Synthesis and evaluation of novel 17-indazole androstene derivatives designed as CYP17 inhibitors

Vânia M. A. Moreira, Tadas S. Vasaitis, Vincent C. O. Njar, Jorge A. R. Salvador

Research output: Contribution to journalArticle

43 Citations (Scopus)

Abstract

A series of novel 1H- and 2H-indazole derivatives of the commercially available dehydroepiandrosterone acetate have been synthesized and tested for inhibition of human cytochrome 17alpha-hydroxylase-C(17,20)-lyase (CYP17), androgen receptor (AR) binding affinity, and cytotoxic potential against three prostate cancer (PC) cell lines.

LanguageEnglish
Pages939-948
Number of pages10
JournalSteroids
Volume72
Issue number14
Early online date15 Aug 2007
DOIs
Publication statusPublished - 31 Dec 2007

Fingerprint

Androstenes
Indazoles
Steroid 17-alpha-Hydroxylase
Derivatives
Androgen Receptors
Cytochromes
Mixed Function Oxygenases
Prostatic Neoplasms
Cells
Cell Line

Keywords

  • binding, competitive
  • cell line, tumor
  • cell proliferation
  • dehydroepiandrosterone

Cite this

Moreira, Vânia M. A. ; Vasaitis, Tadas S. ; Njar, Vincent C. O. ; Salvador, Jorge A. R. / Synthesis and evaluation of novel 17-indazole androstene derivatives designed as CYP17 inhibitors. In: Steroids. 2007 ; Vol. 72, No. 14. pp. 939-948.
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Synthesis and evaluation of novel 17-indazole androstene derivatives designed as CYP17 inhibitors. / Moreira, Vânia M. A.; Vasaitis, Tadas S.; Njar, Vincent C. O.; Salvador, Jorge A. R.

In: Steroids, Vol. 72, No. 14, 31.12.2007, p. 939-948.

Research output: Contribution to journalArticle

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AU - Vasaitis, Tadas S.

AU - Njar, Vincent C. O.

AU - Salvador, Jorge A. R.

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