Design, synthesis, estrogenic and antiestrogenic activities of some triarylpyrazole derivatives
New triarylpyrazole derivatives, substituted with basic side chain, polar group or heterocyclic ring were designed and synthesized. Nineteen compounds were tested for their in vivo uterotrophic activity. Animals treated with compounds 9 , 15a , 15c , 19a , 19f , 20a , and 21b showed pronounced incre...
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Veröffentlicht in: | Medicinal chemistry research 2017-11, Vol.26 (11), p.2785-2808 |
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Hauptverfasser: | , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | New triarylpyrazole derivatives, substituted with basic side chain, polar group or heterocyclic ring were designed and synthesized. Nineteen compounds were tested for their in vivo uterotrophic activity. Animals treated with compounds
9
,
15a
,
15c
,
19a
,
19f
,
20a
, and
21b
showed pronounced increase in uterine weight. It is worth mentioning that compound
19f
was more active than estradiol as an estrogenic compound as evidenced by the increased dry uterine weight. Additionally, compound
19a
produced 128.25% increase in dry uterine weight relative to estradiol. On the other hand, eight compounds were screened for their in vivo antiuterotrophic activity. Animals treated with compounds
5e
,
5f
,
8
, and
13b
showed pronounced decrease in uterine weight. The highest antiuterotrophic effect was observed in mice receiving compound
13b
, which was as potent as the positive control, tamoxifen as evident by the decrease in the uterine wet weight. |
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ISSN: | 1054-2523 1554-8120 |
DOI: | 10.1007/s00044-017-1977-8 |