Antitumor activity of clomiphene analogs in vitro: relationship to affinity for the estrogen receptor and another high affinity antiestrogen-binding site.

Murphy LC, Sutherland RL

The Journal of clinical endocrinology and metabolism1 Aug 1983Cited by 28 (Europe PMC)

PMID6408114DOI10.1210/jcem-57-2-373PepBankPUB-06408114

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Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study8

5 results from studies that gave the peptide. No result from this study comes from people.

01LabIn vitro (cells)Efficacy outcome
In MCF 7 cells, low-dose enclomiphene inhibited growth, and estradiol reversed this effect.
In plain wordsIn cells, low-dose enclomiphene inhibited breast cancer growth, but estradiol reversed this effect.
Peptide
Enclomiphene
Outcome
DecreaseCell growth inhibition at low doses
Study
humann: not reported in source
MCF 7 mammary carcinoma cells
Outcome group
Tumor growth · Cancer
Studied dose
0.25-1.0 microMAs given in this study (human).
Source sentences
Summary
At low doses (0.25-1.0 microM), where the growth-inhibitory effects were reversed by estradiol (except in the case of zuclomiphene), the relative antitumor activity (6866 greater than 10222 greater than enclomiphene greater than 9599 greater than zuclomiphene) was in the same order as RBA for RE.
1 context sentence(design, population, supporting numbers)
Summary · context
The antitumor activity of three enclomiphene (trans-1- (p-beta-diethylaminoethoxyphenyl)1,2-diphenyl-2-chloroethylene) analogs and the cis isomer zuclomiphene was investigated in MCF 7 human mammary carcinoma cells in culture.
Report a problemFND-0640811403
02LabIn vitro (cells)Efficacy outcome
In MCF 7 cells, low-dose enclomiphene was less potent than 6866 and 10222 but more potent than 9599 and zuclomiphene.
In plain wordsIn cells, low-dose enclomiphene inhibited growth less than 6866 and 10222 but more than 9599 and zuclomiphene.
Peptide
Enclomiphene
Outcome
MixedRelative antitumor potency at low doses
Study
humann: not reported in source
MCF 7 mammary carcinoma cells
Comparator
6866, 10222, 9599 and zuclomiphene
Outcome group
Tumor growth · Cancer
Studied dose
0.25-1.0 microMAs given in this study (human).
Source sentences
Summary
At low doses (0.25-1.0 microM), where the growth-inhibitory effects were reversed by estradiol (except in the case of zuclomiphene), the relative antitumor activity (6866 greater than 10222 greater than enclomiphene greater than 9599 greater than zuclomiphene) was in the same order as RBA for RE.
1 context sentence(design, population, supporting numbers)
Summary · context
The antitumor activity of three enclomiphene (trans-1- (p-beta-diethylaminoethoxyphenyl)1,2-diphenyl-2-chloroethylene) analogs and the cis isomer zuclomiphene was investigated in MCF 7 human mammary carcinoma cells in culture.
Report a problemFND-0640811404
03LabIn vitro (cells)Efficacy outcome
In MCF 7 cells, higher-dose enclomiphene was less potent than zuclomiphene but more potent than 6866, 10222 and 9599.
In plain wordsIn cells, higher-dose enclomiphene inhibited growth less than zuclomiphene but more than 6866, 10222 and 9599.
Peptide
Enclomiphene
Outcome
MixedRelative antitumor potency at higher doses
Study
humann: not reported in source
MCF 7 mammary carcinoma cells
Comparator
Zuclomiphene, 6866, 10222 and 9599
Outcome group
Tumor growth · Cancer
Studied dose
>2.5 microMAs given in this study (human).
Source sentences
Summary
Zuclomiphene became the most active, while the potency of enclomiphene increased relative to 6866 and 10222 (zuclomiphene greater than enclomiphene greater than 6866 greater than 10222 greater than 9599).
