Simple route to ferrocenylalkyl nucleobases. Antitumor activity <i>in vivo</i>

Abstract

Abstract Ferrocenylalkyl nucleobases ( 1 – 14 ) were prepared via the reaction of the α‐(hydroxy)alkyl ferrocenes FcCHR(OH) (Fc = ferrocenyl; R = H, Me, Et, Ph) with thymine, cytosine, iodo‐cytosine and adenine in DMSO at 100 °C, yields being 50–80%. The antitumor activities of ferrocenylmethyl thymine ( 1 ) against solid tumor models, carcinoma 755 (Ca755) and Lewis lung carcinoma (LLC) were studied in vivo . Therapeutic synergism of antitumor activity against LLC was demonstrated in the case of combined application of compound 1 with anticancer drug cyclophosphamide. Copyright © 2009 John Wiley &amp; Sons, Ltd.