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Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
Nawrozkij MB, Forgione M, Yablokov AS, Lucidi A, Tomaselli D, Patsilinakos A, Panella C, Hailu GS, Kirillov IA, Badia R, Riveira-Muñoz E, Crespan E, Armijos Rivera JI, Cirilli R, Ragno R, Esté JA, Maga G, Mai A, Rotili D. Nawrozkij MB, et al. J Med Chem. 2019 Jan 24;62(2):604-621. doi: 10.1021/acs.jmedchem.8b01238. Epub 2018 Dec 20. J Med Chem. 2019. PMID: 30525601
Conformational restriction applied to dihydrobenzylpyrimidin-4-(3 H)-ones (DABOs) by the intoduction of a methyl group at the alpha-benzylic position is known to massively improve the anti-HIV-1 activity of these compounds. Here, we report the effects of methoxy substituti …
Conformational restriction applied to dihydrobenzylpyrimidin-4-(3 H)-ones (DABOs) by the intoduction of a methyl group at the alpha-b …
6-[1-(2,6-difluorophenyl)ethyl]pyrimidinones antagonize cell proliferation and induce cell differentiation by inhibiting (a nontelomeric) endogenous reverse transcriptase.
Bartolini S, Mai A, Artico M, Paesano N, Rotili D, Spadafora C, Sbardella G. Bartolini S, et al. J Med Chem. 2005 Nov 3;48(22):6776-8. doi: 10.1021/jm0507330. J Med Chem. 2005. PMID: 16250634
The two compounds significantly reduced cell proliferation and facilitated the morphological differentiation of cells. These results propose F(2)-DABOs as useful tools in preventive and/or curative therapy to counteract the loss of differentiation in dedifferentiating path …
The two compounds significantly reduced cell proliferation and facilitated the morphological differentiation of cells. These results propose …