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Design and synthesis of 21-alkynylaryl pregnenolone derivatives and evaluation of their anticancer activity

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National Hellenic Research Foundation (NHRF)   

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Design and synthesis of 21-alkynylaryl pregnenolone derivatives and evaluation of their anticancer activity
Mavrofrydi O.
Pantzou A.
Szalóki G.
Προύσης, Κυριάκος
Papazafiri P.
Καλογεροπούλου, Θεοδώρα
Άρθρο σε επιστημονικό περιοδικό
2014
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 0.54 μM and drastic inhibition of the prosurvival PI3K-Akt/PKB pathway.
Φαρμακευτική χημεία (EL)
Pharmaceutical chemistry (EN)
Alkynylaryl derivatives (EN)
Anticancer activity (EN)
Pregnenolone (EN)
English
Elsevier Ltd
Bioorganic and Medicinal Chemistry
© 2014 Elsevier Ltd. All rights reserved.
© 2014 Elsevier Ltd. All rights reserved. (EN)
National Hellenic Research Foundation (NHRF)
Helios - Repository of the National Hellenic Research Foundation (NHRF)



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