| 摘要 |
PROBLEM TO BE SOLVED: To provide new compounds having most suitable characteristics of cytotoxicity and selectivity to tumor, decreased in systemic toxicity and improved in pharmacokinetic properties. SOLUTION: There are provided derivatives of ecteinascidin 736 of general formula I; [wherein, R<SB>1</SB>, R<SB>2</SB>, R<SB>3</SB>, R<SB>4</SB>and R<SB>5</SB>are each independently selected from the group consisting of H, OH, OR', SH, SR', SOR', SO<SB>2</SB>R', C(=O)R', C(=O)OR', NO<SB>2</SB>, NH<SB>2</SB>, NHR', N(R')<SB>2</SB>, NHC(O)R', CN, halogen, =O and the like; X is independently selected from OR', CN, (=O), or H; each R' is independently selected from the group consisting of H, OH, NO<SB>2</SB>, NH<SB>2</SB>, SH, CN, halogen, =O, C(=O)H, C(=O)CH<SB>3</SB>, CO<SB>2</SB>H and the like; m is 0, 1 or 2; and n is 0, 1, 2, 3 or 4]. COPYRIGHT: (C)2011,JPO&INPIT
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