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Page 1
DNA Methyltransferases Inhibitors from Natural Sources.
Zwergel C, Valente S, Mai A. Zwergel C, et al. Among authors: mai a. Curr Top Med Chem. 2016;16(7):680-96. doi: 10.2174/1568026615666150825141505. Curr Top Med Chem. 2016. PMID: 26303417 Review.
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Mai A, Sbardella G, Artico M, Ragno R, Massa S, Novellino E, Greco G, Lavecchia A, Musiu C, La Colla M, Murgioni C, La Colla P, Loddo R. Mai A, et al. J Med Chem. 2001 Aug 2;44(16):2544-54. doi: 10.1021/jm010853h. J Med Chem. 2001. PMID: 11472208
5-Alkyl-2-(alkylthio)-6-(2,6-difluorobenzyl)-3,4-dihydropyrimidin-4(3H)-ones (S-DABOs, 2) have been recently described as a new class of human immunodeficiency virus type 1 (HIV-1) non-nucleoside reverse transcriptase (RT) inhibitors (NNRTIs) active at nanomolar concentrat …
5-Alkyl-2-(alkylthio)-6-(2,6-difluorobenzyl)-3,4-dihydropyrimidin-4(3H)-ones (S-DABOs, 2) have been recently described as a new class …
3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-alkylamides as a new class of synthetic histone deacetylase inhibitors. 1. Design, synthesis, biological evaluation, and binding mode studies performed through three different docking procedures.
Mai A, Massa S, Ragno R, Cerbara I, Jesacher F, Loidl P, Brosch G. Mai A, et al. J Med Chem. 2003 Feb 13;46(4):512-24. doi: 10.1021/jm021070e. J Med Chem. 2003. PMID: 12570373
Recently we reported a novel series of hydroxamates, called 3-(4-aroyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides (APHAs), acting as HDAC inhibitors (Massa, S.; et al. ...Such enhancement of inhibitory activity can be explained by the higher flexibility of the pyrrole C4-subs …
Recently we reported a novel series of hydroxamates, called 3-(4-aroyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides (APHAs), acting as HDA …
3-(4-Aroyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamides as a new class of synthetic histone deacetylase inhibitors. 2. Effect of pyrrole-C2 and/or -C4 substitutions on biological activity.
Mai A, Massa S, Cerbara I, Valente S, Ragno R, Bottoni P, Scatena R, Loidl P, Brosch G. Mai A, et al. J Med Chem. 2004 Feb 26;47(5):1098-109. doi: 10.1021/jm030990+. J Med Chem. 2004. PMID: 14971890
Previous SAR studies (Part 1: Mai, A.; et al. J. Med. Chem. 2003, 46, 512-524) performed on some portions (pyrrole-C4, pyrrole-N1, and hydroxamate group) of 3-(4-benzoyl-1-methyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamide (1a) highlighted its 4-phenylacetyl (1b) and 4- …
Previous SAR studies (Part 1: Mai, A.; et al. J. Med. Chem. 2003, 46, 512-524) performed on some portions (pyrrole-C4, pyrrole …
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