Antitumor mechanism of action of a cyclopropyl antiestrogen (compound 7b) on human breast cancer cells in culture

Cancer Chemotherapy and Pharmacology

Volumn 38, Issue 3, 1996, Pages 238-244

  Jain, Pramod T ^a,b   Pento, J Thomas ^a   Magarian, Robert A ^a  

^a UNIVERSITY OF OKLAHOMA HEALTH SCIENCES CENTER   (United States)

^b VIRGINIA COMMONWEALTH UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Anticancer drug; Cyclopropyl antiestrogen; Human breast cancer

Indexed keywords

1,1 DICHLORO 2 [4 [2 (DIMETHYL AMINO)ETHOXY]PHENYL] 2 (4 METHOXYPHENYL) 3 CYCLOPROPANE TAMOXIFEN; ANTIESTROGEN; ANTINEOPLASTIC AGENT; ESTROGEN RECEPTOR; RADIOISOTOPE; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; ARTICLE; BREAST CANCER; CANCER CELL CULTURE; CELL PROLIFERATION; CELL STRAIN MCF 7; CELL STRUCTURE; CELL SURFACE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ANTAGONISM; DRUG MECHANISM; FEMALE; HUMAN; HUMAN CELL; LUNG CANCER; PRIORITY JOURNAL; RECEPTOR AFFINITY; SCANNING ELECTRON MICROSCOPY;

BINDING, COMPETITIVE; BREAST NEOPLASMS; CELL DIVISION; CYCLOPROPANES; ESTRADIOL; ESTROGEN ANTAGONISTS; FEMALE; HUMANS; LUNG NEOPLASMS; MICROSCOPY, ELECTRON, SCANNING; MICROVILLI; RECEPTORS, ESTROGEN; TAMOXIFEN; TUMOR CELLS, CULTURED;

EID: 0030012582     PISSN: 03445704     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002800050477     Document Type: Article

References (41)

