close

Вход

Забыли?

вход по аккаунту

?

код для вставки
2004
Fused pyridine derivatives
R 0450
Synthesis of Nitrated Indenoisoquinolines as Topoisomerase I Inhibitors. — The
of increasing the biological activity of indenoisoquinolines by capitalizing
46- 143 possibility
on potential π-stacking interactions is investigated by introduction of an electron-withdrawing nitro substituent on the isoquinoline ring. Schiff bases (II) are condensed with
nitrohomophthalic anhydride (I) followed by treatment of the condensation product
(III) with P2O5 as a dehydrating agent to affect the ring closure. The construction of a
propylamine substituent on the lactam nitrogen is accompanied by an unexpected oxidation, changing the dihydroindenoisoquinoline skeleton of (IVb) into the indenoisoquinoline skeleton of (V). The new molecules are tested for their in vitro anticancer
activities against 55 cell lines as well as for topoisomerase I inhibition. Substances like
(IV), (V), and (VI) are potent top I inhibitors with sub-micromolar cytotoxicity mean
graph midpoints (MGM) and top I inhibition equal to camptothecin. — (MORRELL,
A.; ANTONY, S.; KOHLHAGEN, G.; POMMIER, Y.; CUSHMAN*, M.; Bioorg.
Med. Chem. Lett. 14 (2004) 14, 3659-3663; Dep. Med. Chem. Mol. Pharmacol., Sch.
Pharm. Pharm. Sci., Purdue Univ., West Lafayette, IN 47907, USA; Eng.) —
H. Hoennerscheid
Документ
Категория
Без категории
Просмотров
0
Размер файла
21 Кб
Теги
1/--страниц
Пожаловаться на содержимое документа