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In Vitro and In Vivo Anti-Breast Cancer Activities of Some Synthesized Pyrazolinyl-estran-17-one Candidates.
- Source :
-
Molecules (Basel, Switzerland) [Molecules] 2018 Jun 28; Vol. 23 (7). Date of Electronic Publication: 2018 Jun 28. - Publication Year :
- 2018
-
Abstract
- A series of estrone derivatives, 2 ⁻ 4 , were synthesized from the corresponding arylidine estrone, 2a , b , as starting materials, which were prepared by condensation of estrone (3-hydroxy-estran-17-one, 1) with 4-bromobenzaldehyde and thiophene-2-aldehyde. Treating of 2a , b with hydrazine derivatives in acetic acid or propionic acid afforded pyrazoline derivatives, 3a ⁻ f and 4a ⁻ f , respectively. Furthermore, results proved the superiority of thienyl derivatives over 4-bromophenol derivatives in terms of cytotoxic effects on MCF-7 cancer cells. In vivo xenograft breast cancer animal model experiments revealed that the synthesized derivatives can be used for decreasing tumor volume, while the most potent derivative ( 4f ) decreased the development of tumor volume by about 87.0% after 12 days.
Details
- Language :
- English
- ISSN :
- 1420-3049
- Volume :
- 23
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Molecules (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 29958453
- Full Text :
- https://doi.org/10.3390/molecules23071572