Synthesis and antiproliferative activity of 2,4-disubstituted 6-aryl-7H-pyrrolo[3,2-d]pyrimidin-7-one 5-oxides

被引：17
作者：
Pudziuvelyte, Erika [1 ]
Rios-Luci, Carla [2 ,3 ]
Leon, Leticia G. [2 ,3 ]
Cikotiene, Inga [1 ]
Padron, Jose M. [2 ,3 ]
机构：
[1] Vilnius State Univ, Fac Chem, Dept Organ Chem, LT-03225 Vilnius, Lithuania
[2] Univ La Laguna, IUBO AG, San Cristobal la Laguna 38206, Spain
[3] ICIC, Biolab, San Cristobal la Laguna 38206, Spain
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 14期
关键词：
Pyrrolo[3,2-d]pyrimidine; Privileged structure; Antitumor drugs; Cell cycle arrest; RECEPTOR ANTAGONISTS; CYTOTOXICITY; INHIBITORS; CULTURES; ANALOGS;
D O I：
10.1016/j.bmc.2009.05.078
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A series of 2,4-disubstituted 6-aryl-7H-pyrrolo[3,2-d] pyrimidin-7-one 5-oxides were synthesized and in vitro antiproliferative activities were examined in the human solid tumor cell lines A2780, HBL-100, HeLa, SW1573, T-47D, and WiDr. The most potent analog induced considerably growth inhibition in the range 0.35-2.0 mu M. Cell cycle studies in the breast and lung cancer cells revealed arrest in the G(2)/M compartment. The results showed that the title compounds bearing alkylamino or dialkylamino moieties in position 2 of the pyrimidine ring are more active than those bearing hydrogen or methylthio groups. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4955 / 4960
页数：6
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