| 摘要 |
<p>PURPOSE:To obtain the new compound, having high selectivity for a cancerous cell, effective for solid tumors and useful as a low toxic antitumor agent. CONSTITUTION:The objective compound of formulas I and II {R is 1-4C alkyl; R<1> is alpha-amino acid residue or formula III [X<1> to X<3> are OH, OR<3> (R<3> is 1-6C alkyl or aryl), etc.; Z<1> is O, S or NR<4> (R<4> 1-6C alkyl or aryl), OCOR<3>, CHO, NO2, etc.], etc.; R<2> is H, OH-protecting group or substituent group; Y is halogen, arylsulfonyloxy, lower alkylsulfonyloxy, azide, etc.}, e.g. methyl 1-chloromethyl-5- hydroxy-7-trifluoromethyl-3-(5,6,7-trimethoxyIH-indol-2-ylcarbonyl)-l, 2,3,6- tetrahydropyrrolo[3,2-e]indole-8-carboxylate. This compound of formula I is obtained by adding an acid to a compound of formula IV, etc.</p> |
