![]() |
ИСТИНА |
Войти в систему Регистрация |
ФНКЦ РР |
||
We developed a synthetic approach to new 4-fluoroalkyl-9Н-pyrimido[4,5-b]indoles by an intramolecular Heck cyclisation of 4-anilino-6-fluoroalkyl-5-iodopyrimidines in the presence of Pd(OAc)2 or CuI as catalysts. Individual 4-fluoroalkyl-9Н-pyrimido[4,5-b]indole derivatives showed preferential cytotoxicity toward the human myeloid leukemia К562 and colon carcinoma НСТ116 cell lines at low submicromolar concentrations whereas non-malignant counterparts were less sensitive. Mechanisms of cytotoxicity and a detailed synthesis of 4-fluoroalkyl-9Н-pyrimido[4,5-b]indoles are discussed.