Synthesis and Antiproliferative Evaluation of Spirothiadiazolopyridazine Derivatives

被引：4
|
作者：
Sekkak, Hanan [1 ]
Mojahidi, Souad [1 ]
Rakib, El Mostapha [1 ]
Abouricha, Said [1 ]
Kerbal, Abdelali [2 ]
Aiello, Cinzia [3 ]
Viale, Maurizio [3 ]
机构：
[1] Univ Sultan Moulay Slimane, Lab Chim Organ & Analyt, Fac Sci & Tech, Beni Mellal, Morocco
[2] Univ Sidi Mohammed Ben Abdellah, Fac Sci Dhar El Mehraz, Chim Organ Lab, Dept Chim, Fes, Morocco
[3] Ist Nazl Ric Canc, SC Terapia Immunol, I-16132 Genoa, Italy
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2010年 / 7卷 / 10期
关键词：
Pyridazinethione; Spirothiadiazolopyridazine; Cytotoxic activity; 1,3-DIPOLAR CYCLOADDITION; REGIOSELECTIVE SYNTHESIS; SPIRO PYRROLIDINES; SPIROHETEROCYCLES; AGENTS;
D O I：
10.2174/1570180811007010743
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The 1,3-dipolar cycloaddition of N-aryl-C-ethoxycarbonylnitrile imines to pyridazin-3-thione afforded novel spirothiadiazolopyridazines in moderate to good yields. The reaction occurs regioselectively at the exocyclic C=S bond. Some of the newly synthesized compounds were tested for their in vitro antitumor activity against three human and murine cell lines [human: A2780, (ovary, carcinoma), A549 (lung, carcinoma); murine: P388 (leukaemia)]. Among the series, some compounds exhibited significant growth inhibitory effects against cell lines P388.
引用
收藏
页码：743 / 746
页数：4
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