1998
DOI: 10.1016/s0960-0760(97)00197-0
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1-Benzyl-2-phenylindole- and 1,2-diphenylindole-based antiestrogens. Estimation of agonist and antagonist activities in transfection assays

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Cited by 33 publications
(25 citation statements)
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“…After binding of hormonally active compounds to the ER, the resulting ER/drug conjugates interact after dimerization with the ERE at the plasmid and activate the reporter sequence which codes for luciferase. The expression of luciferase correlates very well with the estrogenic potency of the drug [19].…”
Section: Biological Activitymentioning
confidence: 91%
“…After binding of hormonally active compounds to the ER, the resulting ER/drug conjugates interact after dimerization with the ERE at the plasmid and activate the reporter sequence which codes for luciferase. The expression of luciferase correlates very well with the estrogenic potency of the drug [19].…”
Section: Biological Activitymentioning
confidence: 91%
“…In 2009, a second class of phenylindole dendrimer conjugates have been developed [162]. These class of ER ligands (2-phenylindoles) have been previously shown to inhibit mammary tumor growth [163] and, as for EDC, the polyamine conjugation process allowed indoles to retain an high binding affinity for ER [162].…”
Section: The Extranuclear Er Mechanisms As Targets For Anticancer Drugsmentioning
confidence: 99%
“…Several groups including our own have shown that the structure of the side chain in steroidal and non-steroidal antiestrogens is crucial for the degree of antagonism that can be reached [4,8,9] . The main role of the carrier molecule is to guarantee both receptor binding and the correct orientation of the side chain inside the binding pocket.…”
Section: Introductionmentioning
confidence: 99%