2 context sentences(design, population, supporting numbers)
Summary · context
At higher doses (greater than 2.5 microM), where the growth-inhibitory effects were unaffected or partially reversed by estradiol, the relative potencies of these compounds as antitumor agents changed.
Summary · context
The antitumor activity of three enclomiphene (trans-1- (p-beta-diethylaminoethoxyphenyl)1,2-diphenyl-2-chloroethylene) analogs and the cis isomer zuclomiphene was investigated in MCF 7 human mammary carcinoma cells in culture.
Report a problemFND-0640811405
04LabIn vitro (cell-free)Activity measurement
In MCF 7 cell extracts, enclomiphene had 2% relative estrogen receptor binding affinity, with estradiol defined as 100%.
In plain wordsIn lab tests, enclomiphene had 2% relative estrogen receptor binding affinity, with estradiol defined as 100%.
Peptide
Enclomiphene
Outcome
Not applicableEstrogen receptor relative binding affinity
Study
humann: not reported in source
MCF 7 cell-free extracts
Comparator
Estradiol = 100%
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
Dose not stated
Measurements
Relative binding affinity
2%
enclomiphene, estrogen receptor
Source sentences
Summary
Deethylation of the side chain (9599) reduced affinity for both sites by 65-70%, while a diethylaminoproproxy side chain (6866) resulted in a 3-fold increase in affinity for RE (enclomiphene = 2%; 6866 = 6%), but reduced the RBA for AEBS by 66% (enclomiphene = 140%; 6866 = 45%).
2 context sentences(design, population, supporting numbers)
Summary · context
Relative antitumor activity was compared with relative binding affinities (RBAs) for the nuclear estrogen receptor (RE; estradiol = 100%) and a microsomal antiestrogen-binding site (AEBS; tamoxifen = 100%) measured in cell-free extracts from MCF 7 cells.
Summary · context
The antitumor activity of three enclomiphene (trans-1- (p-beta-diethylaminoethoxyphenyl)1,2-diphenyl-2-chloroethylene) analogs and the cis isomer zuclomiphene was investigated in MCF 7 human mammary carcinoma cells in culture.
Report a problemFND-0640811401
05LabIn vitro (cell-free)Activity measurement
In MCF 7 cell extracts, enclomiphene had 140% relative antiestrogen-binding site affinity, with tamoxifen defined as 100%.
In plain wordsIn lab tests, enclomiphene had 140% relative antiestrogen-binding site affinity, with tamoxifen defined as 100%.
Peptide
Enclomiphene
Outcome
Not applicableAntiestrogen-binding site relative affinity
Study
humann: not reported in source
MCF 7 cell-free extracts
Comparator
Tamoxifen = 100%
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
Dose not stated
Measurements
Relative binding affinity
140%
enclomiphene, AEBS
Source sentences
Summary
Deethylation of the side chain (9599) reduced affinity for both sites by 65-70%, while a diethylaminoproproxy side chain (6866) resulted in a 3-fold increase in affinity for RE (enclomiphene = 2%; 6866 = 6%), but reduced the RBA for AEBS by 66% (enclomiphene = 140%; 6866 = 45%).
2 context sentences(design, population, supporting numbers)
Summary · context
Relative antitumor activity was compared with relative binding affinities (RBAs) for the nuclear estrogen receptor (RE; estradiol = 100%) and a microsomal antiestrogen-binding site (AEBS; tamoxifen = 100%) measured in cell-free extracts from MCF 7 cells.
Summary · context
The antitumor activity of three enclomiphene (trans-1- (p-beta-diethylaminoethoxyphenyl)1,2-diphenyl-2-chloroethylene) analogs and the cis isomer zuclomiphene was investigated in MCF 7 human mammary carcinoma cells in culture.
Report a problemFND-0640811402

