title: Synthesis and antiproliferative activity of 6-phenylaminopurines.
abstract: A series of novel 6-phenylaminopurines have been efficiently synthesized in 3 steps exploring different groups at positions 2, 8 and 9 of the purine ring and at the exocyclic nitrogen atom at position 6. Among the newly described purines, five compounds showed antiproliferative activity with IC50 values below 10 μM, the tetrahydroquinoline derivative at position 6 of phenylaminopurine being the most active of the series in the six cell lines tested. Moreover, the compounds induced G2/M phase arrest in human cervical carcinoma HeLa cells as reported for tubulin depolymerizing agents.
authors.affiliation: Instituto de Química Médica (IQM-CSIC), c/Juan de la Cierva 3, E-28006 Madrid, Spain.
authors.forename: María-Dolores
authors.initials: MD
authors.lastname: Canela
authors.affiliation: KU Leuven - University of Leuven, Rega Institute for Medical Research, Minderboedersstraat 10 blok x - bus 1030, B-3000 Leuven, Belgium.
authors.forename: Sandra
authors.initials: S
authors.lastname: Liekens
authors.affiliation: Instituto de Química Médica (IQM-CSIC), c/Juan de la Cierva 3, E-28006 Madrid, Spain.
authors.forename: María-José
authors.initials: MJ
authors.lastname: Camarasa
authors.affiliation: Instituto de Química Médica (IQM-CSIC), c/Juan de la Cierva 3, E-28006 Madrid, Spain.
authors.forename: Eva María
authors.initials: EM
authors.lastname: Priego
authors.affiliation: Instituto de Química Médica (IQM-CSIC), c/Juan de la Cierva 3, E-28006 Madrid, Spain. Electronic address: mjperez@iqm.csic.es.
authors.forename: María-Jesús
authors.initials: MJ
authors.lastname: Pérez-Pérez
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D006801:Humans; D008958:Models, Molecular; D008968:Molecular Conformation; D011687:Purines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D055672:Static Electricity; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D011687:Purines
keywords: Antiproliferative agents; Cell cycle analysis; Microwave-assisted synthesis; Purines