Research progress on the selective estrogen receptor modulators

DING Hao; YANG Fan; CAI Yi; CHAI Xiaoyun; WU Qiuye

doi:10.3969/j.issn.1006-0111.2016.01.001

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Article Navigation > Journal of Pharmaceutical Practice and Service > 2016 > 34(1): 1-4,55

DING Hao, YANG Fan, CAI Yi, CHAI Xiaoyun, WU Qiuye. Research progress on the selective estrogen receptor modulators[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(1): 1-4,55. doi: 10.3969/j.issn.1006-0111.2016.01.001

Citation:

DING Hao, YANG Fan, CAI Yi, CHAI Xiaoyun, WU Qiuye. Research progress on the selective estrogen receptor modulators[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(1): 1-4,55. doi: 10.3969/j.issn.1006-0111.2016.01.001

Research progress on the selective estrogen receptor modulators

doi: 10.3969/j.issn.1006-0111.2016.01.001

1.
Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
2.
Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China;School of Pharmacy, Yantai University, Yantai 264005, China

Received Date: 2014-10-13
Rev Recd Date: 2015-06-05

Abstract

Breast cancer has become the main malignant tumors which pose a serious threat to women's health.Selective estrogen receptor modulators, which served as the effective drug treatment,have been attracting more attention. Present research progress on the selective estrogen receptor modulators was summarized in this paper.
- estrogen,
- estrogen receptor,
- selective estrogen receptor modulators

References

[1]	Advani P, Moreno-Aspitia A. Current strategies for the prevention of breast cancer[J], Breast Cancer (Dove Med Press), 2014, 6: 59-71.
[2]	郑莹, 吴春晓, 吴凡, 等. 中国女性乳腺癌死亡现况和发展趋势[J]. 中华预防医学杂志, 2011, 45(2): 150-154.
[3]	Fan L, Strasser-Weippl K, Li JJ, et al. Breast cancer in China[J]. Lancet Oncol, 2014, 15(7): 279-289.
[4]	Germain D. Estrogen carcinogenesis in breast cancer[J]. Endocrinol Metab Clin North Am, 2011, 40(3): 473-484.
[5]	Nelson ER, Wardell SE, McDonnell DP. The molecular mechanisms underlying the pharmacological actions of estrogens, SERMs and oxysterols: Implications for the treatment and prevention of osteoporosis[J]. Bone, 2013, 53(1): 42-50.
[6]	Ortona E, Pierdominici M, Berstein L. Autoantibodies to estrogen receptors and their involvement in autoimmune diseases and cancer[J]. J Steroid Biochem Mol Biol, 2014, 144: 260-267.
[7]	Osborne CK, Schiff R. Estrogen-receptor biology: continuing progress and therapeutic implications[J]. J Clin Oncol, 2005, 23: 1616-1622.
[8]	Mirkin S, Pickar JH. Selective estrogen receptor modulators (SERMs): A review of clinical data[J]. Maturitas, 2015, 53: 52-57.
[9]	Nagaraj G, Ma C. Revisiting the estrogen receptor pathway and its role in endocrine therapy for postmenopausal women with estrogen receptor-positive metastatic breast cancer[J]. Breast Cancer Res Treat, 2015,150(2):231-242.
[10]	Shanle EK, Xu W. Endocrine disrupting chemicals targeting estrogen receptor signaling: identification and mechanisms of action[J]. Chem Res Toxicol, 2011, 24: 6-19.
[11]	Komm BS, Mirkin S. An overview of current and emerging SERMs[J]. J Steroid Biochem Mol Biol, 2014, 143:207-222.
[12]	Williams C, Lin CY. Oestrogen receptors in breast cancer: basic mechanisms and clinical implications[J]. Ecancermedicalscience, 2013, 7:370.
[13]	Hadji P. The evolution of selective estrogen receptor modulators in osteoporosis therapy[J]. Climacteric, 2012, 15 (6): 513-523.
