7 α -Substituted androstenediones as effective in vttro and in vivo inhibitors of aromatase
Research efforts over the past several years have focused on the synthesis of competitive and irreversible aromatase inhibitors and examination of these inhibitors in microsomal preparations, in cell culture, and in vivo. Several 7α-substituted androstenediones have demonstrated high affinity for pl...
Ausführliche Beschreibung
Gespeichert in:
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| Format: |
E-Artikel |
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| Sprache: |
Englisch |
| Erschienen: |
1987 |
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| Reproduktion: |
Elsevier Journal Backfiles on ScienceDirect 1907 - 2002 |
|---|---|
| Übergeordnetes Werk: |
in: Steroids - Amsterdam : Elsevier, 50(1987), 1-3, Seite 163-178 |
| Übergeordnetes Werk: |
volume:50 ; year:1987 ; number:1-3 ; pages:163-178 |
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| 520 | |a Research efforts over the past several years have focused on the synthesis of competitive and irreversible aromatase inhibitors and examination of these inhibitors in microsomal preparations, in cell culture, and in vivo. Several 7α-substituted androstenediones have demonstrated high affinity for placental aromatase, with apparent K"i's ranging from 1 to 30 nM. Inactivation of aromatase occurred following incubation with alkylating and enzyme-activated irreversible inhibitors. 7α-(4'-Amino)phenylthio-4-androstene-3,17-dione (7α-APTA) exhibits potent inhibitory activity of aromatase in the MCF-7 human mammary carcinoma cell line with an ED"5"0 of approximately 25 nM. The inhibitor did not bind to the estrogen receptor of the cells in vitro nor induce levels of progesterone receptors in intact cells. In vivo studies of 7α-APTA in the DMBA-induced rat mammary carcinoma model resulted in 80% of the tumors responding completely or partially at doses of 25 and 50 mg/kg body wt/day. Thus, these 7α-substituted steroidal aromatase inhibitors are effective medicinal agents and may be useful for the treatment of estrogen-dependent breast cancer. | ||
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(DE-627)NLEJ186564481 (DE-599)GBVNLZ186564481 DE-627 ger DE-627 rakwb eng 7 α -Substituted androstenediones as effective in vttro and in vivo inhibitors of aromatase 1987 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Research efforts over the past several years have focused on the synthesis of competitive and irreversible aromatase inhibitors and examination of these inhibitors in microsomal preparations, in cell culture, and in vivo. Several 7α-substituted androstenediones have demonstrated high affinity for placental aromatase, with apparent K"i's ranging from 1 to 30 nM. Inactivation of aromatase occurred following incubation with alkylating and enzyme-activated irreversible inhibitors. 7α-(4'-Amino)phenylthio-4-androstene-3,17-dione (7α-APTA) exhibits potent inhibitory activity of aromatase in the MCF-7 human mammary carcinoma cell line with an ED"5"0 of approximately 25 nM. The inhibitor did not bind to the estrogen receptor of the cells in vitro nor induce levels of progesterone receptors in intact cells. In vivo studies of 7α-APTA in the DMBA-induced rat mammary carcinoma model resulted in 80% of the tumors responding completely or partially at doses of 25 and 50 mg/kg body wt/day. Thus, these 7α-substituted steroidal aromatase inhibitors are effective medicinal agents and may be useful for the treatment of estrogen-dependent breast cancer. Elsevier Journal Backfiles on ScienceDirect 1907 - 2002 Brueggemeier, R.W. oth Pui-Kai, L. oth Snider, C.E. oth Darby, M.V. oth Katlic, N.E. oth in Steroids Amsterdam : Elsevier 50(1987), 1-3, Seite 163-178 (DE-627)NLEJ17701184X (DE-600)1498762-4 0039-128X nnns volume:50 year:1987 number:1-3 pages:163-178 http://linkinghub.elsevier.com/retrieve/pii/0039-128X(83)90069-7 GBV_USEFLAG_H ZDB-1-SDJ GBV_NL_ARTICLE AR 50 1987 1-3 163-178 |
