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一些新型 2,6-取代嘌呤的合成及细胞毒性活性。

Synthesis and cytotoxic activity of some new 2,6-substituted purines.

机构信息

Division of Basic Pharmaceutical Sciences, , College of Pharmacy, Xavier University of Louisiana, New Orleans, LA 70125, USA.

出版信息

Molecules. 2011 Jul 11;16(7):5840-60. doi: 10.3390/molecules16075840.

DOI:10.3390/molecules16075840
PMID:21747338
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6264448/
Abstract

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 10µMconcentration. N₉-[(Z)-4'-chloro-2'-butenyl-1'-yl]-2,6-dichloropurine(5a), N₉-[4'-chloro-2'-butynyl-1'-yl]-2,6-dichloropurine(10a), N₉-[(E)-2',3'-dibromo-4'-chloro-2'-butenyl-1'-yl]-6-methoxypurine(14)and N₉-[4'-chloro-2'-butynyl-1'-yl]-6-(4-methoxyphenyl)-purine(19)exhibited highly potent cytotoxic activity with GI₅₀ values in the 1-5 µM range for most human tumor cell lines. Other compounds exhibited moderate activity.

摘要

合成了一系列二十四种无环不饱和 2,6-取代嘌呤 5a-20b。这些化合物在 10µM 浓度下针对 NCI-60 DTP 人肿瘤细胞系筛选进行了细胞毒性活性评估。N₉-[(Z)-4'-氯-2'-丁烯基-1'-基]-2,6-二氯嘌呤(5a)、N₉-[4'-氯-2'-丁炔基-1'-基]-2,6-二氯嘌呤(10a)、N₉-[(E)-2',3'-二溴-4'-氯-2'-丁烯基-1'-基]-6-甲氧基嘌呤(14)和 N₉-[4'-氯-2'-丁炔基-1'-基]-6-(4-甲氧基苯基)-嘌呤(19)对大多数人类肿瘤细胞系表现出高度有效的细胞毒性活性，GI₅₀ 值在 1-5µM 范围内。其他化合物表现出中等活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c355/6264448/f4261c810c51/molecules-16-05840-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c355/6264448/d6479d12ddb9/molecules-16-05840-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c355/6264448/85a8cc32ab5c/molecules-16-05840-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c355/6264448/4c25f7b3095d/molecules-16-05840-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c355/6264448/7682bf35dfde/molecules-16-05840-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c355/6264448/49d376a3fea9/molecules-16-05840-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c355/6264448/f4261c810c51/molecules-16-05840-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c355/6264448/d6479d12ddb9/molecules-16-05840-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c355/6264448/85a8cc32ab5c/molecules-16-05840-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c355/6264448/4c25f7b3095d/molecules-16-05840-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c355/6264448/7682bf35dfde/molecules-16-05840-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c355/6264448/49d376a3fea9/molecules-16-05840-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c355/6264448/f4261c810c51/molecules-16-05840-g006.jpg

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