FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2079647883> ?p ?o ?g. }

• W2079647883 abstract "Five putative iodinated progesterone receptor (PR) binding ligands were synthesized and evaluated as potential imaging agents for PR-positive human breast tumours. Two compounds (E- and Z-17-hydroxy-21-iodo-19-nor-17alpha-pregna-4,20-dien-3-one; E- and Z-IPG1) were previously described, but are re-evaluated. The other three were novel compounds: two nortestosterone analogues derived from ORG 3236 (E- and Z-13-ethyl-17-hydroxy-21-iodo-11-methylene-18,19-dinor-17alpha-pre gna-4,20-diene-3-one; E- and Z-IPG2) and one norprogesterone analogue derived from ORG 2058 (21-[4-iodophenoxy]-16alpha-ethyl-19-norpregn-4-ene-3, 20-dione; IPG3). The E-iodovinyl nortestosterone compounds were obtained by a new route of synthesis. Competitive binding studies were performed to determine their binding affinities for the PR in three types of tissue (human MCF-7 breast tumour cells and rat uterine and mammary tumour tissue) and for the androgen receptor (AR) in human MCF-7 breast tumour cells, as well as for the sex hormone-binding globulin (SHBG) and corticosteroid-binding globulin (CBG) in human plasma. All four 17alpha-iodovinyl nortestosterone derivatives displayed high binding affinity for the human PR, that of Z-IPG1 and E- and Z-IPG2 being even higher than that of ORG2058. Their affinities for the rat PR were somewhat lower, especially those of both E-isomers. The affinity of IPG3 was lower for both the human and rat PR. The nortestosterone derivatives also showed AR binding, the relative binding affinities ranging from 4.3 to 17.0% as compared with 5alphaDHT. Additionally, neither of these steroids displayed any significant binding to either SHBG or CBG in human plasma. We conclude that the in vitro binding properties of all four 17alpha-iodovinyl nortestosterone derivatives warrant evaluation of the distribution characteristics of their 123I-labelled analogues to determine their usefulness as PR imaging agents." @default.
• W2079647883 created "2016-06-24" @default.
• W2079647883 creator A5015854605 @default.
• W2079647883 creator A5021278800 @default.
• W2079647883 creator A5041877658 @default.
• W2079647883 creator A5044958395 @default.
• W2079647883 creator A5051182148 @default.
• W2079647883 creator A5085896083 @default.
• W2079647883 date "1998-11-01" @default.
• W2079647883 modified "2023-09-27" @default.
• W2079647883 title "New iodinated progestins as potential ligands for progesterone receptor imaging in breast cancer. part 1: synthesis and in vitro pharmacological characterization" @default.
• W2079647883 cites W1871085519 @default.
• W2079647883 cites W1963908442 @default.
• W2079647883 cites W1964625082 @default.
• W2079647883 cites W1967679508 @default.
• W2079647883 cites W1982684003 @default.
• W2079647883 cites W1983660015 @default.
• W2079647883 cites W1983793378 @default.
• W2079647883 cites W1987026350 @default.
• W2079647883 cites W1988105358 @default.
• W2079647883 cites W1993800646 @default.
• W2079647883 cites W1995487052 @default.
• W2079647883 cites W2008329556 @default.
• W2079647883 cites W2008797955 @default.
• W2079647883 cites W2010774737 @default.
• W2079647883 cites W2012041763 @default.
• W2079647883 cites W2012254875 @default.
• W2079647883 cites W2023286468 @default.
• W2079647883 cites W2028373255 @default.
• W2079647883 cites W2040791520 @default.
• W2079647883 cites W2043813981 @default.
• W2079647883 cites W2052519080 @default.
• W2079647883 cites W2053177046 @default.
• W2079647883 cites W2053317448 @default.
• W2079647883 cites W2053925035 @default.
• W2079647883 cites W2058623521 @default.
• W2079647883 cites W2059571548 @default.
• W2079647883 cites W2060481646 @default.
• W2079647883 cites W2061648353 @default.
• W2079647883 cites W2066547059 @default.
• W2079647883 cites W2070394498 @default.
• W2079647883 cites W2084468371 @default.
• W2079647883 cites W2093055398 @default.
• W2079647883 cites W2107496898 @default.
• W2079647883 cites W2108870738 @default.
• W2079647883 cites W2128635872 @default.
• W2079647883 cites W2130944389 @default.
• W2079647883 cites W2150150420 @default.
• W2079647883 cites W2186658896 @default.
• W2079647883 cites W2217039510 @default.
• W2079647883 cites W2220500259 @default.
• W2079647883 cites W2346662122 @default.
• W2079647883 cites W2352854009 @default.
• W2079647883 cites W2396158642 @default.
• W2079647883 cites W2466127369 @default.
• W2079647883 doi "https://doi.org/10.1016/s0969-8051(98)00041-9" @default.
• W2079647883 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/9863567" @default.
• W2079647883 hasPublicationYear "1998" @default.
• W2079647883 type Work @default.
• W2079647883 sameAs 2079647883 @default.
• W2079647883 citedByCount "6" @default.
• W2079647883 countsByYear W20796478832013 @default.
• W2079647883 countsByYear W20796478832020 @default.
• W2079647883 crossrefType "journal-article" @default.
• W2079647883 hasAuthorship W2079647883A5015854605 @default.
• W2079647883 hasAuthorship W2079647883A5021278800 @default.
• W2079647883 hasAuthorship W2079647883A5041877658 @default.
• W2079647883 hasAuthorship W2079647883A5044958395 @default.
• W2079647883 hasAuthorship W2079647883A5051182148 @default.
• W2079647883 hasAuthorship W2079647883A5085896083 @default.
• W2079647883 hasConcept C121608353 @default.
• W2079647883 hasConcept C126322002 @default.
• W2079647883 hasConcept C134018914 @default.
• W2079647883 hasConcept C170493617 @default.
• W2079647883 hasConcept C185592680 @default.
• W2079647883 hasConcept C202751555 @default.
• W2079647883 hasConcept C2777911890 @default.
• W2079647883 hasConcept C2780283098 @default.
• W2079647883 hasConcept C2780902042 @default.
• W2079647883 hasConcept C2994423619 @default.
• W2079647883 hasConcept C30092816 @default.
• W2079647883 hasConcept C530470458 @default.
• W2079647883 hasConcept C55493867 @default.
• W2079647883 hasConcept C71240020 @default.
• W2079647883 hasConcept C71315377 @default.
• W2079647883 hasConcept C71924100 @default.
• W2079647883 hasConcept C81358767 @default.
• W2079647883 hasConcept C84606932 @default.
• W2079647883 hasConcept C86803240 @default.
• W2079647883 hasConcept C90134679 @default.
• W2079647883 hasConcept C98717036 @default.
• W2079647883 hasConceptScore W2079647883C121608353 @default.
• W2079647883 hasConceptScore W2079647883C126322002 @default.
• W2079647883 hasConceptScore W2079647883C134018914 @default.
• W2079647883 hasConceptScore W2079647883C170493617 @default.
• W2079647883 hasConceptScore W2079647883C185592680 @default.
• W2079647883 hasConceptScore W2079647883C202751555 @default.
• W2079647883 hasConceptScore W2079647883C2777911890 @default.
• W2079647883 hasConceptScore W2079647883C2780283098 @default.
• W2079647883 hasConceptScore W2079647883C2780902042 @default.

• next