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Chemical manipulations on the 1,4-dioxane ring of 5-HT1A receptor agonists lead to antagonists endowed with antitumor activity in prostate cancer cells.
Del Bello F, Bonifazi A, Giorgioni G, Quaglia W, Amantini C, Morelli MB, Santoni G, Battiti FO, Vistoli G, Cilia A, Piergentili A. Del Bello F, et al. Among authors: cilia a. Eur J Med Chem. 2019 Apr 15;168:461-473. doi: 10.1016/j.ejmech.2019.02.056. Epub 2019 Feb 25. Eur J Med Chem. 2019. PMID: 30844609
The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HT1A receptor over α1-adrenoceptor and D2-like receptor subtypes.
Del Bello F, Bonifazi A, Giannella M, Giorgioni G, Piergentili A, Petrelli R, Cifani C, Micioni Di Bonaventura MV, Keck TM, Mazzolari A, Vistoli G, Cilia A, Poggesi E, Matucci R, Quaglia W. Del Bello F, et al. Among authors: cilia a. Eur J Med Chem. 2017 Jan 5;125:233-244. doi: 10.1016/j.ejmech.2016.09.026. Epub 2016 Sep 9. Eur J Med Chem. 2017. PMID: 27662034
Multitarget 1,4-Dioxane Compounds Combining Favorable D2-like and 5-HT1A Receptor Interactions with Potential for the Treatment of Parkinson's Disease or Schizophrenia.
Del Bello F, Ambrosini D, Bonifazi A, Newman AH, Keck TM, Giannella M, Giorgioni G, Piergentili A, Cappellacci L, Cilia A, Franchini S, Quaglia W. Del Bello F, et al. Among authors: cilia a. ACS Chem Neurosci. 2019 May 15;10(5):2222-2228. doi: 10.1021/acschemneuro.8b00677. Epub 2019 Jan 9. ACS Chem Neurosci. 2019. PMID: 30609891 Free PMC article.
1,3-Dioxane as a scaffold for potent and selective 5-HT1AR agonist with in-vivo anxiolytic, anti-depressant and anti-nociceptive activity.
Franchini S, Sorbi C, Linciano P, Carnevale G, Tait A, Ronsisvalle S, Buccioni M, Del Bello F, Cilia A, Pirona L, Denora N, Iacobazzi RM, Brasili L. Franchini S, et al. Among authors: cilia a. Eur J Med Chem. 2019 Aug 15;176:310-325. doi: 10.1016/j.ejmech.2019.05.024. Epub 2019 May 11. Eur J Med Chem. 2019. PMID: 31112892
Synthesis and structure-activity relationships of novel arylpiperazines as potent antagonists of α1-adrenoceptor.
Silva RO, de Oliveira AS, Nunes Lemes LF, de Camargo Nascente L, Coelho do Nascimento Nogueira P, Silveira ER, Brand GD, Vistoli G, Cilia A, Poggesi E, Buccioni M, Marucci G, Bolognesi ML, Romeiro LAS. Silva RO, et al. Among authors: cilia a. Eur J Med Chem. 2016 Oct 21;122:601-610. doi: 10.1016/j.ejmech.2016.06.052. Epub 2016 Jun 30. Eur J Med Chem. 2016. PMID: 27448917
The Versatile 2-Substituted Imidazoline Nucleus as a Structural Motif of Ligands Directed to the Serotonin 5-HT1A Receptor.
Del Bello F, Cilia A, Carrieri A, Fasano DC, Ghelardini C, Di Cesare Mannelli L, Micheli L, Santini C, Diamanti E, Giannella M, Giorgioni G, Mammoli V, Paoletti CD, Petrelli R, Piergentili A, Quaglia W, Pigini M. Del Bello F, et al. Among authors: cilia a. ChemMedChem. 2016 Oct 19;11(20):2287-2298. doi: 10.1002/cmdc.201600383. Epub 2016 Sep 30. ChemMedChem. 2016. PMID: 27690321
Synthesis, biological evaluation and molecular modeling of 1-oxa-4-thiaspiro- and 1,4-dithiaspiro[4.5]decane derivatives as potent and selective 5-HT1A receptor agonists.
Franchini S, Manasieva LI, Sorbi C, Battisti UM, Fossa P, Cichero E, Denora N, Iacobazzi RM, Cilia A, Pirona L, Ronsisvalle S, Aricò G, Brasili L. Franchini S, et al. Among authors: cilia a. Eur J Med Chem. 2017 Jan 5;125:435-452. doi: 10.1016/j.ejmech.2016.09.050. Epub 2016 Sep 17. Eur J Med Chem. 2017. PMID: 27689727 Free article.
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
Franchini S, Prandi A, Baraldi A, Sorbi C, Tait A, Buccioni M, Marucci G, Cilia A, Pirona L, Fossa P, Cichero E, Brasili L. Franchini S, et al. Among authors: cilia a. Eur J Med Chem. 2010 Sep;45(9):3740-51. doi: 10.1016/j.ejmech.2010.05.023. Epub 2010 May 15. Eur J Med Chem. 2010. PMID: 20605276
48 results