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Chemical Compound Review

CGS 16949A     4-(1,8- diazabicyclo[4.3.0]nona-6,8- dien-2...

Synonyms: Arensin, Afema, Fadrozole HCl, Fadrozole.HCl, SureCN4143, ...
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Disease relevance of FADROZOLE


High impact information on FADROZOLE


Chemical compound and disease context of FADROZOLE


Biological context of FADROZOLE


Anatomical context of FADROZOLE


Associations of FADROZOLE with other chemical compounds


Gene context of FADROZOLE

  • PURPOSE: The study investigated the therapeutic effects of fadrozole (CGS 16949A), a new aromatase inhibitor, in women who had received prior treatment for metastatic breast cancer [24].
  • The specific involvement of estrogen in the stimulation of this protein was established by demonstrating a reduction in the level of this protein by the addition of CGS 16949 A, an inhibitor of aromatase, a key enzyme in the biosynthesis of estradiol 17-beta and ICI 182,780, an estrogen receptor antagonist [25].
  • In vitro investigations with dispersed normal and hyperplastic human adrenocortical cells showed that CGS-16949A at 10(-7)-10(-6) M is a potent 11 beta-hydroxylase inhibitor, which inhibits ACTH-stimulated cortisol release to a similar extent as an equimolar concentration of metyrapone (IC50 for both compounds, 10(-7)-5 X 10(-7) M) [3].
  • The gonads of X. laevis were successfully maintained for 14 days in vitro in a medium containing 20 microg/ml aromatase inhibitor (CGS 16949A) [26].
  • The results suggest the mechanisms of CGS 16949A action not to be influenced by the presence or absence of ER, but to be due to its potent aromatase inhibition of the conversion of androgens to estrogens [27].

