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RSS FeedsMolecules, Vol. 28, Pages 1196: Synthesis and Antiproliferative Activity of Steroidal Diaryl Ethers (Molecules)

 
 

25 january 2023 16:29:47

 
Molecules, Vol. 28, Pages 1196: Synthesis and Antiproliferative Activity of Steroidal Diaryl Ethers (Molecules)
 


Novel 13α-estrone derivatives have been synthesized via direct arylation of the phenolic hydroxy function. Chan–Lam couplings of arylboronic acids with 13α-estrone as a nucleophilic partner were carried out under copper catalysis. The antiproliferative activities of the newly synthesized diaryl ethers against a panel of human cancer cell lines (A2780, MCF-7, MDA-MB 231, HeLa, SiHa) were investigated by means of MTT assays. The quinoline derivative displayed substantial antiproliferative activity against MCF-7 and HeLa cell lines with low micromolar IC50 values. Disturbance of tubulin polymerization has been confirmed by microplate-based photometric assay. Computational calculations reveal significant interactions of the quinoline derivative with the taxoid binding site of tubulin.


 
47 viewsCategory: Biochemistry, Chemistry, Molecular Biology
 
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