220693-38-9Relevant academic research and scientific papers
Zidampidine, an aryl phosphate derivative of AZT: In vivo pharmacokinetics, metabolism, toxicity, and anti-viral efficacy against hemorrhagic fever caused by Lassa virus
Uckun,Venkatachalam,Erbeck,Chen,Petkevich,Vassilev
, p. 3279 - 3288 (2005)
The pharmacokinetics, metabolism, and toxicity of Zidampidine, an aryl phosphate derivative of AZT, 3′-azidothymidine-5′-[p-bromophenyl methoxyalaninyl phosphate] were investigated in CD-1 mice. Following iv injection, Zidampidine was rapidly converted to
Anti-proliferative and anti-leukemic activity of DDE46 (compound WHI-07), a novel bromomethoxylated arylphosphate derivative of zidovudine, and related compounds: Studies using human acute lymphoblastic leukemia cells and the zebrafish model
Benyumov, Alexey O.,Venkatachalam, Taracad K.,Grigoriants, Olga O.,Vassilev, Alexei O.,Tibbles, Heather E.,Downs, Suzanne,Dumez, Darin,Uckun, Fatih M.
, p. 114 - 122 (2007/10/03)
The anti-proliferative effects of a novel bromomethoxylated arylphosphate derivative of zidovudine (compound DDE46, CAS 213982-96-8) were first examined in a zebra fish embryo model. DDE46 blocked the cell division at the 2-cell stage of the embryonic development followed by total cell fusion. DDE46 also inhibited the proliferation of the leukemic cell lines NALM-6 and MOLT-3. DDE46 enhanced the activity of the pro-apoptotic enzymes Caspase-3, Caspase-6, Caspase-8, and Caspase-9 leading to the apoptotic death of the leukemic cell line Jurkat. These results justify the further development of this agent as a new anti-leukemic drug candidate. ECV · Editio Cantor Verlag, Aulendorf (Germany).
Aryl phosphate derivatives of d4T having anti-HIV activity
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Page column 15-16, (2008/06/13)
Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.
