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

页码：743 / 746

页数：4

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