Synthesis and cytotoxic evaluation of some cribrostatin-ecteinascidin analogues.
Analogues of cribrostatin IV ( 1) and the potent antineoplastic agent ecteinascidin 743 ( 2) have been synthesized. The cytotoxic activity of these compounds ( 5, 14, 20) has been determined, and the cyanoamine-cribrostatin analogue ( 14) exhibits a 20-fold improvement with regard to the natural product 1.
Wright
Benjamin J D
BJ
Department of Chemistry, Columbia University, New york, NY 10027, USA.
Chan
Collin
C
Danishefsky
Samuel J
SJ
D018906:Antineoplastic Agents, Alkylating / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004149:Dioxoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000077606:Trabectedin
D018906:Antineoplastic Agents, Alkylating; D004149:Dioxoles; D007546:Isoquinolines; D044005:Tetrahydroisoquinolines; C412688:cribrostatin 4; D000077606:Trabectedin