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(DE-627)NLEJ186564481 (DE-599)GBVNLZ186564481 DE-627 ger DE-627 rakwb eng 7 α -Substituted androstenediones as effective in vttro and in vivo inhibitors of aromatase 1987 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Research efforts over the past several years have focused on the synthesis of competitive and irreversible aromatase inhibitors and examination of these inhibitors in microsomal preparations, in cell culture, and in vivo. Several 7α-substituted androstenediones have demonstrated high affinity for placental aromatase, with apparent K"i's ranging from 1 to 30 nM. Inactivation of aromatase occurred following incubation with alkylating and enzyme-activated irreversible inhibitors. 7α-(4'-Amino)phenylthio-4-androstene-3,17-dione (7α-APTA) exhibits potent inhibitory activity of aromatase in the MCF-7 human mammary carcinoma cell line with an ED"5"0 of approximately 25 nM. The inhibitor did not bind to the estrogen receptor of the cells in vitro nor induce levels of progesterone receptors in intact cells. In vivo studies of 7α-APTA in the DMBA-induced rat mammary carcinoma model resulted in 80% of the tumors responding completely or partially at doses of 25 and 50 mg/kg body wt/day. Thus, these 7α-substituted steroidal aromatase inhibitors are effective medicinal agents and may be useful for the treatment of estrogen-dependent breast cancer. Elsevier Journal Backfiles on ScienceDirect 1907 - 2002 Brueggemeier, R.W. oth Pui-Kai, L. oth Snider, C.E. oth Darby, M.V. oth Katlic, N.E. oth in Steroids Amsterdam : Elsevier 50(1987), 1-3, Seite 163-178 (DE-627)NLEJ17701184X (DE-600)1498762-4 0039-128X nnns volume:50 year:1987 number:1-3 pages:163-178 http://linkinghub.elsevier.com/retrieve/pii/0039-128X(83)90069-7 GBV_USEFLAG_H ZDB-1-SDJ GBV_NL_ARTICLE AR 50 1987 1-3 163-178 |
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(DE-627)NLEJ186564481 (DE-599)GBVNLZ186564481 DE-627 ger DE-627 rakwb eng 7 α -Substituted androstenediones as effective in vttro and in vivo inhibitors of aromatase 1987 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Research efforts over the past several years have focused on the synthesis of competitive and irreversible aromatase inhibitors and examination of these inhibitors in microsomal preparations, in cell culture, and in vivo. Several 7α-substituted androstenediones have demonstrated high affinity for placental aromatase, with apparent K"i's ranging from 1 to 30 nM. Inactivation of aromatase occurred following incubation with alkylating and enzyme-activated irreversible inhibitors. 7α-(4'-Amino)phenylthio-4-androstene-3,17-dione (7α-APTA) exhibits potent inhibitory activity of aromatase in the MCF-7 human mammary carcinoma cell line with an ED"5"0 of approximately 25 nM. The inhibitor did not bind to the estrogen receptor of the cells in vitro nor induce levels of progesterone receptors in intact cells. In vivo studies of 7α-APTA in the DMBA-induced rat mammary carcinoma model resulted in 80% of the tumors responding completely or partially at doses of 25 and 50 mg/kg body wt/day. Thus, these 7α-substituted steroidal aromatase inhibitors are effective medicinal agents and may be useful for the treatment of estrogen-dependent breast cancer. Elsevier Journal Backfiles on ScienceDirect 1907 - 2002 Brueggemeier, R.W. oth Pui-Kai, L. oth Snider, C.E. oth Darby, M.V. oth Katlic, N.E. oth in Steroids Amsterdam : Elsevier 50(1987), 1-3, Seite 163-178 (DE-627)NLEJ17701184X (DE-600)1498762-4 0039-128X nnns volume:50 year:1987 number:1-3 pages:163-178 http://linkinghub.elsevier.com/retrieve/pii/0039-128X(83)90069-7 GBV_USEFLAG_H ZDB-1-SDJ GBV_NL_ARTICLE AR 50 1987 1-3 163-178 |
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7 α -substituted androstenediones as effective in vttro and in vivo inhibitors of aromatase |
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7 α -Substituted androstenediones as effective in vttro and in vivo inhibitors of aromatase |
