(2-phenyl-1,3,2]dithiarsolan-4-yl)-methanol derivatives show in vitro antileukemic activity

被引:14
作者
Gibaud, S
Alfonsi, R
Mutzenhardt, P
Fries, I
Astier, A
机构
[1] Univ Henri Poincare, Fac Pharm, EA 3452, Lab Pharm Clin, F-54000 Nancy, France
[2] Univ Henri Poincare, Fac Sci, RMN, Serv Commun, F-54506 Vandoeuvre Les Nancy, France
关键词
arsenic; melarsoprol; arsthinol; leukemia; toxicity;
D O I
10.1016/j.jorganchem.2005.11.007
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
The antileukemic activity of a series of (2-Phenyl-[1,3,2]dithiarsolan-4-yl)-methanol derivatives was tested on K562 and U937 human leukemia cell lines. Their systemic toxicity was estimated by the corresponding LD50 on mice. The cytotoxic activity of each derivative was significantly better than that of arsenic trioxide and the therapeutic index (T.I. = LD50/IC50) was improved. No correlation between log P and the activity or the toxicity was found. (c) 2005 Elsevier B.V. All rights reserved.
引用
收藏
页码:1081 / 1084
页数:4
相关论文
共 18 条
[1]   Arsenic induces apoptosis in B-cell leukaemic cell lines in vitro: activation of caspases and down-regulation of Bcl-2 protein [J].
Akao, Y ;
Mizoguchi, H ;
Kojima, S ;
Naoe, T ;
Ohishi, N ;
Yagi, K .
BRITISH JOURNAL OF HAEMATOLOGY, 1998, 102 (04) :1055-1060
[2]   Arylaminoheterocyclic compounds I Synthetic method [J].
Banks, CK .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1944, 66 :1127-1130
[3]   ARSENICAL-RESISTANT TRYPANOSOMES LACK AN UNUSUAL ADENOSINE TRANSPORTER [J].
CARTER, NS ;
FAIRLAMB, AH .
NATURE, 1993, 361 (6408) :173-176
[4]  
Chen GQ, 1996, BLOOD, V88, P1052
[5]  
Friedheim E., 1942, United States Patent, Patent No. [2,295,574, 2295574]
[6]  
FRIEDHEIM EAH, 1947, P SOC EXP BIOL MED, V65, P180, DOI 10.3181/00379727-65-15902
[7]  
FRIEDHEIM EAH, 1953, Patent No. 2659723
[8]   RE-EXAMINATION AND FURTHER DEVELOPMENT OF A PRECISE AND RAPID DYE METHOD FOR MEASURING CELL-GROWTH CELL KILL [J].
HANSEN, MB ;
NIELSEN, SE ;
BERG, K .
JOURNAL OF IMMUNOLOGICAL METHODS, 1989, 119 (02) :203-210
[9]   The importance of 2,3-dimercaptopropinol (British anti-lewisite, BAL) in the trypanocidal activity of topical melarsoprol [J].
Jennings, FW ;
Atouguia, JM ;
Murray, M .
ACTA TROPICA, 1996, 62 (02) :83-89
[10]   Comparative activity of melarsoprol and arsenic trioxide in chronic B-cell leukemia lines [J].
Konig, A ;
Wrazel, L ;
Warrell, RP ;
Rivi, R ;
Pandolfi, PP ;
Jakubowski, A ;
Gabrilove, JL .
BLOOD, 1997, 90 (02) :562-570