Catsoulacos P, Catsoulacos D
School of Health and Sciences, Department of Pharmacy, University of Patras, Greece.
Anticancer Res. 1994 Nov-Dec;14(6B):2525-8.
The homo-aza-steroidal esters of conjugated carboxylic derivatives of nitrogen mustards are reviewed. Particularly we discuss the antitumor activity of cinnamic acid and benzoic acid mustard isomers, esters of homo-aza-steroids in which the mustard acid is linked to the C-3 or C17 position, while the lactam nucleus is in the D or A ring of the steroid respectively. The current literature indicates that the potential is due to the synergistic activity of both the steroidal lactam and the mustard of the acids. Steroidal lactams, namely 3 beta-hydroxy-13 alpha-amino-13,17-seco-5 alpha-androstan-17-oic-13,17-lactam, the isomer 3 alpha-hydroxy-13 alpha-amino-13,17-seco-5 alpha-androstan-17-oic- 13,17-lactam, 3 beta-hydroxy-13 alpha-amino 13,17-seco-5-androsten-17-oic-13,17-lactam and the 17 beta-hydroxy-3-aza-A-homo- 4 alpha-androsten-4-one, have been used as biological platforms of the cinnamic acid, of the benzoic acid mustard isomers and the 4-methyl-benzoic acid mustard. The twelve esters of cinnamic acid mustard isomers were tested against P388, L1210 leukemias Ehrlich ascites tumor (EAT) and melanoma B16 in vivo. The effect of homo-aza-steroidal esters of N,N-bis(2-chloroethyl) amino cinnamic acid isomers on the incorporation of the radioactive precursors into DNA, RNA and proteins of L1210, P388 leukemias, Ehrlich ascites tumor (EAT) and Baby Hamster Kidney (BHK) cells, was investigated. The effect of the homo-aza-steroidal esters of N,N-bis(2-chloroethyl) aminobenzoic acid isomers on the incorporation of radioactive precursors into DNA, RNA and proteins was studied in L1210, P388 leukemias, Ehrlich ascites tumor and Baby hamster kidney cells.
对氮芥共轭羧酸衍生物的同氮杂甾体酯进行了综述。特别地，我们讨论了肉桂酸和苯甲酸氮芥异构体、同氮杂甾体酯的抗肿瘤活性，其中氮芥酸连接在甾体的C-3或C17位，而内酰胺核分别位于甾体的D环或A环。当前文献表明，这种潜力归因于甾体内酰胺和酸的氮芥的协同活性。甾体内酰胺，即3β-羟基-13α-氨基-13,17-开环-5α-雄甾烷-17-酸-13,17-内酰胺、异构体3α-羟基-13α-氨基-13,17-开环-5α-雄甾烷-17-酸-13,17-内酰胺、3β-羟基-13α-氨基-13,17-开环-5-雄烯-17-酸-13,17-内酰胺以及17β-羟基-3-氮杂-A-高-4α-雄烯-4-酮，已被用作肉桂酸、苯甲酸氮芥异构体和4-甲基苯甲酸氮芥的生物平台。对肉桂酸氮芥异构体的十二种酯进行了体内抗P388、L1210白血病、艾氏腹水瘤（EAT）和黑色素瘤B16的测试。研究了N,N-双(2-氯乙基)氨基肉桂酸异构体的同氮杂甾体酯对放射性前体掺入L1210、P388白血病、艾氏腹水瘤（EAT）和幼仓鼠肾（BHK）细胞的DNA、RNA和蛋白质中的影响。研究了N,N-双(2-氯乙基)氨基苯甲酸异构体的同氮杂甾体酯对放射性前体掺入L1210、P388白血病、艾氏腹水瘤和幼仓鼠肾细胞的DNA、RNA和蛋白质中的影响。
