期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 53, 期 42, 页码 11356-11360出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201405650
关键词
antitumor agents; natural products; photoactivation; pretubulysin; tubulysin
资金
- Deutsche Forschungsgemeinschaft [FOR 1406, Ka880/10-1/2]
- Studienstiftung des Deutschen Volkes
The development of a new photolabile protecting group containing an additional allyl functionality allows the synthesis of cyclic photoactivatable natural products. Cyclization occurs between the allyl moiety in the protecting group and a second double bond in the target molecule by means of ring-closing metathesis. Cyclization should increase the metabolic stability towards proteases. On the other hand, the conformational change should cause diminished biological activity. As illustrated for tubulysin derivatives, cyclic and photoactivatable drug candidates can easily be obtained in only two steps from simple building blocks through Ugi reaction and ring-closing metathesis. The photolabile protecting group is introduced by means of the isocyanide component during the Ugi reaction.
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