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Research efforts over the past several years have focused on the synthesis of competitive and irreversible aromatase inhibitors and examination of these inhibitors in microsomal preparations, in cell culture, and in vivo. Several 7α-substituted androstenediones have demonstrated high affinity for placental aromatase, with apparent K"i's ranging from 1 to 30 nM. Inactivation of aromatase occurred following incubation with alkylating and enzyme-activated irreversible inhibitors. 7α-(4'-Amino)phenylthio-4-androstene-3,17-dione (7α-APTA) exhibits potent inhibitory activity of aromatase in the MCF-7 human mammary carcinoma cell line with an ED"5"0 of approximately 25 nM. The inhibitor did not bind to the estrogen receptor of the cells in vitro nor induce levels of progesterone receptors in intact cells. In vivo studies of 7α-APTA in the DMBA-induced rat mammary carcinoma model resulted in 80% of the tumors responding completely or partially at doses of 25 and 50 mg/kg body wt/day. Thus, these 7α-substituted steroidal aromatase inhibitors are effective medicinal agents and may be useful for the treatment of estrogen-dependent breast cancer. |
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Research efforts over the past several years have focused on the synthesis of competitive and irreversible aromatase inhibitors and examination of these inhibitors in microsomal preparations, in cell culture, and in vivo. Several 7α-substituted androstenediones have demonstrated high affinity for placental aromatase, with apparent K"i's ranging from 1 to 30 nM. Inactivation of aromatase occurred following incubation with alkylating and enzyme-activated irreversible inhibitors. 7α-(4'-Amino)phenylthio-4-androstene-3,17-dione (7α-APTA) exhibits potent inhibitory activity of aromatase in the MCF-7 human mammary carcinoma cell line with an ED"5"0 of approximately 25 nM. The inhibitor did not bind to the estrogen receptor of the cells in vitro nor induce levels of progesterone receptors in intact cells. In vivo studies of 7α-APTA in the DMBA-induced rat mammary carcinoma model resulted in 80% of the tumors responding completely or partially at doses of 25 and 50 mg/kg body wt/day. Thus, these 7α-substituted steroidal aromatase inhibitors are effective medicinal agents and may be useful for the treatment of estrogen-dependent breast cancer. |
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Research efforts over the past several years have focused on the synthesis of competitive and irreversible aromatase inhibitors and examination of these inhibitors in microsomal preparations, in cell culture, and in vivo. Several 7α-substituted androstenediones have demonstrated high affinity for placental aromatase, with apparent K"i's ranging from 1 to 30 nM. Inactivation of aromatase occurred following incubation with alkylating and enzyme-activated irreversible inhibitors. 7α-(4'-Amino)phenylthio-4-androstene-3,17-dione (7α-APTA) exhibits potent inhibitory activity of aromatase in the MCF-7 human mammary carcinoma cell line with an ED"5"0 of approximately 25 nM. The inhibitor did not bind to the estrogen receptor of the cells in vitro nor induce levels of progesterone receptors in intact cells. In vivo studies of 7α-APTA in the DMBA-induced rat mammary carcinoma model resulted in 80% of the tumors responding completely or partially at doses of 25 and 50 mg/kg body wt/day. Thus, these 7α-substituted steroidal aromatase inhibitors are effective medicinal agents and may be useful for the treatment of estrogen-dependent breast cancer. |
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<?xml version="1.0" encoding="UTF-8"?><collection xmlns="http://www.loc.gov/MARC21/slim"><record><leader>01000caa a22002652 4500</leader><controlfield tag="001">NLEJ186564481</controlfield><controlfield tag="003">DE-627</controlfield><controlfield tag="005">20210707051734.0</controlfield><controlfield tag="007">cr uuu---uuuuu</controlfield><controlfield tag="008">070506s1987 xx |||||o 00| ||eng c</controlfield><datafield tag="035" ind1=" " ind2=" "><subfield code="a">(DE-627)NLEJ186564481</subfield></datafield><datafield tag="035" ind1=" " ind2=" "><subfield code="a">(DE-599)GBVNLZ186564481</subfield></datafield><datafield tag="040" ind1=" " ind2=" "><subfield code="a">DE-627</subfield><subfield code="b">ger</subfield><subfield code="c">DE-627</subfield><subfield code="e">rakwb</subfield></datafield><datafield tag="041" ind1=" " ind2=" "><subfield