摘要 |
Compounds of the saframycin-ecteinascidin series with cytotoxic properties having the following general formula, their uses and synthesis, are disclosed: wherein R<SUB>1 </SUB>and R<SUB>4 </SUB>is H, a C<SUB>1 </SUB>to C<SUB>4 </SUB>alkyl group, or an acyl group; wherein R<SUB>2 </SUB>is an ether, ester, amide, or a phthalimide group; wherein R<SUB>3 </SUB>is -O, OH, an ether group, an acyl group such as OC(O)Me, OC(O)Bn and OC(O)Et, or a sulfide group; wherein R<SUB>5 </SUB>is H, halogen, OH, an ether group, an acyl group, or an amide group; wherein R<SUB>6 </SUB>is -O, OH, OCH<SUB>3</SUB>, CN, or an acyloxy group; wherein R<SUB>7</SUB>, is -O, OH, halogen, an ether group, or an acyl group; wherein R<SUB>8 </SUB>and R<SUB>9 </SUB>are independently H, CH<SUB>3</SUB>, OCH<SUB>3</SUB>, OC<SUB>2</SUB>H<SUB>5</SUB>, CF<SUB>3</SUB>, halogen such as Br and F, or R<SUB>8 </SUB>and R<SUB>9 </SUB>are joined together as a methylenedioxy group, or other five or six membered ring; wherein R<SUB>10 </SUB>and R<SUB>11 </SUB>are independently CH<SUB>3</SUB>, OCH<SUB>3</SUB>, OC<SUB>2</SUB>H<SUB>5</SUB>, SCH<SUB>3</SUB>, or SC<SUB>2</SUB>H<SUB>5</SUB>; wherein R<SUB>12 </SUB>is H, a C<SUB>1 </SUB>to C<SUB>4 </SUB>alkyl group, or an acyl group; and wherein the chiral center marked * has the R or the S configuration. |