[14]	Maximov PY, Lee TM, Jordan VC. The discovery and development of selective estrogen receptor modulators (SERMs) for clinical practice[J]. Curr Clin Pharmacol, 2013, 8(2): 135-155.
[15]	Jordan VC, McDaniel R, Agboke F, et al. The evolution of nonsteroidalantiestrogens to become selective estrogen receptor modulators[J]. Steroids, 2014, 90: 3-12.
[16]	Kaur G, Mahajan MP, Pandey MK. Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents[J]. Eur J Med Chem, 2014, 86: 211-218.
[17]	Silverman S, Christiansen C. Individualizing osteoporosis therapy[J]. Osteoporos Int, 2012, 23 (3): 797-809.
[18]	Gennari L, Merlotti D, Stolakis K, et al. Lasofoxifene, from the preclinicaldrug discovery to the treatment of postmenopausal osteoporosis[J]. Expert Opin Drug Discov, 2011, 6 (2): 205-217.
[19]	Michalsen BT, Gherezghiher TB, Choi J, et al. The selective estrogen receptor modulator (SERM) Lasofoxifeneformsreactive quinonessimilar to estradiol[J]. Chem Res Toxicol, 2012, 25(7) : 1472-1483.
[20]	Vessières A, Top S, Beck W, et al. Metal complex SERMs (selective estrogen receptor modulators). The influence of different metal units on breast cancer cell antiproliferativeeffects[J]. Dalton Trans, 2006, 4: 529-541.
[21]	Li M J, Greenblatt HM, Dym O, et al. Structure of estradiol metal chelate and estrogen receptor complex: The basis for designing a new class of selective estrogen receptor modulators[J]. J Med Chem, 2011, 54(10): 3575-3580.
[22]	Top S, Vessi res A, Leclercq G, et al. Synthesis, biochemical properties and molecular modelling studies of organometallic specific estrogen receptor modulators (SERMs), the ferrocifens and hydroxyferrocifens: evidence for an antiproliferative effect of hydroxyferrocifens on both hormone-dependent and hormone-independent breast cancer cell lines[J]. Chemistry, 2003, 9(21): 5223-5236.
[23]	Plazuk D, Vessi res A, Hillard EA, et al. A[3]ferrocenophane polyphenol showing a remarkable antiproliferative activity on breast and prostate cancer cell lines[J]. J Med Chem, 2009, 52(15): 4964-4967.
[24]	Jain N, Kanojia RM, Xu J, et al. Novelchromene-derived selective estrogen receptor modulators usefulfor alleviating hot flushes and vaginal dryness[J]. J Med Chem, 2006, 49(11): 3056-3059.
[25]	Jain N, Xu J, Kanojia RM, et al. Identification and structure-activity relationships of chromene-derived selective estrogen receptor modulators for treatment of postmenopausal symptoms[J]. J Med Chem, 2009, 52: 7544-7569.
[26]	Paterni I, Granchi C, Katzenellenbogen JA, et al. Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selectiveligands and clinicalpotential[J]. Steroids, 2014, 90: 13-29.
[27]	Kim S, Wu JY, Birzin ET, et al. Estrogen Receptor Ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptorαmodulators[J]. J Med Chem, 2004, 47(9): 2171-2175.
[28]	Liao ZQ, Dong C, Carlson KE, et al. Triaryl-substitutedschiff bases are high-affinity subtype-selective ligands for the estrogenreceptor[J]. J Med Chem, 2014, 57: 3532-3545.
[29]	Carroll VM, Jeyakumar M, Carlson KE, et al. Diarylpropionitrile (DPN) enantiomers: synthesis and evaluation of estrogen receptor β-selective ligands[J]. J Med Chem, 2012, 55: 528-537.
[30]	Ohta K, Ogawa T, Kaise A, et al. Aliphatic substitution of ocarboranyl phenols enhances estrogen receptor beta selectivity[J]. Chem Pharm Bull, 2014, 62: 386-391.

