Jongsik Gam

A convenient approach to the synthesis of 6-substituted 1,5-dialkyluracils and -2-thiouracils

Abstract A general and convenient approach to the synthesis of 6-substituted 1,5-dialkyluracils and -2-thiouracils via 1,5-dialkyl-6-(methylsulfonyl)uracils 1 and 1,5-dialkyl-6-(methylsulfinyl)-2-thiouracils 2 , respectively, has been described. The compounds 1 and 2 were synthesized from ethyl 2-alkyl-3,3-di(methylthio)acrylates 3 in five steps in good yields.

Synthesis and antitumor activity of (2R,3R)-2,3-dihydroxy- and -2,3-dialkoxy-1,4-diaminobutane platinum(II) complexes

Abstract The synthesis and antitumor activity of (2R,3R)-2,3-dihydroxy- and -2,3-dialkoxy-1,4-diaminobutane platinum(II) complexes 10–15 are described. cis-Dichloro[(2R,3R)-2,3-dimethoxy-1,4-diaminobutane]platinum(II) (bd11) and cis-(cyclobutane01,1-dicarboxylato)[(2R,3R)-2,3-dihydroxy-1,4-diaminobutane]platinum(II) (bd13) showed the potent antitumor activity against L1210 leukemia in mice with % T/C values of around 200.

Synthesis and in vitro cytotoxicity of cis-(glycolato-O,O′)-[2-substituted-(4R,5R)-4,5-bis(aminomethyl)-1,3-dioxolane]platinum (II)

Abstract The synthesis and in vitro cytotoxicity of cis-(glycolato-O,O′)[2-substituted-(4R,5R)-4,5-bis(aminomethyl)-1,3-dioxolane]platinum(II) are described. Among them, cis-(glycolato-O,O′)[(4R,5R)-4,5-bis(aminomethyl)-2,2-diethyl-1,3-dioxolane]platinum(II) (26) was found to be almost equally cytotoxic to cisplatin against two human non-small cell lung cancer cell lines, PC-9 and PC-14, and two human stomach cancer cell lines, MKN-45 and KATO III.

Synthesis and in vitro cytotoxicity of 1,3-dioxolane-2-(2-ethanamine)-2-methanamine platinum(II) complexes

Abstract The synthesis and in vitro cytotoxicity of novel 1,3-dioxolane-2-(2-ethanamine)-2-methanamine platinum(II) complexes having a seven-membered ring structure are described. It has been demonstrated that cisplatin-resistant murine L1210 leukemia cells have lower cross-resistance to this class of compounds than to cisplatin and carboplatin, and the human stomach cancer cell lines, SNU-1, SNU-5, and SNU-16, are highly sensitive to the members of this class.