title: Constrained analogues of procaine as novel small molecule inhibitors of DNA methyltransferase-1.
abstract: Constrained analogues of procaine were synthesized, and their inhibiting activity against DNMT1 was tested. Among them, the most potent compound, derivative 3b, was also able to induce a recognizable demethylation of chromosomal satellite repeats in HL60 human myeloid leukemia cells and thus represents a lead compound for the development of a novel class of non-nucleoside DNMT1 inhibitors.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano (SA), Italy.
authors.forename: Sabrina
authors.initials: S
authors.lastname: Castellano
authors.forename: Dirk
authors.initials: D
authors.lastname: Kuck
authors.forename: Marina
authors.initials: M
authors.lastname: Sala
authors.forename: Ettore
authors.initials: E
authors.lastname: Novellino
authors.forename: Frank
authors.initials: F
authors.lastname: Lyko
authors.forename: Gianluca
authors.initials: G
authors.lastname: Sbardella
mesh_terms: D045744:Cell Line, Tumor; D000076123:DNA (Cytosine-5-)-Methyltransferase 1; D004248:DNA (Cytosine-5-)-Methyltransferases / Q000037:antagonists & inhibitors*; D019175:DNA Methylation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D008970:Molecular Weight; D010080:Oxazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011343:Procaine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D010080:Oxazoles; D011994:Recombinant Proteins; D011343:Procaine; D000076123:DNA (Cytosine-5-)-Methyltransferase 1; D004248:DNA (Cytosine-5-)-Methyltransferases; C000619380:DNMT1 protein, human