Compounds > cdri 85-287
Page last updated: 2024-12-08

cdri 85-287

Description

CDRI 85-287: structure given in first source; an antiestrogen and antiimplantation agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID159508
CHEMBL ID27283
SCHEMBL ID6669000
MeSH IDM0182783

Synonyms (16)

Synonym
nsc607873
nsc-607873
cdri 85-287
cdri-85-287
2-(4-(2-piperidinoethoxy)phenyl)-3-phenyl-2h-1-benzopyran
cdri-85/287
1-(2-(4-(3-phenyl-2h-1-benzopyran-2-yl)phenoxy)ethyl)piperidine
piperidine, 1-(2-(4-(3-phenyl-2h-1-benzopyran-2-yl)phenoxy)ethyl)-
2-(4-(2-n-piperidino)ethoxyphenyl)-3-phenyl(2h)benzo(b)pyran
CHEMBL27283
130064-18-5
1-[2-[4-(3-phenyl-2h-chromen-2-yl)phenoxy]ethyl]piperidine
SCHEMBL6669000
DTXSID30926582
1-{2-[4-(3-phenyl-2h-1-benzopyran-2-yl)phenoxy]ethyl}piperidine
PD162080

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
"5 mg/kg body weight) of the compound administered on days 1, 2 or 3 of pregnancy or multiple dosing (0."( Biological profile of 2-[4-(2-N-piperidinoethoxy) phenyl]-3-phenyl (2H) benzo (b) pyran--a potent antiimplantation agent in rat.
Dhar, JD; Duran, S; Kapil, RS; Setty, BS, 1991)		0.28
" This was prevented by ormeloxifene and the effect, though apparently more in females supplemented with higher dose of ormeloxifene, was not always significantly different and clear dose-response was not evident until BMD data was evaluated on T-/Z-score basis."( In vitro anti-resorptive activity and prevention of ovariectomy-induced osteoporosis in female Sprague-Dawley rats by ormeloxifene, a selective estrogen receptor modulator.
Arshad, M; Ghosh, R; Sawlani, V; Sengupta, S; Sharma, S; Singh, MM, 2004)		0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID186399Antiestrogenic activity in presence of unlabeled estradiol as mean uterine weight in rats after 0.3 ug dose1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Effect of the side chain and its position on the activity of 2,3-diaryl-2H-1-benzopyrans.
AID38726Relative binding affinity against Antiestrogen binding site(AEBS)1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID70669Mean percent inhibition of Estrogen receptor beta in rat1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Effect of the side chain and its position on the activity of 2,3-diaryl-2H-1-benzopyrans.
AID187060Estrogenic activity as mean uterine weight in rats on 10 ug dose1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID38725Relative binding affinity against Antiestrogen binding site(AEBS)1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Effect of the side chain and its position on the activity of 2,3-diaryl-2H-1-benzopyrans.
AID187059Antiestrogenic activity in presence of unlabeled estradiol as mean uterine weight in rats at 0.3 ug dose1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID69530Relative binding affinity against estrogen receptor(ER)1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Effect of the side chain and its position on the activity of 2,3-diaryl-2H-1-benzopyrans.
AID69512Relative binding affinity(RBA) against Estrogen receptor in rat liver1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Synthesis of 2-(p-chlorobenzyl)-3-aryl-6-methoxybenzofurans as selective ligands for antiestrogen-binding sites. Effects on cell proliferation and cholesterol synthesis.
AID186407Estrogenic activity as mean uterine weight in rats on 10 ug dose1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Effect of the side chain and its position on the activity of 2,3-diaryl-2H-1-benzopyrans.
AID69688Relative binding affinity against estrogen receptor(ER)1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID185420Percent inhibition of estradiol stimulated uterine growth in rats1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
AID38618Relative binding affinity(RBA) against AEBS (Antiestrogen binding site) in rat liver1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Synthesis of 2-(p-chlorobenzyl)-3-aryl-6-methoxybenzofurans as selective ligands for antiestrogen-binding sites. Effects on cell proliferation and cholesterol synthesis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (22)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's18 (81.82)18.2507
2000's1 (4.55)29.6817
2010's3 (13.64)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other22 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
nafoxidine
Nafoxidine: An estrogen antagonist that has been used in the treatment of breast cancer.		1.9810benzenes;
naphthalenes;
ring assembly
proadifen
Proadifen: An inhibitor of drug metabolism and CYTOCHROME P-450 ENZYME SYSTEM activity.		1.9810diarylmethane
trifluoperazine
[no description available]		1.9910N-alkylpiperazine;
N-methylpiperazine;
organofluorine compound;
phenothiazines		antiemetic;
calmodulin antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor;
phenothiazine antipsychotic drug
ethinyl estradiol
Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration.		2.021017-hydroxy steroid;
3-hydroxy steroid;
terminal acetylenic compound		xenoestrogen
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		1.9710mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
