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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

  • Alexey O. Benyumov
  • , Taracad K. Venkatachalam
  • , Olga O. Grigoriants
  • , Alexei O. Vassilev
  • , Heather E. Tibbles
  • , Suzanne Downs
  • , Darin Dumez
  • , Fatih M. Uckun

Research output: Contribution to journalArticlepeer-review

Abstract

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.

Original languageEnglish (US)
Pages (from-to)114-122
Number of pages9
JournalArzneimittel-Forschung/Drug Research
Volume55
Issue number2
DOIs
StatePublished - 2005

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

  1. SDG 3 - Good Health and Well-being
    SDG 3 Good Health and Well-being

Keywords

  • CAS 213982-96-8
  • DDE46, antileukemic activity, apoptosis, Zebrafish model
  • Zidovudine, bromomethoxylated arylphosphate derivative

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