两种新型硫吖啶衍生物的合成及其体外生物活性比较。

Synthesis of two novel thioacridinic derivatives and comparison of their in vitro biological activities.

作者信息

Mannani R, Galy J P, Sharples D, Barbe J, Barra Y

机构信息

Groupe d'Etudes et Recherches en Chimie Thérapeutique Organique et Physique, Faculté de Pharmacie, Marseille, France.

出版信息

Chem Biol Interact. 1990;74(3):291-303. doi: 10.1016/0009-2797(90)90046-p.

DOI:10.1016/0009-2797(90)90046-p

PMID:1693312

Abstract

Two novel compounds, 3-amino-9-(diethylaminoethylthio) acridine and 9-diethylaminoethylthioacridine, were synthesized and characterized. They were shown to be cytotoxic against K562 and Raji cell lines. A concentration of 10(-5) M killed around 40% of the cells after 3 h time of incubation. Intercalation into DNA was more efficient when a protonated nitrogen was present in a side chain of the ring system. At the cytotoxic concentrations (10(-5) M, 10(-6) M), inhibition of nucleic acid synthesis in K562, Raji cell lines and human leukocytes has been shown. The results presented suggest that the cytotoxicity and the inhibition of nucleic acid synthesis of the two compounds studied are inversely related to their intercalating capability into the DNA helix.

摘要

合成并表征了两种新型化合物，3-氨基-9-（二乙氨基乙硫基）吖啶和9-二乙氨基乙硫基吖啶。结果表明它们对K562和Raji细胞系具有细胞毒性。在孵育3小时后，10⁻⁵ M的浓度可杀死约40%的细胞。当质子化氮存在于环系统的侧链中时，其插入DNA的效率更高。在细胞毒性浓度（10⁻⁵ M，10⁻⁶ M）下，已表明对K562、Raji细胞系和人白细胞的核酸合成有抑制作用。所呈现的结果表明，所研究的两种化合物的细胞毒性和核酸合成抑制作用与其插入DNA螺旋的能力呈负相关。