close

Вход

Забыли?

вход по аккаунту

?

код для вставки
2005
Fused pyrimidine derivatives
R 0515
Antiproliferative Activity of New 1-Aryl-4-amino-1H-pyrazolo[3,4-d]pyrimidine
Toward the Human Epidermoid Carcinoma A431 Cell Line. — The
11- 160 Derivatives
title pyrazolopyrimidines (VI) and (IX), structurally related to pyrazolo[3,4-d]pyrimidines with potent inhibitory activity towards EGFR tyrosine kinase, but possessing a
2-chloro-2-phenylethyl or a styryl chain on the N-1 of the pyrazole ring, are synthesized
and their biological evaluation is carried out. Compounds (VIa) and (IX) inhibit the
tyrosine-threonine MEK kinase activity responsible for ERK phosphorylation. In particular (VIa) emerges as a potent inhibitor of EGFR dependent tumor cell growth
(e.g. A431) and its inhibitory effect appears to be not related to the inhibition of protein
tyrosine kinase EGFR, but associated with both the Src and MAPK pathways. —
(SCHENONE*, S.; et al.; Eur. J. Med. Chem. 39 (2004) 11, 939-946; Dip. Sci. Farm.,
Univ. Studi Genova, I-16132 Genova, Italy; Eng.) — H. Hoennerscheid
Документ
Категория
Без категории
Просмотров
0
Размер файла
20 Кб
Теги
1/--страниц
Пожаловаться на содержимое документа