http://www.cnr.it/ontology/cnr/individuo/prodotto/ID168629
Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors (Articolo in rivista)
- Type
- Label
- Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors (Articolo in rivista) (literal)
- Anno
- 2011-01-01T00:00:00+01:00 (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
- 10.1021/jm200734j (literal)
- Alternative label
Sbardella G, Mai A, Bartolini S, Castellano S, Cirilli R, Rotili D, Milite C, Santoriello M, Orlando S, Sciamanna I, Serafino A, Lavia P, Spadafora C. (2011)
Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors
in Journal of medicinal chemistry
(literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
- Sbardella G, Mai A, Bartolini S, Castellano S, Cirilli R, Rotili D, Milite C, Santoriello M, Orlando S, Sciamanna I, Serafino A, Lavia P, Spadafora C. (literal)
- Pagina inizio
- Pagina fine
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- Rivista
- Note
- ISI Web of Science (WOS) (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
- Dipartimento di Scienze Farmaceutiche e Biomediche, Università degli Studi di Salerno, Italy
Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Italy
Istituto Superiore di Sanità, Rome, Italy
Istituto di Biologia e Patologia MolecolarI, CNR, Rome, Italy
Istituto di Farmacologia Traslazionale, CNR, Rome, Italy (literal)
- Titolo
- Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors (literal)
- Abstract
- A series of 5-alkyl-2-(alkylthio)-6-(1-(2,6-difluorophenyl)propyl)-3,4-dihydropyrimidin-4(3H)-one derivatives (3a-h) belonging to the F(2)-DABOs class of non-nucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs) are endowed with a strong antiproliferative effect and induce cytodifferentiation in A375 melanoma cells. Among tested compounds, the most potent is 3g (SPV122), which also induces apoptosis in a cell-density-dependent manner and antagonizes tumor growth in animal models. All these effects are similar or even more pronounced than those previously reported for other nucleoside or non-nucleoside inhibitors of reverse transcriptase or by functional knockout of the reverse-transcriptase-encoding long interspersed element 1 by RNA interference (RNAi). Taken together with our previously reported results, these data further confirm our idea that cellular alterations induced by NNRTIs are a consequence of the inhibition of the endogenous reverse transcriptase in A375 cells and support the potential of NNRTIs as valuable agents in cancer therapy. (literal)
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