Synthesis and antiproliferative activity of 6-phenylaminopurines

Eur J Med Chem. 2014 Nov 24:87:421-8. doi: 10.1016/j.ejmech.2014.09.093.

María-Dolores Canela ¹, Sandra Liekens ², María-José Camarasa ¹, Eva María Priego ¹, María-Jesús Pérez-Pérez ³

Affiliations

1 Instituto de Química Médica (IQM-CSIC), c/Juan de la Cierva 3, E-28006 Madrid, Spain.
2 KU Leuven - University of Leuven, Rega Institute for Medical Research, Minderboedersstraat 10 blok x - bus 1030, B-3000 Leuven, Belgium.
3 Instituto de Química Médica (IQM-CSIC), c/Juan de la Cierva 3, E-28006 Madrid, Spain. Electronic address: mjperez@iqm.csic.es.

PMID: 25282265 DOI: 10.1016/j.ejmech.2014.09.093

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.

Keywords

Antiproliferative agents; Cell cycle analysis; Microwave-assisted synthesis; Purines.

Name
Email *

	Sorry, but the email address you supplied was invalid.