+++Curr Med Chem (1999)

[privalov]

Всем энтузиастам большой привет!
У меня есть задача от шефа: найти статью, которой нет в онлайне, поэтому прошу помочь.
ТТХ:
Curr Med Chem 1999 Jul;6(7):615-28.

Minakawa N1, Matsuda A

Mechanism-based design of inosine 5-monophosphate dehydrogenase inhibitors: synthesis and biological activities of 5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (EICAR) and its derivatives.

Abstract
Inosine 5 -monophosphate dehydrogenase (IMPDH) catalyzes the nicotinamide adenine dinucleotide (NAD)-dependent oxidation of inosine 5 -monophosphate (IMP) to xanthosine 5 -monophosphate (XMP), and is one of the key rate-determining enzymes of de novo guanine nucleotide biosynthesis in mammalian systems. Based on the proposed catalytic mechanism of IMPDH, we designed and synthesized 5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (5b, EICAR) from 5-amino-1-beta-D-ribofuranosylimida-zole-4-carboxamide (AICAR) via palladium chemistry.EICAR is a potent cytostatic agent that inhibits various tumor cells in culture including human solid tumor cells in vitro and in vivo. EICAR also showed broad-spectrum antiviral activities, about 10- to 100-fold greater than those of ribavirin. An examination of the structure-activity relationships revealed that an alkynyl group, especially an ethynyl group at the 5-position, is important for its activity due to the inhibition of IMPDH. The mode of action of EICAR is also discussed.

Буду очень признателен!

[aiven1978]

Качество правда не очень, т.к. скачено с гуглбукс. Может кто лучше найдет.

[privalov]

Большое спасибо! Никак не ожидал такого быстрого ответа!