Covalent analogues of DNA base-pairs and triplets. Part 2. Synthesis and cytostatic activity of bis(purin-6-yl) acetylenes, -diacetylenes and related compounds

The title bis(purin-6-yl)acetylenes, -diacetylenes, -ethylenes and -ethanes were prepared as covalent base-pair analogues starting from 6-ethynylpurines and 6-iodopurines by cross-coupling and homo-coupling reactions and hydrogenations. The bis(purin-6-yl)acetylenes and -diacetylenes exhibited significant cytostatic activity in vitro (IC50=0.4-1.0 mumol/l). (C) 2002 Elsevier Science Ltd. All rights reserved.