Total Syntheses of Pladienolide-Derived Spliceosome Modulators

Pladienolides, an emerging class of naturally occurring spliceosome modulators, exhibit interesting structural features, such as highly substituted 12-membered macrocycles and epoxide-containing diene side chains. The potential of pladienolides as anti-cancer agents is confirmed by H3B-8800, a synth...

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Bibliographic Details
Published in:	Molecules (Basel, Switzerland) Switzerland), 2021-09, Vol.26 (19), p.5938
Main Authors:	Sim, Jaehoon, Jang, Eunbin, Kim, Hyun Jin, Jeon, Hongjun
Format:	Article
Language:	eng
Subjects:	Animals Antineoplastic Agents, Phytogenic - pharmacology Biological Products - pharmacology Cancer Clinical trials Epoxy Compounds - pharmacology Humans Leukemia macrocycles Macrolides - pharmacology Modulators Natural products Neoplasms - drug therapy Neoplasms - pathology pladienolide class Reagents Review Severe acute respiratory syndrome coronavirus 2 spliceosome Spliceosomes - drug effects total synthesis Tumors
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Summary:	Pladienolides, an emerging class of naturally occurring spliceosome modulators, exhibit interesting structural features, such as highly substituted 12-membered macrocycles and epoxide-containing diene side chains. The potential of pladienolides as anti-cancer agents is confirmed by H3B-8800, a synthetic analog of this natural product class, which is currently under Phase I clinical trials. Since its isolation in 2004 and the first total synthesis in 2007, a dozen total syntheses and synthetic approaches toward the pladienolide class have been reported to date. This review focuses on the eight completed total syntheses of naturally occurring pladienolides or their synthetic analogs, in addition to a synthetic approach to the main framework of the natural product.
ISSN:	1420-3049 1420-3049