Choi B G, Kim O Y, Chung B H, Cho W J, Cheon S H, Choi S U, Lee C O
College of Pharmacy, Chonnam National University, Kwangju, Korea.
Arch Pharm Res. 1998 Apr;21(2):157-63. doi: 10.1007/BF02974021.
Several aniline mustard analogues were obtained by introducing N,N-bis(2-chloroethyl)amino moiety to phenyl ring of A10 analogues in order to increase reactivity of A10 analogs and selectivity into DNA. The in vitro antitumor activity of synthesized compounds was evaluated using five different solid tumor cell lines by SRB method. Aniline mustard analogues exhibited more potent antitumor activity than A10 analogs. Especially, m-aniline mustard of benzoyl analogue displayed remarkable antitumor activity.
通过将N,N-双(2-氯乙基)氨基部分引入A10类似物的苯环来获得几种苯胺氮芥类似物,以提高A10类似物的反应活性和对DNA的选择性。使用SRB方法通过五种不同的实体瘤细胞系评估合成化合物的体外抗肿瘤活性。苯胺氮芥类似物表现出比A10类似物更强的抗肿瘤活性。特别是,苯甲酰类似物的间苯胺氮芥显示出显著的抗肿瘤活性。