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1-[2-(氯乙基)-3-(2-取代-10H-吩噻嗪-10-基)烷基]-1-脲作为强效抗癌剂的合成及其抗肿瘤活性

Synthesis and antitumor activity of 1-[2-(chloroethyl)-3-(2-substituted-10H-phenothiazin-10-yl)alkyl- 1-urea s as potent anticancer agents.

作者信息

Motohashi N, Kawase M, Kurihara T, Hevér A, Nagy S, Ocsocvszki I, Tanaka M, Molnár J

机构信息

Department of Medicinal Chemistry, Meiji College of Pharmacy, Tokyo, Japan.

出版信息

Anticancer Res. 1996 Sep-Oct;16(5A):2525-32.

PMID:8917346
Abstract

10-[N-(Phthalimido)alkyl]-2-substituted-10H-phenothiazines and 1-(2-chloroethyl)-3-(2-substituted-10H-phenothiazin-10-yl)alkyl-1- ureas were synthesized and found to have antiproliferative effects on human HEp-2 and L5178Y cell cultures. The multi-drug resistant subline of mouse lymphoma was sensitive to the reversal effects of some 10-[N-(phthalimido)alkyl]-2-substituted-10H-phenothiazines, while 1-(2-chloro-ethyl)-3-(2-substituted-10H-phenothiazin-10-yl)alkyl-1 -ureas were less effective but had a similar degree of antiproliferative effect on both cell lines.

摘要

合成了10 - [N -(邻苯二甲酰亚胺基)烷基] - 2 -取代 - 10H -吩噻嗪和1 -(2 -氯乙基)- 3 -(2 -取代 - 10H -吩噻嗪 - 10 -基)烷基 - 1 -脲,并发现它们对人HEp - 2和L5178Y细胞培养物具有抗增殖作用。小鼠淋巴瘤的多药耐药亚系对某些10 - [N -(邻苯二甲酰亚胺基)烷基] - 2 -取代 - 10H -吩噻嗪的逆转作用敏感,而1 -(2 -氯乙基)- 3 -(2 -取代 - 10H -吩噻嗪 - 10 -基)烷基 - 1 -脲效果较差,但对两种细胞系具有相似程度的抗增殖作用。

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