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

页码：4955 / 4960

页数：6

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