Synthesis and Antitumor Activity of Methoxy‐indolo[2,1‐a]isoquinolines

Methoxy‐indolo[2,1‐a]isoquinolines 8a‐f and their dihydroderivatives 7a‐f were synthesized by Bischler‐Napieralski reaction of the (bromomethoxyphenyl)‐[2‐(methoxyphenyl)‐ethyl]acetamides 4a‐f, reduction, subsequent cyclization and dehydrogenation. They were tested for cytostatic activity in vitro using P388 D1, leukemia and MDA MB 231 mammary tumor cells. The trimethoxy‐5,6‐dihydroindoloisoquinoline 7d and the tetramethoxyindoloisoquinoline 8f showed an inhibition of cellproliferation of about 70 % at a concentration of 10−5 molar.