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Original Article

Potent and selective aromatase inhibitor: in vitro and in vivo studies with s-triazine derivative sef19

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Pages 1-13 | Published online: 07 Aug 2009

References

  • Lonning P E, Kvinnsland S, Thorsen T, Ueland P M. Alterations in the metabolism of oestrogens during treatment with aminoglutethimide in breast cancer patients. Preliminary findings. Clin Pharmacokinet 1987; 13: 393–406
  • Dexter R N, Fishman L M, Ney R L, Liddle G W. Inhibition of adrenal corticosteroid synthesis by aminoglutethimide: Studies of the mechanism of action. J Clin Endocr 1967; 27: 473–480
  • Cohen M P. Aminoglutethimide inhibition of adrenal desmolase activity. Proc Soc Exper Biol Med 1968; 127: 1086–1900
  • Gower D B. Modifiers of steroid-hormone metabolism: A review of their chemistry biochemistry and clinical application. J Steroid Biochem 1974; 5: 501–523
  • Santen R J. Suppression of estrogens with aminoglutethimide and hydrocortisone (medical adrenalectomy) as treatment of advanced breast carcinoma: a review. Breast Cancer Res Treat 1981; 1: 183–202
  • Dowsett M, Goss P E, Powles T J, Hutchinson G, Brodie AM H, Jeffcoate S L, Coombes R C. Use of the aromatase inhibitor 4-hydroxyandrostenedione in postmenopausal breast cancer: Optimization of therapeutic dose and route. Cancer Res 1987; 47: 1957–1961
  • Cunningham D, Powles T J, Dowsett M, Hutchinson G, Brodie AM H, Ford H T, Gazet J-C, Coombes R C. Oral 4-hydroxyandrostenedione a new endocrine treatment for disseminated breast cancer. Cancer Chemother Pharmacol 1987; 20: 253–255
  • Iino Y, Sugamata N, Susumu N, Owada S, Tago T, Sato H, Yokoe T, Maemura M, Morishita Y, Horiuchi R. Antitumor effects of a nonsteroidal aromatase inhibitor (CGS 16949A) on 7,12-dimethylbenz[α]anthracene-induced mammary tumors in rats. Jpn J Clin Oacol 1991; 21: 153–159
  • Schieweck K, Bhatnagar A S, Batzl C, Lang M. Anti-tumor and endocrine effects of non-steroidal aromatase inhibitors on estrogen-dependent rat mammary tumors. J Steroid Biochem Molec Biol 1993; 44: 633–636
  • Lipton A, Harvey H A, Demers L M, Hanagan J R, Mulagha M T, Kochak G M, Fitzsimmons S, Sanders S I, Santen R J. A phase I trial of CGS 16949A. Cancer 1990; 65: 1279–1285
  • Raats J I, Falkson G, Falkson H C. A study of fadrozole, a new aromatase inhibitor, in postmenopausal women with advanced metastatic breast cancer. J Clin Oncol 1992; 10: 111–116
  • Brodie AM H. Aromatase inhibitors in the treatment of breast cancer. J Steroid Biochem Molec Biol 1994; 49: 281–287
  • Dowsett M, Smithers D, Moore J, Trunet P F, Coombes R C, Powles T J, Rubens R, Smith I E. Endocrine changes with the aromatase inhibitor fadrozole hydrochloride in breast cancer. Eur J Cancer 1994; 30A: 453–1458
  • Tanino H, Kubota T, Yamada Y, Koh J, Takeuchi T, Kase S, Furuawa T, Takahashi M, Fukuda S, Ogose N, Komatsu T, Sakato M, Kitajima M, Sakurai T, Naito Y, Hoffman R M. A newly developed haxamethymelamine derivative SAE9 with both antitumor and aromatase-inhibitory activity. Anticancer Res 1993; 13: 623–626
  • Matsuno T, Kato M, Tsuchida Y, Takahashi M, Yaguchi S, Terada S. Synthesis of imidazolyl-1,3,5-triazine derivatives and their aromatase inhibitory activity. Chem Pharmac Bull 1996, In press
  • Yuan P-M, Nakajin S, Haniu M, Shinoda M, Hall P F, Shively J E. Steroid 21-hydroxylase (cytochrome P-450) from porcine adrenocortical microsomes: Microsequence analysis of cysteine-containing peptides. Biochemistry 1983; 22: 143–149
