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PREPARATION PROCESS OF ECTEINASCIDIN AND ANALOGUES |
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Principal Investigator: J. ZHU
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TECHNICAL DESCRIPTION
The present invention concerns ecteinascidins intermediate, their preparation and their use, in particular Ecteinascidin 597 and Ecteinascidin-583.
The ecteinascidins, a family of tetrahydroisoquinoline alkaloids isolated from the Caribbean tunicate Ecteinascidia turbinate possess potent cytotoxic activity against a variety of tumor cell lines in vitro and against several rodent tumors and human tumor xenografts in vivo.
One of its members, ecteinascidin 743 is currently in phase 11/111 clinical trials in Europe and the United States for ovarian, endometrium, breast cancer and several types of sarcoma. It showed particularly high activity in cases of advanced sarcoma that had relapsed or were resistant to conventional therapy. The antiproliferative activity of ecteinascidin 743 is greater than that of taxol, camptothecin, adriamycin, mitomycin C, cisplatin, bleomycin and etoposide by 1-3 orders of magnitude.
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