Studies that did not test the peptide alone3

In this study, Enclomiphene was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking Enclomiphene.

06LabNot a test of Enclomiphene aloneIn vitro (cells)Mechanism
Across compounds including enclomiphene, estrogen-irreversible antitumor activity in MCF 7 cells was unrelated to estrogen receptor affinity.
In plain wordsIn cells, estrogen-irreversible growth inhibition across compounds including enclomiphene did not correlate with estrogen receptor affinity.
Peptide
Enclomiphene
Outcome
No significant changeEstrogen receptor affinity correlation at higher doses
Study
humann: not reported in source
MCF 7 mammary carcinoma cells
Outcome group
Tumor growth · Cancer
Source sentences
Summary
At these doses, estrogen-irreversible antitumor activity was unrelated to affinity for RE, but showed some correlation with affinity for AEBS.
2 context sentences(design, population, supporting numbers)
Summary · context
Zuclomiphene became the most active, while the potency of enclomiphene increased relative to 6866 and 10222 (zuclomiphene greater than enclomiphene greater than 6866 greater than 10222 greater than 9599).
Summary · context
The antitumor activity of three enclomiphene (trans-1- (p-beta-diethylaminoethoxyphenyl)1,2-diphenyl-2-chloroethylene) analogs and the cis isomer zuclomiphene was investigated in MCF 7 human mammary carcinoma cells in culture.
In this study, Enclomiphene was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Enclomiphene.
Report a problemFND-0640811406
07LabNot a test of Enclomiphene aloneIn vitro (cells)Mechanism
Across compounds including enclomiphene, estrogen-irreversible antitumor activity in MCF 7 cells showed some correlation with antiestrogen-binding site affinity.
In plain wordsIn cells, estrogen-irreversible growth inhibition across compounds including enclomiphene showed some correlation with antiestrogen-binding site affinity.
Peptide
Enclomiphene
Outcome
Direction not reportedAntiestrogen-binding site affinity correlation at higher doses
Study
humann: not reported in source
MCF 7 mammary carcinoma cells
Outcome group
Tumor growth · Cancer
Source sentences
Summary
At these doses, estrogen-irreversible antitumor activity was unrelated to affinity for RE, but showed some correlation with affinity for AEBS.
3 context sentences(design, population, supporting numbers)
Summary · context
Zuclomiphene became the most active, while the potency of enclomiphene increased relative to 6866 and 10222 (zuclomiphene greater than enclomiphene greater than 6866 greater than 10222 greater than 9599).
Summary · context
At higher doses (greater than 2.5 microM), where the growth-inhibitory effects were unaffected or partially reversed by estradiol, the relative potencies of these compounds as antitumor agents changed.
Summary · context
The antitumor activity of three enclomiphene (trans-1- (p-beta-diethylaminoethoxyphenyl)1,2-diphenyl-2-chloroethylene) analogs and the cis isomer zuclomiphene was investigated in MCF 7 human mammary carcinoma cells in culture.
In this study, Enclomiphene was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Enclomiphene.
Report a problemFND-0640811407
08LabNot a test of Enclomiphene aloneIn vitro (cells)Mechanism
In MCF 7 cells, growth inhibition by compounds including enclomiphene above 2.5 microM was unaffected or partly reversed by estradiol.
In plain wordsIn cells, estradiol left growth inhibition unchanged or partly reversed it at higher doses of compounds including enclomiphene.
Peptide
Enclomiphene
Outcome
MixedEstradiol reversal of growth inhibition at higher doses
Study
humann: not reported in source
MCF 7 mammary carcinoma cells
Outcome group
Tumor growth · Cancer
Source sentences
Summary
At higher doses (greater than 2.5 microM), where the growth-inhibitory effects were unaffected or partially reversed by estradiol, the relative potencies of these compounds as antitumor agents changed.
2 context sentences(design, population, supporting numbers)
Summary · context
Zuclomiphene became the most active, while the potency of enclomiphene increased relative to 6866 and 10222 (zuclomiphene greater than enclomiphene greater than 6866 greater than 10222 greater than 9599).
Summary · context
The antitumor activity of three enclomiphene (trans-1- (p-beta-diethylaminoethoxyphenyl)1,2-diphenyl-2-chloroethylene) analogs and the cis isomer zuclomiphene was investigated in MCF 7 human mammary carcinoma cells in culture.
In this study, Enclomiphene was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Enclomiphene.
Report a problemFND-0640811408

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
21 Oct 2026, 15:58 UTC
Study results updated
Version 1
21 Oct 2026, 12:50 UTC
First added · source update from Europe PMC

Subjects

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