Synthesis and evaluation of 17 alpha-arylestradiols as ligands for estrogen receptor alpha and beta

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F10%3A00356112" target="_blank" >RIV/61388963:_____/10:00356112 - isvavai.cz</a>

Alternative codes found

RIV/68378050:_____/10:00356112

Result on the web

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DOI - Digital Object Identifier

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Result language

angličtina

Original language name

Synthesis and evaluation of 17 alpha-arylestradiols as ligands for estrogen receptor alpha and beta

Original language description

To identify novel estrogen receptor ligands a series of substituted 17 alpha-arylestradiols were synthesized using the catalytic [2 + 2 + 2]cyclotrimerization of 17 alpha-ethynylestradiol with various 1,7-diynes in the presence of Wilkinson's catalysts [Rh(PPH3)(3)Cl]. The compounds were subjected to competitive binding assays, cell-based luciferase reporter assays, and proliferation assays. These experiments confirmed their estrogenic character and revealed some interesting properties like mixed partial/full agonism for ER alpha/ER beta and different selectivity as a result of differing potencies for either ER.

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

EB - Genetics and molecular biology

OECD FORD branch

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Project

<a href="/en/project/LC06077" target="_blank" >LC06077: Center of Chemical Genetics</a><br>

Continuities

Z - Vyzkumny zamer (s odkazem do CEZ)

Publication year

2010

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Journal of Medicinal Chemistry

ISSN

0022-2623

e-ISSN

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Volume of the periodical

53

Issue of the periodical within the volume

10

Country of publishing house

US - UNITED STATES

Number of pages

5

Pages from-to

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UT code for WoS article

000277766900040

EID of the result in the Scopus database

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