11a-N-Tosyl-5-deoxi-pterocarpan (LQB-223), a promising prototype for targeting MDR leukemia cell lines

被引：15
作者：
Buarque, Camilla D. [1 ]
Salustiano, Eduardo J. [2 ]
Fraga, Kevin C. [1 ]
Alves, Bruna R. M. [1 ]
Costa, Paulo R. R. [2 ]
机构：
[1] Pontificia Univ Catolica Rio Janeiro, Dept Quim, BR-22435900 Gcivea Rio De Janeiro, RJ, Brazil
[2] Inst Bioquim Medico Leopoldo Meis, Ctr Ciencias, Lab Imunol Tumoral, BR-21941590 Rio De Janeiro, Brazil
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 78卷
关键词：
Aza-heck; Aza-arylation; Antileukemic activity; Sulfonamide; CHRONIC MYELOID-LEUKEMIA; RAPID COLORIMETRIC ASSAY; CARBONIC-ANHYDRASE; ANTINEOPLASIC ACTIVITY; MULTIDRUG-RESISTANCE; DERIVATIVES; INHIBITION; (+/-)-3,4-DIHYDROXY-8,9-METHYLENEDIOXYPTEROCARPAN; PTEROCARPANQUINONES; CYTOTOXICITY;
D O I：
10.1016/j.ejmech.2014.03.039
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Aza-deoxi-pterocarpans (1) were synthesized through palladium-catalyzed aza-arylation of dihydronaphtalen, and showed antineoplastic effect on MDR leukemic cell lines (K562, Lucena-1 and FEPS). Compounds 1c-d were prepared to identify the pharmacophoric group responsible for the activity as well as compounds 2a-c were prepared to evaluate the structural requirements in the D-ring. LQB-223 (1b) is the most promising antileukemic agent since it was the most active on MDR cells without detectable toxicity to normal immune system cells. (C) 2014 Elsevier Masson SAS. All rights reserved.
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收藏
页码：190 / 197
页数：8
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