Design, Synthesis, and Evaluation of Analogues of (+)-14-Normethyldiscodermolide

200425 citationsJournal Article

Authors

Amos B. Smith · Albert Einstein College of Medicine

B. Scott Freeze · Albert Einstein College of Medicine

Matthew J. LaMarche · University of Pennsylvania

Tomoyasu Hirose · Albert Einstein College of Medicine

Ignacio Brouard · University of Pennsylvania

Ming Xian · University of Pennsylvania

Kurt F. Sundermann

Abstract

[Structure: see text] The design, syntheses, and biological evaluation of nine totally synthetic analogues of the microtubule-stabilizing agent (+)-14-normethyldiscodermolide (2) are reported. Simplification at the C(21)-C(24) terminal diene and at the C(1)-C(5) lactone moieties reveals significant structure-activity relationships.

Topics & Keywords

Synthetic Organic Chemistry Methods Cancer Treatment and Pharmacology Asymmetric Synthesis and Catalysis

Publication Details

Published in: Organic Letters

Volume 7, Issue 2, pp. 315-318

DOI: 10.1021/ol0476873

Field-Weighted Citation Impact: 2.68

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Design, Synthesis, and Evaluation of Analogues of (+)-14-Normethyldiscodermolide

Authors

Abstract

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Publication Details