含1,3-苯并二氧杂环戊烯系统的新型肽基衍生物的合成、抗肿瘤及抗菌活性

Synthesis, antitumour and antimicrobial activities of new peptidyl derivatives containing the 1,3-benzodioxole system.

作者信息

Leite Ana Cristina Lima, da Silva Kezia Peixoto, de Souza Ivone A, de Araújo Janete Magali, Brondani Dalci José

机构信息

Labsinfa, Departamento de Ciências Farmacêuticas, Universidade Federal de Pernambuco--Rua Prof. Artur Sá S/N, CDU, 50740-520, Recife, Pernambuco, Brazil.

出版信息

Eur J Med Chem. 2004 Dec;39(12):1059-65. doi: 10.1016/j.ejmech.2004.09.007.

DOI:10.1016/j.ejmech.2004.09.007

PMID:15571867

Abstract

Two series of 5 and 6-substituted 1,3-benzodioxole peptidyl derivatives were synthesized and evaluated as antitumour and antimicrobial agents. The compounds that could be conveniently prepared in a few steps processes from natural safrole have been characterised by IR and 1H-NMR spectroscopy. In vivo antitumor activity tests showed that some of the compounds were able to inhibit carcinoma S-180 tumour growth in mice. The in vitro antimicrobial activity of all compounds revealed that they are able to promote the growth of some organisms, including Bacillus subtilis.

摘要

合成了两个系列的5-和6-取代的1,3-苯并二恶唑肽基衍生物，并将其作为抗肿瘤和抗菌剂进行了评估。这些化合物可以通过几步反应从天然黄樟素方便地制备出来，已通过红外光谱和1H-核磁共振光谱进行了表征。体内抗肿瘤活性测试表明，其中一些化合物能够抑制小鼠S-180癌瘤的生长。所有化合物的体外抗菌活性表明，它们能够促进包括枯草芽孢杆菌在内的一些生物体的生长。