Biopolym. Cell. 2003; 19(6):548-552.
Bioorganic Chemistry
Antitumor activity among derivatives of the 3-chloro-4-(3-hydroxyanilino) -2,5-dihydropyrrole-2,5-dione
- Institute of Molecular Biology and Genetics, NAS of Ukraine
150, Akademika Zabolotnoho Str., Kyiv, Ukraine, 03680
Abstract
Fourteen derivatives of the 3-chloro-4-(3-hydroxyanilino)-2,5-di-hydropyrrole-2,5-dione with various substituents at 1 and 3 positions of maleimide cycle have been synthesized and tested for antitumor activity in vitro. Ten compounds have been selected after pre-screening and tested on 52 human tumor cell lines. It has been revealed that 1 -(2,3-dichlorophenyl)-3-chloro-4-(3-hydroxyanili-no)-2,5-dihydro-1H-2,5-pyrroledione and l-benzyl-3-(3-hydroxy-anilino)-4-phenylsulfanyl-2,5-dihydro-1H-2,5-pyrroledione suppress growth of some cancer cell lines with GI50 < 0.5 ·10–7 M and 10–8 M.
Full text: (PDF, in Ukrainian)
References
[1]
Fischer PM, Lane DP. Inhibitors of cyclin-dependent kinases as anti-cancer therapeutics. Curr Med Chem. 2000;7(12):1213-45.
[2]
Senderowicz AM. The cell cycle as a target for cancer therapy: basic and clinical findings with the small molecule inhibitors flavopiridol and UCN-01. Oncologist. 2002;7 Suppl 3:12-9.
[3]
Bailly C, Qu X, Chaires JB, Colson P, Houssier C, Ohkubo M, Nishimura S, Yoshinari T. Substitution at the F-ring N-imide of the indolocarbazole antitumor drug NB-506 increases the cytotoxicity, DNA binding, and topoisomerase I inhibition activities. J Med Chem. 1999;42(15):2927-35.
[4]
Andricopulo AD, Yunes RA, Nunes RJ, Savi AOS, Correa R, Cruz AB, Filho VC. Synthesis and antibacterial activity of cyclic imides: 3,4-dichloromaleimides and 4-substituted 3-chloromaleimides. Quim Nova. 1998; 21(5):573-7.
[5]
Tarnavskiy SS, Dubinina GG, Golovach SM, Yarmoluk SM. Search for antitumor activity among derivatives of the 2,5-dihydropyrrole-2,5-dione. Biopolym Cell. 2003; 19(3):287-91.