title: Synthesis, biological evaluation and docking studies of 4-amino-tetrahydroquinazolino[3,2-e]purine derivatives.
abstract: The synthesis of new 4-amino-tetrahydroquinazolino[3,2-e]purine derivatives along with their activity in cell-free enzymatic assays on Src is reported. Some compounds emerged as moderately active inhibitors of the enzyme and showed antiproliferative effects on the murine leukemia L1210 cell line. Docking studies have been also performed to analyze the binding mode of compounds under study and to identify the structural determinants of their interaction. Therefore, this study provides a new promising scaffold with moderate enzymatic inhibitory activities for further development of new anticancer drugs targeting Src tyrosine kinase.
authors.affiliation: Laboratoire de Chimie Therapeutique, Faculte des Sciences Pharmaceutiques et Biologiques de Lille, 3 rue du Professeur Laguesse, 59000 Lille, France.
authors.forename: Valerie
authors.initials: V
authors.lastname: Verones
authors.forename: Nathalie
authors.initials: N
authors.lastname: Flouquet
authors.forename: Amaury
authors.initials: A
authors.lastname: Farce
authors.forename: Pascal
authors.initials: P
authors.lastname: Carato
authors.forename: Stephane
authors.initials: S
authors.lastname: Leonce
authors.forename: Bruno
authors.initials: B
authors.lastname: Pfeiffer
authors.forename: Pascal
authors.initials: P
authors.lastname: Berthelot
authors.forename: Nicolas
authors.initials: N
authors.lastname: Lebegue
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D011687:Purines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D019061:src-Family Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D011687:Purines; D011799:Quinazolines; D019061:src-Family Kinases