Journal
MOLECULES
Volume 23, Issue 7, Pages -Publisher
MDPI
DOI: 10.3390/molecules23071572
Keywords
steroidal scaffold; estrone; biological activities; cytotoxicty; anti-breast cancer
Funding
- Deanship of Scientific Research, king Saud University
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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.
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