Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines

A seriesof twenty four acyclic unsaturated 2,6-substututed purines 5a-20b were synthesized. These compounds were evaluated for cytotoxic activity against NCI-60 DTP human tumor cell line screen at 10µM concentration. N(9)-[(Z)-4'-chloro-2'-butenyl-1'-yl]-2,6-dichloropurine(5a), N(9)-[...

Descripción completa

Detalles Bibliográficos
Autores principales: Kode, Nageswara Rao, Phadtare, Shashikant
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2011
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6264448/
https://www.ncbi.nlm.nih.gov/pubmed/21747338
http://dx.doi.org/10.3390/molecules16075840
_version_ 1783375499058216960
author Kode, Nageswara Rao
Phadtare, Shashikant
author_facet Kode, Nageswara Rao
Phadtare, Shashikant
author_sort Kode, Nageswara Rao
collection PubMed
description A seriesof twenty four acyclic unsaturated 2,6-substututed purines 5a-20b were synthesized. These compounds were evaluated for cytotoxic activity against NCI-60 DTP human tumor cell line screen at 10µM concentration. N(9)-[(Z)-4'-chloro-2'-butenyl-1'-yl]-2,6-dichloropurine(5a), N(9)-[4'-chloro-2'-butynyl-1'-yl]-2,6-dichloropurine(10a), N(9)-[(E)-2',3'-dibromo-4'-chloro-2'-butenyl-1'-yl]-6-methoxypurine(14) and N(9)-[4'-chloro-2'-butynyl-1'-yl]-6-(4-methoxyphenyl)-purine(19) exhibited highly potent cytotoxic activity with GI(50) values in the 1–5 µM range for most human tumor cell lines. Other compounds exhibited moderate activity.
format Online
Article
Text
id pubmed-6264448
institution National Center for Biotechnology Information
language English
publishDate 2011
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-62644482018-12-10 Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines Kode, Nageswara Rao Phadtare, Shashikant Molecules Article A seriesof twenty four acyclic unsaturated 2,6-substututed purines 5a-20b were synthesized. These compounds were evaluated for cytotoxic activity against NCI-60 DTP human tumor cell line screen at 10µM concentration. N(9)-[(Z)-4'-chloro-2'-butenyl-1'-yl]-2,6-dichloropurine(5a), N(9)-[4'-chloro-2'-butynyl-1'-yl]-2,6-dichloropurine(10a), N(9)-[(E)-2',3'-dibromo-4'-chloro-2'-butenyl-1'-yl]-6-methoxypurine(14) and N(9)-[4'-chloro-2'-butynyl-1'-yl]-6-(4-methoxyphenyl)-purine(19) exhibited highly potent cytotoxic activity with GI(50) values in the 1–5 µM range for most human tumor cell lines. Other compounds exhibited moderate activity. MDPI 2011-07-11 /pmc/articles/PMC6264448/ /pubmed/21747338 http://dx.doi.org/10.3390/molecules16075840 Text en © 2011 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Kode, Nageswara Rao
Phadtare, Shashikant
Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines
title Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines
title_full Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines
title_fullStr Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines
title_full_unstemmed Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines
title_short Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines
title_sort synthesis and cytotoxic activity of some new 2,6-substituted purines
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6264448/
https://www.ncbi.nlm.nih.gov/pubmed/21747338
http://dx.doi.org/10.3390/molecules16075840
work_keys_str_mv AT kodenageswararao synthesisandcytotoxicactivityofsomenew26substitutedpurines
AT phadtareshashikant synthesisandcytotoxicactivityofsomenew26substitutedpurines

Ejemplares similares