Analytical, diagnostic and therapeutic context of FADROZOLE


  1. Preliminary study of the treatment of advanced breast cancer in postmenopausal women with the aromatase inhibitor CGS 16949A. Stein, R.C., Dowsett, M., Davenport, J., Hedley, A., Ford, H.T., Gazet, J.C., Coombes, R.C. Cancer Res. (1990) [Pubmed]
  2. CGS 16949A, a new nonsteroidal aromatase inhibitor: effects on hormone-dependent and -independent tumors in vivo. Schieweck, K., Bhatnagar, A.S., Matter, A. Cancer Res. (1988) [Pubmed]
  3. The new aromatase inhibitor CGS-16949A suppresses aldosterone and cortisol production by human adrenal cells in vitro. Lamberts, S.W., Bruining, H.A., Marzouk, H., Zuiderwijk, J., Uitterlinden, P., Blijd, J.J., Hackeng, W.H., De Jong, F.H. J. Clin. Endocrinol. Metab. (1989) [Pubmed]
  4. Aromatase inhibition in the dog. II. Effect on growth, function, and pathology of the prostate. Oesterling, J.E., Juniewicz, P.E., Walters, J.R., Strandberg, J.D., Steele, R.E., Ewing, L.L., Coffey, D.S. J. Urol. (1988) [Pubmed]
  5. A new nude mouse model for postmenopausal breast cancer using MCF-7 cells transfected with the human aromatase gene. Yue, W., Zhou, D., Chen, S., Brodie, A. Cancer Res. (1994) [Pubmed]
  6. Specificity of low dose fadrozole hydrochloride (CGS 16949A) as an aromatase inhibitor. Santen, R.J., Demers, L.M., Lynch, J., Harvey, H., Lipton, A., Mulagha, M., Hanagan, J., Garber, J.E., Henderson, I.C., Navari, R.M. J. Clin. Endocrinol. Metab. (1991) [Pubmed]
  7. Inhibition of aromatase with CGS 16949A in postmenopausal women. Santen, R.J., Demers, L.M., Adlercreutz, H., Harvey, H., Santner, S., Sanders, S., Lipton, A. J. Clin. Endocrinol. Metab. (1989) [Pubmed]
  8. The effects of CGS 16949A, an aromatase inhibitor on adrenal mineralocorticoid biosynthesis. Demers, L.M., Melby, J.C., Wilson, T.E., Lipton, A., Harvey, H.A., Santen, R.J. J. Clin. Endocrinol. Metab. (1990) [Pubmed]
  9. First-line fadrozole HCI (CGS 16949A) versus tamoxifen in postmenopausal women with advanced breast cancer. Prospective randomised trial of the Swiss Group for Clinical Cancer Research SAKK 20/88. Thürlimann, B., Beretta, K., Bacchi, M., Castiglione-Gertsch, M., Goldhirsch, A., Jungi, W.F., Cavalli, F., Senn, H.J., Fey, M., Löhnert, T. Ann. Oncol. (1996) [Pubmed]
  10. Mechanisms of the actions of aromatase inhibitors 4-hydroxyandrostenedione, fadrozole, and aminoglutethimide on aromatase in JEG-3 cell culture. Yue, W., Brodie, A.M. J. Steroid Biochem. Mol. Biol. (1997) [Pubmed]
  11. Fourteen-day oral combination dose toxicity study of CGS 16949 A (aromatase inhibitor) with 5-fluorouracil or tamoxifen in rats. Matsuda, A., Higuchi, K., Karasawa, M., Yoneyama, S., Deguchi, J., Miyamoto, M. The Journal of toxicological sciences. (1997) [Pubmed]
  12. Inhibitory effect of a novel non-steroidal aromatase inhibitor, YM511 on the proliferation of MCF-7 human breast cancer cell. Kudoh, M., Susaki, Y., Ideyama, Y., Nanya, T., Mori, M., Shikama, H., Fujikura, T. J. Steroid Biochem. Mol. Biol. (1996) [Pubmed]
  13. Effect of interleukin-1beta on aromatase activity and cell proliferation in human osteoblast-like cells (HOS). Morioka, M., Shimodaira, K., Kuwano, Y., Fujikawa, H., Saito, H., Yanaihara, T. Biochem. Biophys. Res. Commun. (2000) [Pubmed]
  14. Blockade of estrogen synthesis with an aromatase inhibitor affects luteal function of the pseudopregnant rat. Shetty, G., Bhatnagar, A.S., Moudgal, N.R. J. Steroid Biochem. Mol. Biol. (1995) [Pubmed]
  15. Effects of the nonsteroidal aromatase inhibitor, Fadrozole, on sexual behavior in male rats. Bonsall, R.W., Clancy, A.N., Michael, R.P. Hormones and behavior. (1992) [Pubmed]
  16. Control of aromatase in breast cancer cells and its importance for tumor growth. Dowsett, M., Macaulay, V., Gledhill, J., Ryde, C., Nicholls, J., Ashworth, A., McKinna, J.A., Smith, I.E. J. Steroid Biochem. Mol. Biol. (1993) [Pubmed]
  17. Expression of AMH, SF1, and SOX9 in gonads of genetic female chickens during sex reversal induced by an aromatase inhibitor. Vaillant, S., Magre, S., Dorizzi, M., Pieau, C., Richard-Mercier, N. Dev. Dyn. (2001) [Pubmed]
  18. Estrogen stimulates brain-derived neurotrophic factor expression in embryonic mouse midbrain neurons through a membrane-mediated and calcium-dependent mechanism. Ivanova, T., Küppers, E., Engele, J., Beyer, C. J. Neurosci. Res. (2001) [Pubmed]
  19. In vitro and in vivo studies demonstrating potent and selective estrogen inhibition with the nonsteroidal aromatase inhibitor CGS 16949A. Steele, R.E., Mellor, L.B., Sawyer, W.K., Wasvary, J.M., Browne, L.J. Steroids (1987) [Pubmed]
  20. The effects of the aromatase inhibitor fadrozole hydrochloride on fetuses and uteri in late pregnant rats. Tamada, H., Shimizu, Y., Inaba, T., Kawate, N., Sawada, T. J. Endocrinol. (2004) [Pubmed]
  21. Effect of aromatase inhibitors on estrogen 2-hydroxylase in rat liver. Purba, H.S., King, E.J., Richert, P., Bhatnagar, A.S. J. Steroid Biochem. Mol. Biol. (1994) [Pubmed]
  22. Highly selective inhibition of estrogen biosynthesis by CGS 20267, a new non-steroidal aromatase inhibitor. Bhatnagar, A.S., Häusler, A., Schieweck, K., Lang, M., Bowman, R. J. Steroid Biochem. Mol. Biol. (1990) [Pubmed]
  23. In vitro potency and selectivity of the non-steroidal androgen aromatase inhibitor CGS 16949A compared to steroidal inhibitors in the brain. Wozniak, A., Holman, S.D., Hutchison, J.B. J. Steroid Biochem. Mol. Biol. (1992) [Pubmed]
  24. A study of fadrozole, a new aromatase inhibitor, in postmenopausal women with advanced metastatic breast cancer. Raats, J.I., Falkson, G., Falkson, H.C. J. Clin. Oncol. (1992) [Pubmed]
  25. Identification of actin as an estradiol 17-beta-stimulated protein in the human placenta. Sudha, S., Kumari, U., Rao, V.S., Rao, A.J. Biochem. Mol. Biol. Int. (1997) [Pubmed]
  26. In vitro effects of estradiol and aromatase inhibitor treatment on sex differentiation in Xenopus laevis gonads. Miyata, S., Kubo, T. Gen. Comp. Endocrinol. (2000) [Pubmed]
  27. Antitumor effects of a nonsteroidal aromatase inhibitor (CGS 16949A) on 7, 12-dimethylbenz[alpha]anthracene-induced mammary tumors in rats. Iino, Y., Sugamata, N., Owada, S., Tago, T., Sato, H., Yokoe, T., Maemura, M., Morishita, Y., Horiuchi, R. Jpn. J. Clin. Oncol. (1991) [Pubmed]
  28. Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds. Furet, P., Batzl, C., Bhatnagar, A., Francotte, E., Rihs, G., Lang, M. J. Med. Chem. (1993) [Pubmed]
  29. Recent progress in development of aromatase inhibitors. Santen, R.J. J. Steroid Biochem. Mol. Biol. (1990) [Pubmed]
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