SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME ACYCLICα-(1H-PYRAZOLO[3,4-d]PYRIMIDIN-4-YL)THIOALKYLAMIDE NUCLEOSIDES

Autor:	M. L. Taha, Jean-Jacques Vasseur, Omar Moukha-Chafiq, E. De Clercq, Hassan B. Lazrek
Rok vydání:	2002
Předmět:	Chemistry Stereochemistry Nucleosides Biological activity Microbial Sensitivity Tests General Medicine Alkylation Antiviral Agents Biochemistry Chemical synthesis chemistry.chemical_compound Pyrimidines Chlorocebus aethiops Tumor Cells Cultured Genetics Animals Pyrazoles Molecular Medicine Drug Screening Assays Antitumor Vero Cells DNA Biological evaluation
Zdroj:	Nucleosides, Nucleotides and Nucleic Acids. 21:165-176
ISSN:	1532-2335 1525-7770
DOI:	10.1081/ncn-120003180
Popis:	The chemical synthesis of some acyclic alpha-(1H-pyrazolo[3,4-d]pyrimidin-4-yl)thioalkylamide nucleosides (10-12)a-c is described. The treatment of IH-pyrazolo[3,4-d]pyrimidin-4-thione 1 with compounds 2a-c gave, regioselectively, ethyl alpha-(1H-pyrazolo[3,4-d]pyrimidin-4-yl)thioalkylates 3a-c, respectively. These heterocycles were alkylated, separately, with alkylating agents 4, 5 and 6 to give, regioselectively, the N1-acyclic nucleosides (7-9)a-c which were deprotected to afford the desired products (10-12)a-c. All synthetic compounds were characterized on the basis of their physical and spectroscopic properties. The products (10-12)a-c were evaluated for their inhibitory effects against the replication of HIV-1 (III(B)), HIV-2 (ROD), various DNA viruses, a variety of tumor-cell lines and M. tuberculosis. No marked biological activity was found.
Databáze:	OpenAIRE
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