code="a">eng</subfield></datafield><datafield tag="245" ind1="1" ind2="0"><subfield code="a">7 α -Substituted androstenediones as effective in vttro and in vivo inhibitors of aromatase</subfield></datafield><datafield tag="264" ind1=" " ind2="1"><subfield code="c">1987</subfield></datafield><datafield tag="336" ind1=" " ind2=" "><subfield code="a">nicht spezifiziert</subfield><subfield code="b">zzz</subfield><subfield code="2">rdacontent</subfield></datafield><datafield tag="337" ind1=" " ind2=" "><subfield code="a">nicht spezifiziert</subfield><subfield code="b">z</subfield><subfield code="2">rdamedia</subfield></datafield><datafield tag="338" ind1=" " ind2=" "><subfield code="a">nicht spezifiziert</subfield><subfield code="b">zu</subfield><subfield code="2">rdacarrier</subfield></datafield><datafield tag="520" ind1=" " ind2=" "><subfield code="a">Research efforts over the past several years have focused on the synthesis of competitive and irreversible aromatase inhibitors and examination of these inhibitors in microsomal preparations, in cell culture, and in vivo. Several 7α-substituted androstenediones have demonstrated high affinity for placental aromatase, with apparent K"i's ranging from 1 to 30 nM. Inactivation of aromatase occurred following incubation with alkylating and enzyme-activated irreversible inhibitors. 7α-(4'-Amino)phenylthio-4-androstene-3,17-dione (7α-APTA) exhibits potent inhibitory activity of aromatase in the MCF-7 human mammary carcinoma cell line with an ED"5"0 of approximately 25 nM. The inhibitor did not bind to the estrogen receptor of the cells in vitro nor induce levels of progesterone receptors in intact cells. In vivo studies of 7α-APTA in the DMBA-induced rat mammary carcinoma model resulted in 80% of the tumors responding completely or partially at doses of 25 and 50 mg/kg body wt/day. Thus, these 7α-substituted steroidal aromatase inhibitors are effective medicinal agents and may be useful for the treatment of estrogen-dependent breast cancer.</subfield></datafield><datafield tag="533" ind1=" " ind2=" "><subfield code="f">Elsevier Journal Backfiles on ScienceDirect 1907 - 2002</subfield></datafield><datafield tag="700" ind1="1" ind2=" "><subfield code="a">Brueggemeier, R.W.</subfield><subfield code="4">oth</subfield></datafield><datafield tag="700" ind1="1" ind2=" "><subfield code="a">Pui-Kai, L.</subfield><subfield code="4">oth</subfield></datafield><datafield tag="700" ind1="1" ind2=" "><subfield code="a">Snider, C.E.</subfield><subfield code="4">oth</subfield></datafield><datafield tag="700" ind1="1" ind2=" "><subfield code="a">Darby, M.V.</subfield><subfield code="4">oth</subfield></datafield><datafield tag="700" ind1="1" ind2=" "><subfield code="a">Katlic, N.E.</subfield><subfield code="4">oth</subfield></datafield><datafield tag="773" ind1="0" ind2="8"><subfield code="i">in</subfield><subfield code="t">Steroids</subfield><subfield code="d">Amsterdam : Elsevier</subfield><subfield code="g">50(1987), 1-3, Seite 163-178</subfield><subfield code="w">(DE-627)NLEJ17701184X</subfield><subfield code="w">(DE-600)1498762-4</subfield><subfield code="x">0039-128X</subfield><subfield code="7">nnns</subfield></datafield><datafield tag="773" ind1="1" ind2="8"><subfield code="g">volume:50</subfield><subfield code="g">year:1987</subfield><subfield code="g">number:1-3</subfield><subfield code="g">pages:163-178</subfield></datafield><datafield tag="856" ind1="4" ind2="0"><subfield code="u">http://linkinghub.elsevier.com/retrieve/pii/0039-128X(83)90069-7</subfield></datafield><datafield tag="912" ind1=" " ind2=" "><subfield code="a">GBV_USEFLAG_H</subfield></datafield><datafield tag="912" ind1=" " ind2=" "><subfield code="a">ZDB-1-SDJ</subfield></datafield><datafield tag="912" ind1=" " ind2=" "><subfield code="a">GBV_NL_ARTICLE</subfield></datafield><datafield tag="951" ind1=" " ind2=" "><subfield code="a">AR</subfield></datafield><datafield tag="952" ind1=" " ind2=" "><subfield code="d">50</subfield><subfield code="j">1987</subfield><subfield code="e">1-3</subfield><subfield code="h">163-178</subfield></datafield></record></collection>
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