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通讯作者: 陈斌, bchen63@163.com

1.
沈阳化工大学材料科学与工程学院沈阳 110142

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Research progress on the selective estrogen receptor modulators

1. Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

2. Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China;School of Pharmacy, Yantai University, Yantai 264005, China

Received Date: 2014-10-13

Rev Recd Date: 2015-06-05

Key words:

Abstract: Breast cancer has become the main malignant tumors which pose a serious threat to women's health.Selective estrogen receptor modulators, which served as the effective drug treatment,have been attracting more attention. Present research progress on the selective estrogen receptor modulators was summarized in this paper.

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Reference (30)

[1]	Advani P, Moreno-Aspitia A. Current strategies for the prevention of breast cancer[J], Breast Cancer (Dove Med Press), 2014, 6: 59-71.
[2]	郑莹, 吴春晓, 吴凡, 等. 中国女性乳腺癌死亡现况和发展趋势[J]. 中华预防医学杂志, 2011, 45(2): 150-154.
[3]	Fan L, Strasser-Weippl K, Li JJ, et al. Breast cancer in China[J]. Lancet Oncol, 2014, 15(7): 279-289.
[4]	Germain D. Estrogen carcinogenesis in breast cancer[J]. Endocrinol Metab Clin North Am, 2011, 40(3): 473-484.
[5]	Nelson ER, Wardell SE, McDonnell DP. The molecular mechanisms underlying the pharmacological actions of estrogens, SERMs and oxysterols: Implications for the treatment and prevention of osteoporosis[J]. Bone, 2013, 53(1): 42-50.
[6]	Ortona E, Pierdominici M, Berstein L. Autoantibodies to estrogen receptors and their involvement in autoimmune diseases and cancer[J]. J Steroid Biochem Mol Biol, 2014, 144: 260-267.
[7]	Osborne CK, Schiff R. Estrogen-receptor biology: continuing progress and therapeutic implications[J]. J Clin Oncol, 2005, 23: 1616-1622.
[8]	Mirkin S, Pickar JH. Selective estrogen receptor modulators (SERMs): A review of clinical data[J]. Maturitas, 2015, 53: 52-57.
[9]	Nagaraj G, Ma C. Revisiting the estrogen receptor pathway and its role in endocrine therapy for postmenopausal women with estrogen receptor-positive metastatic breast cancer[J]. Breast Cancer Res Treat, 2015,150(2):231-242.
[10]	Shanle EK, Xu W. Endocrine disrupting chemicals targeting estrogen receptor signaling: identification and mechanisms of action[J]. Chem Res Toxicol, 2011, 24: 6-19.
[11]	Komm BS, Mirkin S. An overview of current and emerging SERMs[J]. J Steroid Biochem Mol Biol, 2014, 143:207-222.
[12]	Williams C, Lin CY. Oestrogen receptors in breast cancer: basic mechanisms and clinical implications[J]. Ecancermedicalscience, 2013, 7:370.
[13]	Hadji P. The evolution of selective estrogen receptor modulators in osteoporosis therapy[J]. Climacteric, 2012, 15 (6): 513-523.
[14]	Maximov PY, Lee TM, Jordan VC. The discovery and development of selective estrogen receptor modulators (SERMs) for clinical practice[J]. Curr Clin Pharmacol, 2013, 8(2): 135-155.
[15]	Jordan VC, McDaniel R, Agboke F, et al. The evolution of nonsteroidalantiestrogens to become selective estrogen receptor modulators[J]. Steroids, 2014, 90: 3-12.
[16]	Kaur G, Mahajan MP, Pandey MK. Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents[J]. Eur J Med Chem, 2014, 86: 211-218.
[17]	Silverman S, Christiansen C. Individualizing osteoporosis therapy[J]. Osteoporos Int, 2012, 23 (3): 797-809.
[18]	Gennari L, Merlotti D, Stolakis K, et al. Lasofoxifene, from the preclinicaldrug discovery to the treatment of postmenopausal osteoporosis[J]. Expert Opin Drug Discov, 2011, 6 (2): 205-217.
[19]	Michalsen BT, Gherezghiher TB, Choi J, et al. The selective estrogen receptor modulator (SERM) Lasofoxifeneformsreactive quinonessimilar to estradiol[J]. Chem Res Toxicol, 2012, 25(7) : 1472-1483.
[20]	Vessières A, Top S, Beck W, et al. Metal complex SERMs (selective estrogen receptor modulators). The influence of different metal units on breast cancer cell antiproliferativeeffects[J]. Dalton Trans, 2006, 4: 529-541.
[21]	Li M J, Greenblatt HM, Dym O, et al. Structure of estradiol metal chelate and estrogen receptor complex: The basis for designing a new class of selective estrogen receptor modulators[J]. J Med Chem, 2011, 54(10): 3575-3580.
[22]	Top S, Vessi res A, Leclercq G, et al. Synthesis, biochemical properties and molecular modelling studies of organometallic specific estrogen receptor modulators (SERMs), the ferrocifens and hydroxyferrocifens: evidence for an antiproliferative effect of hydroxyferrocifens on both hormone-dependent and hormone-independent breast cancer cell lines[J]. Chemistry, 2003, 9(21): 5223-5236.
[23]	Plazuk D, Vessi res A, Hillard EA, et al. A[3]ferrocenophane polyphenol showing a remarkable antiproliferative activity on breast and prostate cancer cell lines[J]. J Med Chem, 2009, 52(15): 4964-4967.
[24]	Jain N, Kanojia RM, Xu J, et al. Novelchromene-derived selective estrogen receptor modulators usefulfor alleviating hot flushes and vaginal dryness[J]. J Med Chem, 2006, 49(11): 3056-3059.
[25]	Jain N, Xu J, Kanojia RM, et al. Identification and structure-activity relationships of chromene-derived selective estrogen receptor modulators for treatment of postmenopausal symptoms[J]. J Med Chem, 2009, 52: 7544-7569.
[26]	Paterni I, Granchi C, Katzenellenbogen JA, et al. Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selectiveligands and clinicalpotential[J]. Steroids, 2014, 90: 13-29.
[27]	Kim S, Wu JY, Birzin ET, et al. Estrogen Receptor Ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptorαmodulators[J]. J Med Chem, 2004, 47(9): 2171-2175.
[28]	Liao ZQ, Dong C, Carlson KE, et al. Triaryl-substitutedschiff bases are high-affinity subtype-selective ligands for the estrogenreceptor[J]. J Med Chem, 2014, 57: 3532-3545.
[29]	Carroll VM, Jeyakumar M, Carlson KE, et al. Diarylpropionitrile (DPN) enantiomers: synthesis and evaluation of estrogen receptor β-selective ligands[J]. J Med Chem, 2012, 55: 528-537.
[30]	Ohta K, Ogawa T, Kaise A, et al. Aliphatic substitution of ocarboranyl phenols enhances estrogen receptor beta selectivity[J]. Chem Pharm Bull, 2014, 62: 386-391.

Message Board

Research progress on the selective estrogen receptor modulators

doi: 10.3969/j.issn.1006-0111.2016.01.001

Abstract

References

Proportional views

通讯作者: 陈斌, bchen63@163.com

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