1. Antalky T, Pelletier G, Zeytinoglu F, Labrie F (1980) Changes of morphology and prolactin secretion induced by 2-Br-ergocryptine estradiol, and thyrotropin-releasing hormone in rat anterior pituitary cells in culture. J Cell Biol 86:377
2. Bardon S, Vignon F, Montcourrier P, Rochefort H (1987) Steroid receptor-mediated cytotoxicity of an antiestrogen and antiprogestin in breast cancer cells. Cancer Res 47:1441
3. Black LJ, Goode RL (1980) Uterine assay of tamoxifen, trioxifene and a new antagonist (LY 117018) in rats and mice. Life Sci 26:1453
4. Boccaardo F, Bruzzi P, Rubagotti A, Nicolo G, Rosso R (1981) Estrogen-like action of tamoxifen on vaginal epithelium in breast cancer patients. Oncology 38:281
5. Briand P, Lykkesfeldt AE (1984) Effect of estrogen and antiestrogen on the human breast cancer cell line MCF-7 adapted to growth at low serum concentration. Cancer Res 44:1114
6. Buttler WB, Kelsey WH, Goran N (1981) Effect of serum and insulin on the sensitivity of the human breast cancer cell-line MCF-7 to estrogen and antiestrogen. Cancer Res 41:82
7. Cavailles V, Augereau P, Garcia M, Rochefort H (1988) Estrogens and growth factors induce the mRNA of the 52K-pro-cathepsin-D secreted by breast cancer cells. Nucleic Acids Res 16:1903
8. Day BW, Magarian RA, Jain PT, Pento JT, Moussissian GK, Meyer K (1991) Synthesis and biological evaluation of a series of 1,1-dichloro-2,2,3-triaryl cyclopropanes as pure antiestrogens. J Med Chem 34:842
9. Dickson RB, Huff KK, Spencer EM, Lippman ME (1986) Induction of epidermal growth factor-related polypeptides by 17β-estradiol in MCF-7 human breast cancer cells. Endocrinology 118:138
10. Dix CJ, Jordan VC (1980) Subcellular effects of monohydroxytamoxifen in the rat uterus: steroid receptors and mitosis. J Endocrinol 85:393
11. Edwards DP, Adams DJ, McGuire WL (1982) Estrogen regulation of growth and specific protein synthesis in human breast cancer cells in tissue culture. Adv Exp Med Biol 138:133
12. Fornander T, Cedermark B, Mattsson A, Skoog L, Theve T, Askergren J, Rutqvist LE, Glas U, Silfversward C, Somell A, Wilking N, Hjalmar M (1989) Adjuvant tamoxifen in early breast cancer: occurrence of new primary cancers. Lancet 1:117
13. Gottardis MM, Jordan VC (1988) Development of tamoxifen-stimulated growth of MCF-7 tumor in athymic mouse after long-term tamoxifen administration. Cancer Res 48:5183
14. Horwitz KB, McGuire WL (1978) Estrogen control of progesterone receptor in human breast cancer. J Biol Chem 253:2223
15. Huff KK, Kauffman D, Gabbay K, Spencer EM, Lippman ME, Spencer EM, Dickson RB (1986) Human breast cancer cells secrete an insulin-like growth factor I-related peptide. Cancer Res 46:(4613
16. Jain PT, Pento JT (1991) A vehicle for the evaluation of hydrophobic compounds in cell culture. Res Commun Chem Pathol Pharmacol 74:105
17. Jain PT, Pento JT (1991) Growth medium for the evaluation of antiestrogenic compounds in MCF-7 cell-culture. Methods Find Expclin Pharmacol 13:595
18. Jain PT, Pento JT, Magarian RA, Graves DC (1991) Anti-proliferative activity of a series of cyclopropyl antiestrogens on MCF-7 human breast cancer cells in culture. Anticancer Drugs 2:487
19. Jain PT, Pento JT, Graves DC (1992) Cell-growth quantitation methods for the evaluation of antiestrogens in human breast cancer cells in culture. J Pharmacol Toxicol Methods 27:203
20. Jain PT, Pento JT, Magarian RA (1994) A comparison of the antitumor activity of two triarylcyclopropyl antiestrogens (compounds 4d and 5c) on human breast cancer cells in culture. Anticancer Drugs 5:429
21. Jordan VC, Murphy CS (1990) Endocrine pharmacology of antiestrogens as antitumor agents. Endocrine Rev 11:578
22. Jordan VC, Haldemann B, Allen KE (1981) Geometric isomers of substituted triphenylethylenes and antiestrogen actions. Endocrinology 108:1353
23. Katzenellenbogen BS, Ferguson ER (1975) Antiestrogen action in the uterus: biological ineffectiveness of nuclear bound estradiol after antiestrogen. Endocrinology 97:1
24. Katzenellenbogen BS, Tsai TS, Tatee T, Katzenellenbogen JA (1979) Estrogen and antiestrogen action: studies in reproductive target tissues and tumors. Recent Prog Horm Res 35:259
25. King MM, Magarian RA, Terao J, Brueggeman G (1985) Effect of non-steroidal antiestrogen, analog II and tamoxifen on a metastatic transplantable rat mammary tumor. J Natl Cancer Inst 74:447
26. Knabbe C, Lippman ME, Wakefield LM, Flanders KC, Kasid A, Derynck R, Dickson RB (1987) Evidence that transforming growth factor-β is a hormonally regulated negative growth factor in human breast cancer cells. Cell 48:417
27. Lam H (1984) Tamoxifen is a calmodulin antagonist in the activation of cAMP phosphodiestrase. Biochem Biophys Res Commun 118:27
28. Laymann SD, Jordan VC (1985) Possible mechanisms for the agonist actions of tamoxifen and the antagonist actions of MER-25 (ethamoxitriphetol) in the mouse uterus. Biochem Pharmacol 34:2795
29. Leavitt WW, Chen TJ, Allen TC (1977) Regulation of progesterone receptor formation by estrogen action. Ann NY Acad Sci 286:210
30. Lerner L, Jordan VC (1990) Development of antiestrogens and their use in breast cancer: Eighth Cain Memorial Award Lecture. Cancer Res 50:4177
31. Lippman ME, Bolan G, Huff K (1976) The effects of estrogens and antiestrogens on hormone responsive human breast cancer cells in long-term tissue culture. Cancer Res 36:4595
32. May FEB, Westley BR (1987) Effects of tamoxifen and hydroxytamoxifen on the pNR-1 and pNR-2 estrogen-regulated RNAs in human breast cancer cells. J Biol Chem 262:15894
33. Osborne CK, Coronado EB, Robinson JR (1987) Human breast cancer in athymic mouse: cytostatic effects of long-term antiestrogen therapy. Eur J Cancer Clin Oncol 23:1189
34. Pento JT, Magarian RA, King MM (1982) A comparison of efficacy for antitumor activity of non-steroidal antiestrogen analog II and tamoxifen in 7,12-dimethylbenz(a)anthracene-induced rat mammary tumors. Cancer Lett 15:261
35. Russo J, Bradley RH, McGrath C, Russo IH (1977) Scanning and transmission electron microscopy study of human breast carcinoma cell line (MCF-7) cultured in collagen-coated cellulose sponge. Cancer Res 37: 2004
36. Stoessel S, Leclercq G (1987) Competitive binding assay for estrogen receptor in monolayer culture: measure of receptor activation potency. J Steroid Biochem 25:677
37. Sutherland RL, Hall RE, Taylor IW (1983) Cell proliferation kinetics of MCF-7 human breast carcinoma cells in culture and effect of tamoxifen on exponentially growing and plateau-phase cells. Cancer Res 43:3998
38. Sutherland RL, Watt CKW, Ruenitz PC (1986) Definition of two distinct mechanisms of action of human breast cancer cell proliferation using hydroxytriphenylethylenes with high affinity for estrogen receptor. Biochem Biophys Res Commun 140:523
39. Vic P, Vignon F, Derocq D, Rochefort H (1982) Effect of estradiol on the ultrastructure of the growth of MCF-7 cells in culture. Cancer Res 42:667
40. Westley B, May FE, Brown MC, Krust A, Chambon P, Lippman ME, Rochefort H (1984) Effects of antiestrogens on the estrogen-regulated pS2 RNA and the 52 and 160-kilodalton proteins in MCF-7 cells and two tamoxifen-resistant sublines. J Biol Chem 259:10030
41. Yates J, King RJB (1981) Correlation of growth properties and morphology with hormone responsiveness of mammary tumor cells in culture. Cancer Res 41:258