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PRACTICAL INDUSTRY-ORIENTED SYNTHESIS OF ECTEINASCIDIN ET743 AND ET770 |
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Principal investigator : Jieping ZHU
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CONTEXT
The
ecteinascidins (Et), 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.
Due to the
extremely low natural availability (
1 gram from 1 ton of tunicate), the drug supply
is becoming a key issue. To obtain enough amount of drug for cancer treatment,
a simpler and more efficient process was thus needed. Total synthesis or
hemisynthesis from simpler natural product became an important alternative and,
in this particular case probably the only available alternative. Among the
discovered so far methods, they are difficult to be applied into a large-scale
production leading therefore for a high demand in a another efficient method
for an industrial application.
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