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高氮杂甾体酯类抗肿瘤活性的进一步研究。

Further studies on the antineoplastic activity of homo-aza-steroidal esters.

作者信息

Pairas G, Catsoulacos P, Papageorgiou A, Boutis L

出版信息

Oncology. 1986;43(6):344-8. doi: 10.1159/000226399.

Abstract

The modified steroidal alkylating agents, 17 beta-hydroxy-3-aza-A-homo-4 alpha-androsten-4- one(p-[bis(2-chloroethyl)amino]phenyl)butyrate(1),3 alpha-hydroxy- 13,17-seco-5 alpha- butyrate(2),3 beta-hydroxy-13,17-seco-5-androsten-17-oic- 13,17-lactam(p-[bis-(2-chloroethyl)amino]phenyl)butyrate(3) and and (p-[bis(2-chloroethyl)amino]phenyl)butyric acid(4) have been tested against L1210, P388, Ehrlich ascites tumors (EAT), Lewis lung (LL) carcinoma and adenocarcinoma CA-755. Of four compounds evaluated in L1210 leukemia, none displayed antileukemic activity. Almost all of the four compounds were more or less active against P388 leukemia. Compound 2 possesses a slight antitumor activity in EAT, while only compound 1 appears to be active in LL carcinoma. The antitumor activity of the three modified steroidal esters on adenocarcinoma CA-755 seems to be interesting.

摘要

已对修饰的甾体烷基化剂17β-羟基-3-氮杂-A-高-4α-雄甾烯-4-酮(对-[双(2-氯乙基)氨基]苯基)丁酸酯(1)、3α-羟基-13,17-开环-5α-雄甾烯-17-羧酸(对-[双(2-氯乙基)氨基]苯基)丁酸酯(2)、3β-羟基-13,17-开环-5-雄甾烯-17-内酰胺(对-[双(2-氯乙基)氨基]苯基)丁酸酯(3)以及对-[双(2-氯乙基)氨基]苯基丁酸(4)针对L1210、P388、艾氏腹水瘤(EAT)、刘易斯肺癌(LL)和腺癌CA - 755进行了测试。在针对L1210白血病评估的四种化合物中,没有一种表现出抗白血病活性。这四种化合物几乎都或多或少对P388白血病有活性。化合物2在EAT中具有轻微的抗肿瘤活性,而只有化合物1在LL癌中似乎有活性。三种修饰的甾体酯对腺癌CA - 755的抗肿瘤活性似乎很有趣。

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