Document Detail

Design and synthesis of 21-alkynylaryl pregnenolone derivatives and evaluation of their anticancer activity.
MedLine Citation:
PMID:  25456391     Owner:  NLM     Status:  In-Data-Review    
A series of novel C21-alkynylaryl derivatives of pregnenolone were synthesized and screened for anticancer activity against a panel of seven human cancer cell lines (LNCaP, A549, MCF7, HeLa, A431, HepG2, HT29). The data revealed that these compounds can be potential antitumour agents against the specific cell models. Compound 6f bearing a 2-trifluoromethylphenyl group displayed improved cytotoxicity towards all cancer cell lines used. A431 cells were the most sensitive with derivatives 6e-6h bearing electron withdrawing substituents exhibiting high potency with IC50 values ranging between 2.18 and 0.54μM and drastic inhibition of the prosurvival PI3K-Akt/PKB pathway.
György Szalóki; Athanasia Pantzou; Kyriakos C Prousis; Olga Mavrofrydi; Panagiota Papazafiri; Theodora Calogeropoulou
Publication Detail:
Type:  Journal Article     Date:  2014-10-25
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  22     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2014 Dec 
Date Detail:
Created Date:  2014-12-03     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  6980-8     Citation Subset:  IM    
Copyright Information:
Copyright © 2014 Elsevier Ltd. All rights reserved.
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