dihydrotestosterone
Dihydrotestosterone: A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.. 17beta-hydroxyandrostan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4-5 double bond has been reduced to a single bond with unspecified configuration at position 5.. 17beta-hydroxy-5alpha-androstan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4,5 double bond has been reduced to a single bond with alpha-configuration at position 5.		2.432017beta-hydroxy steroid;
17beta-hydroxyandrostan-3-one;
3-oxo-5alpha-steroid		androgen;
Daphnia magna metabolite;
human metabolite;
mouse metabolite
glycerylphosphorylcholine
Glycerylphosphorylcholine: A component of PHOSPHATIDYLCHOLINES or LECITHINS, in which the two hydroxy groups of GLYCEROL are esterified with fatty acids. (From Stedman, 26th ed)		1.9910glycerophosphocholine
trioxifene
trioxifene: RN given refers to parent cpd		1.9710
finasteride
Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.. finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia.		2.07103-oxo steroid;
aza-steroid;
delta-lactam		androgen antagonist;
antihyperplasia drug;
EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor
ly 117018
LY 117018: from Eli Lilly; less estrogenic & more estrogen-antagonistic than tamoxifen & trioxifene in rats & mice; LY 139478 is the HCl salt of LY 117018; LY 139478 is an estrogen agonist; structure in first source; a raloxifene analog. LY 117018 : A member of the class of 1-benzothiophenes that is raloxifene in which the piperidin-1-yl group has been replaced by a pyrrolidin-1-yl group.		2.67301-benzothiophenes;
aromatic ketone;
N-alkylpyrrolidine;
phenols		bone density conservation agent;
estrogen receptor antagonist;
estrogen receptor modulator
tesmilifene
[no description available]		1.9810diarylmethane
centchroman
Centchroman: A non-steroidal anti-fertility agent with anti-hormonal properties.		3.150
n-acetylneuraminic acid
N-Acetylneuraminic Acid: An N-acyl derivative of neuraminic acid. N-acetylneuraminic acid occurs in many polysaccharides, glycoproteins, and glycolipids in animals and bacteria. (From Dorland, 28th ed, p1518). N-acetylneuraminic acid : An N-acylneuraminic acid where the N-acyl group is specified as acetyl.		1.9910N-acetylneuraminic acidsantioxidant;
bacterial metabolite;
EC 3.2.1.18 (exo-alpha-sialidase) inhibitor;
human metabolite;
mouse metabolite
diethylstilbestrol
Diethylstilbestrol: A synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders. It was also used formerly as a growth promoter in animals. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), diethylstilbestrol has been listed as a known carcinogen. (Merck, 11th ed). diethylstilbestrol : An olefinic compound that is trans-hex-3-ene in which the hydrogens at positions 3 and 4 have been replaced by p-hydroxyphenyl groups.		2.3820olefinic compound;
polyphenol		antifungal agent;
antineoplastic agent;
autophagy inducer;
calcium channel blocker;
carcinogenic agent;
EC 1.1.1.146 (11beta-hydroxysteroid dehydrogenase) inhibitor;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
endocrine disruptor;
xenoestrogen
afimoxifene
afimoxifene : A tertiary amino compound that is tamoxifen in which the phenyl group which is in a Z- relationship to the ethyl substituent is hydroxylated at the para- position. It is the active metabolite of tamoxifen.		2.0710phenols;
tertiary amino compound		antineoplastic agent;
estrogen receptor antagonist;
metabolite
tamoxifen
[no description available]		3.2460stilbenoid;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
piperidines
Piperidines: A family of hexahydropyridines.		4.35200
epidermal growth factor
Epidermal Growth Factor: A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.		2.0810
cyclin d1
Cyclin D1: Protein encoded by the bcl-1 gene which plays a critical role in regulating the cell cycle. Overexpression of cyclin D1 is the result of bcl-1 rearrangement, a t(11;14) translocation, and is implicated in various neoplasms.		2.0810
contraceptives, postcoital
Contraceptives, Postcoital: Contraceptive substances to be used after COITUS. These agents include high doses of estrogenic drugs; progesterone-receptor blockers; ANTIMETABOLITES; ALKALOIDS, and PROSTAGLANDINS.		1.9710
ConditionIndicatedRelationship StrengthStudiesTrials
Breast Cancer
[description not available]		02.4920
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.4920
Adenoma, Prostatic
[description not available]		02.0710
Prostatic Hyperplasia
Increase in constituent cells in the PROSTATE, leading to enlargement of the organ (hypertrophy) and adverse impact on the lower urinary tract function. This can be caused by increased rate of cell proliferation, reduced rate of cell death, or both.		02.0710
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.0210
Bone Loss, Osteoclastic
[description not available]		02.4120
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.0210
Age-Related Osteoporosis
[description not available]		02.0210
Osteoporosis
Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.		02.0210
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		03.2460
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