SYNTHESIS AND CYTOTOXIC ACTIVITY ON ISLETS OF LANGERHANS OF BENZAMIDE THIOSEMICARBAZONE DERIVATIVES

被引：13

作者：

CAMPANA, M

LABORIE, C

BARBIER, G

ASSAN, R

MILCENT, R

机构：

[1] UNIV PARIS 07,FAC MED XAVIER BICHAT,CHIM ORGAN MED LAB,UNITE RECH CHIM & PHARMACOL,F-75018 PARIS,FRANCE

[2] UNIV PARIS 07,FAC MED XAVIER BICHAT,DIABETOL EXPTL & CLIN LAB,F-75018 PARIS,FRANCE

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 26卷 / 03期

关键词：

BENZAMIDE THIOSEMICARBAZONE DERIVATIVES; BENZAMIDE SEMICARBAZONE DERIVATIVES; LANGERHANS ISLETS;

D O I：

10.1016/0223-5234(91)90059-V

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Eleven 1-(4-substituted alpha-arylaminobenzylidene)thiosemicarbazides 1 and the related semicarbazones 2 were synthesized and tested in vitro for their inhibitory effects on the islets of Langerhans. Only the thiosemicarbazones 1 suppressed the insulin and glucagon secretions while the somatostatin release persisted. The 1-(alpha-anilino-4-methylbenzylidene)thiosemicarbazide 1f was the most potent suppressor of insulin release and lysed the islet beta cells. Zinc sulfate protected islets from the suppressive and toxic effects of 1f. These compounds 1 could be potential drugs for the treatment of insulinomas.

引用

页码：273 / 278

页数：6

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[2]

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[3]

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