Jansa, Josef, Lyčka, Antonín, Padělková, Zdeňka, Grepl, Martin, Konečný, Petr, Hajdúch, Marián, and Džubák, Petr
This work describes the synthesis of 8-iodoimidazo[1,2- c]pyrimidin-5(6 H)-one 2 from 5-iodocytosine 1. This compound was subjected to Suzuki with aryl and heteroarylboronic acids. After optimization, 10 products 3a, 3b, 3c, 3d, 3e, 3f, 3g, 3h, 3i, 3j were obtained in good yields 61-90%. Cytotoxic activity of all new products was evaluated on seven tumor cell lines including resistant variants and on normal human fibroblasts. Two derivatives showed promising and good therapeutic index in the case of 3h. [ABSTRACT FROM AUTHOR]