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Биотрансформация 1-β-D-рибофуранозил-4-метилмеркаптопиразоло-(3,4-d)пиримидина и его 5΄-монофосфатастатья
Статья опубликована в журнале из списка RSCI Web of Science
Статья опубликована в журнале из перечня ВАКСтатья опубликована в журнале из списка Web of Science и/или Scopus
- Авторы: Корбух И.А., Горюнова О.В., Стукалов Ю.В., Иванова Т.П., Добрынин Я.В., Преображенская М.Н.
- Журнал: Биоорганическая химия
- Том: 10
- Номер: 7
- Год издания: 1984
- Издательство: Российская академия наук
- Местоположение издательства: Москва
- Первая страница: 963
- Последняя страница: 969
- Аннотация: 1-beta-D-Ribofuranosyl-4-methylthiopyrazolo(3,4-d)pyrimidine (I) has been converted into its 5'-monophosphate (III) by reacting with POCl3 in trialkyl phosphates or by phosphorylating 2',3'-O-ethoxymethylidene derivative of riboside (I) using 2-cyanoethyl phosphate in the presence of DCC and subsequent removal of blocking groups. Condensation of nucleotide (III) imidazolide with pyrophosphoric acid afforded corresponding 5'-triphosphate. Pools of natural NTPs and riboside (I) phosphates were monitored by HPLC after administering riboside (I), phosphate (III), or 4-methylthiopyrazolo(3,4-d)pyrimidine (II) into mice with leukemia L1210 or after incubating CaOv culture cells with these compounds. Treatment with riboside (I) or nucleotide (III) possessing antileukemic and cytotoxic activites led to much higher level of monophosphate (III), than treatment with biologically inactive base (II). ATP and GTP levels in CaOv cells incubated with (I) or (III) decreased by 60-70%, whereas (II) did not affect NTP pool. Bioactivation of nucleoside (I) into monophosphate (III) proceeds via direct phosphorylation by adenosine kinase. No tranformation of (II) into (I) or (III) occurs under these conditions.
- Добавил в систему: Пугачева Ружена Борисовна