphoblastic leukemic cells (CCRF-CEM) in vitro but are significantly less toxic than actinomycin D to normal CDF1 mice in vivo.Unlike actinomycin, these analogues are metabolised in rats, and the methabolite are excreted in rat urine at a rapid rate.Compared to actinomycin D, the antitumor activity of the 7-(2,3-epoxypropoxy)actinomycin analogue against P-388 leukemia in mice is decidedly superior, and the therapeutic index is improved several fold.
