Brzozowski Zdzisław, Saczewski Franciszek, Sławiński Jarosław
Department of Chemical Technology of Drugs, Medical University of Gdańsk, Al. Gen. J. Hallera 107, 80-416 Gdańsk, Poland.
Eur J Med Chem. 2007 Sep;42(9):1218-25. doi: 10.1016/j.ejmech.2007.01.020. Epub 2007 Jan 27.
Novel 3-amino-2-(4-chloro-2-mercaptobenzenesulfonyl)guanidine derivatives have been synthesized as potential anticancer agents. The in vitro antitumor activity of these compounds has been evaluated in the US National Cancer Institute (NCI), and relationships between structure and antitumor activity are discussed. The prominent compound was 1-allyl-2-[4-chloro-5-(4-chlorophenylcarbamoyl)-2-methylthiobenzenesulfonyl]-3-(5-nitrofurfurylideneamino)guanidine (8) with remarkable activity against 21 human tumor cell lines representing leukemia, lung, colon, melanoma, ovarian, renal, prostate and breast (GI(50)=0.3-3.0microM), and selectivity toward leukemia RPMI-8226 cell line (GI(50)=0.3microM, TGI=1.4microM).
新型3-氨基-2-(4-氯-2-巯基苯磺酰基)胍衍生物已被合成为潜在的抗癌剂。这些化合物的体外抗肿瘤活性已在美国国立癌症研究所（NCI）进行了评估，并讨论了结构与抗肿瘤活性之间的关系。突出的化合物是1-烯丙基-2-[4-氯-5-(4-氯苯基氨基甲酰基)-2-甲基硫代苯磺酰基]-3-(5-硝基糠叉亚氨基)胍(8)，对代表白血病、肺癌、结肠癌、黑色素瘤、卵巢癌、肾癌、前列腺癌和乳腺癌的21种人类肿瘤细胞系具有显著活性（GI(50)=0.3-3.0微摩尔），并且对白血病RPMI-8226细胞系具有选择性（GI(50)=0.3微摩尔，TGI=1.4微摩尔）。
