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Molecules, Vol. 23, Pages 1572: In Vitro and In Vivo Anti-Breast Cancer Activities of Some Synthesized Pyrazolinyl-estran-17-one Candidates

Molecules, Vol. 23, Pages 1572: In Vitro and In Vivo Anti-Breast Cancer Activities of Some Synthesized Pyrazolinyl-estran-17-one Candidates

Molecules doi: 10.3390/molecules23071572

Authors: Abd El-Galil E. Amr Mohamed El-Naggar Mohamed A. Al-Omar Elsayed Ahmed Elsayed Mohamed M. Abdalla

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.

Authors:   Amr, Abd El-Galil E.; El-Naggar, Mohamed ; Al-Omar, Mohamed A.; Elsayed, Elsayed Ahmed; Abdalla, Mohamed M.
Journal:   Molecules
Volume:   23
edition:   7
Year:   2018
Pages:   1572
DOI:   10.3390/molecules23071572
Publication date:   28-Jun-2018
Facts, background information, dossiers
  • molecules
  • breast cancer
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