Phenothiazine-based CaaX competitive inhibitors of human farnesyltransferase bearing a cysteine, methionine, serine or valine moiety as a new family of antitumoral compounds

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 20, 2015, Pages 4447-4452

  Dumitriu, Gina Mirabela ^a   Bîcu, Elena ^a   Belei, Dalila ^a   Rigo, Benoît ^b,c   Dubois, Joëlle ^d   Farce, Amaury ^b,e   Ghinet, Alina ^a,b,c  

^a ALEXANDRU IOAN CUZA UNIVERSITY OF IASI   (Romania)

^b INSERM   (France)

^c Laboratoire de Pharmacochimie   (France)

^d INSTITUT DE CHIMIE DES SUBSTANCES NATURELLES   (France)

^e UNIV LILLE   (France)

Author keywords

CAAX inhibitor; Cysteine; Farnesyltransferase; Methionine; Phenothiazine; Serine; Valine

Indexed keywords

ANTINEOPLASTIC AGENT; CYSTEINE; METHIONINE; PHENOTHIAZINE DERIVATIVE; PROTEIN FARNESYLTRANSFERASE INHIBITOR; SERINE; VALINE; AMINO ACID; ENZYME INHIBITOR; FARNESYL TRANS TRANSFERASE; PHENOTHIAZINE;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CATALYSIS; COMPETITIVE INHIBITION; CONTROLLED STUDY; DRUG CONFORMATION; DRUG DESIGN; DRUG SCREENING; DRUG SYNTHESIS; HUMAN; IC50; MOLECULAR DOCKING; QUANTITATIVE STRUCTURE ACTIVITY RELATION; SAPONIFICATION; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; METABOLISM; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

AMINO ACIDS; ANTINEOPLASTIC AGENTS; CYSTEINE; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INHIBITORS; FARNESYLTRANSTRANSFERASE; HUMANS; METHIONINE; MOLECULAR STRUCTURE; PHENOTHIAZINES; SERINE; STRUCTURE-ACTIVITY RELATIONSHIP; VALINE;

EID: 84942827530     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.09.008     Document Type: Article

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