  • Kimura T. Biochemical aspect of iron-sulfur linkage in non-heme iron protein, with special reference to “adrenodoxin”. Structure and Bonding, vol. 5, J B Neilands, R S Nyholm, D Reinen, RJ P Williams. Springer-Verlag, Berlin 1968; pp. 1–40
  • Thompson E A, Jr., Thompson SP K. Utilization of oxygen and reduced nicotinamide adenine dinucleotide phosphate by human placental microsomes during aromatization of androstenedione. J Biol Chem 1974; 249: 5364–5372
  • Numazawa M, Mutsumi A, Asano N, Ito Y. A time-dependent inactivation of aromatase by 19-substituted androst-4-ene-3,6,17-triones. Steroids 1993; 58: 40–46
  • Shikita M, Hall P F. The Stoichiometry of the conversion of cholesterol and hydroxycholesterols to pregnenolone (3β-hydroxypregn-5-en-20-one) catalyzed by adrenal cytochrome P-450. Proc Natl Acad Sci U.S.A 1974; 71: 1441–1445
  • Nakajin S, Hall P F. Microsomal cytochrome P-450 from neonatal pig testis. J Biol Chem 1981; 256: 3871–3876
  • Shizuta Y, Kawano T, Mitsuuci Y, Toda K, Miyahara K, Ichikawa Y, Imura H, Ulick S. Molecular genetic studies on the biosynthesis of aldosterone in humans. J Steroid Biochem Molec Biol 1992; 43: 981–987
  • Lowry O H, Rosebrough N J, Farr A L, Randall R J. Protein measurement with the Folin phenol reagent. J Biol Chem 1951; 193: 265–275
  • Sakoda M, Hiromi K. Determination of the best-fit values of kinetic parameters of the Michaelis-Menten equation by the method of least squares with the Taylor expansion. J Biochem 1976; 80: 547–555
  • Nakajin S, Hall P F. Purification to homogeneity of aromatase from human placenta. Biochem Biophys Res Commun 1986; 134: 704–710
  • Meyer A S. Conversion of 19-hydroxy-Δ4-androstene-3,17-dione to estrone by endocrine tissue. Biochim Biophys Acta 1955; 17: 441–442
  • Santen R J, Samojlik E, Demers L, Badder E. Adrenal of male dog secretes androgens and estrogens. Am J Physiol 1980; 239: E109–E112
  • Lamberts SW J, Bruining H A, Marzouk H, Zuiderwijk J, Uitterlinden P, Blijd J J, Hackeng WH L, deJong F H. The new aromatase inhibitor CGS-16949A suppresses aldosterone and cortisol production by human adrenal cells in vitro. J Clin Endocrinol Metab 1989; 69: 896–901
  • Santen R J, Demers L M, Adlercreutz H, Harvey H, Santner S, Sanders S, Lipton A. Inhibition of aromatase with CGS 16949A in postmenopausal women. J Clin Endocrinol Metab 1989; 68: 99–106
  • Dowsett M, Stein R C, Mehta A, Coombes R C. Potency and selectivity of the non-steroidal aromatase inhibitor CGS 16949A in postmenopausal breast cancer patients. Clin Endocr 1990; 32: 623–634
  • Hausler A, Monnet G, Borer C, Bhatnagar A S. Evidence that corticosterone is not an obligatory intermediate in aldosterone biosynthesis in the rat adrenal. J Steroid Biochem 1989; 34: 567–570
  • Steel R E, Mellor L B, Sawyer W K, Wasvary J M, Browne L J. In vitro and in vivo studies demonstrating potent and selective estrogen inhibition with the nonsteroidal aromatase inhibitor CGS 16949A. Steroids 1987; 50: 147–161
  • Bhatnagar A S, Häusler A, Schieweck K. Inhibition of aromatase in vitro and in vivo by aromatase inhibitors. J Enz Inhibit 1990; 4: 179–186
  • Selvaraj N, Shetty G, Vijayalakshmi K, Bhatnagar A S, Moudgal N R. Effect of blocking oestrogen synthesis with a new generation aromatase inhibitor CGS 16949A on follicular maturation induced by pregnant mare serum gonadotrophin in the immature rat. J Endocr 1994; 142: 563–570

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