942133-13-3Relevant academic research and scientific papers
CERTAIN PLADIENOLIDE COMPOUNDS AND METHODS OF USE
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Page/Page column 168; 169-170, (2019/11/04)
The present disclosure provides novel pladienolide compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancers, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful. Also provided herein are methods of treating cancers by administering at least one compound disclosed herein and at least one additional therapy.
Synthesis, molecular editing, and biological assessment of the potent cytotoxin leiodermatolide
Mailhol, Damien,Willwacher, Jens,Kausch-Busies, Nina,Rubitski, Elizabeth E.,Sobol, Zhanna,Schuler, Maik,Lam, My-Hanh,Musto, Sylvia,Loganzo, Frank,Maderna, Andreas,Fürstner, Alois
supporting information, p. 15719 - 15729 (2014/12/11)
It was by way of total synthesis that the issues concerning the stereostructure of leiodermatolide (1) have recently been solved; with the target now being unambiguously defined, the mission of synthesis changes as to secure a meaningful supply of this ex
Divergent total synthesis of the antimitotic agent leiodermatolide
Willwacher, Jens,Kausch-Busies, Nina,Fürstner, Alois
supporting information, p. 12041 - 12046 (2013/01/16)
Subtle but distinctive: The stereostructure of the biologically highly promising antimitotic agent leiodermatolide was uncertain. A short, efficient, and flexible total synthesis based on ring-closing alkyne metathesis as the key step has now solved the p
Synthesis of a pladienolide B analogue with the fully functionalized core structure
Mueller, Sarah,Mayer, Timo,Sasse, Florenz,Maier, Martin E.
scheme or table, p. 3940 - 3943 (2011/09/16)
Starting from (R)-(-)-linalool (6), terminus differentiation and chain extension via aldol type reactions led to ketophosphonate 16 (C1-C8 building block). In a Horner-Wadsworth-Emmons reaction, 16 reacted with aldehyde 22, which contained the vicinal ant
Modular total synthesis of archazolid A and B
Menche, Dirk,Hassfeld, Jorma,Li, Jun,Mayer, Kerstin,Rudolph, Sven
supporting information; experimental part, p. 7220 - 7229 (2010/02/17)
(Chemical Equation Presented) A modular total synthesis of the potent V-ATPase inhibitors archazolid A and B is reported. The convergent preparation was accomplished by late-stage diversification of joint intermediates. Key synthetic steps involve asymmetric boron-mediated aldol reactions, two consecutive Still-Gennari olefinations to set the characteristic (Z,Z)-diene system, a Brown crotyboration, and a diastereo-selective aldol condensation of highly elaborate intermediates. For macrocyclization, both an HWE reaction and a Heck coupling were successfully employed to close the 24-membered macrolactone. During the synthetic campaign, a generally useful protocol for an E-selective Heck reaction of nonactivated alkenes and a method for the direct nucleophilic displacement of the Abiko-Masamune auxiliary with sterically hindered nucleophiles were developed. The expedient and flexible strategy will enable further SAR studies of the archazolids and more detailed evaluations of target-inhibitor interactions. 2009 American Chemical Society.
Total synthesis of archazolid A
Menche, Dirk,Hassfeld, Jorma,Li, Jun,Rudolph, Sven
, p. 6100 - 6101 (2008/02/08)
The archazolids are complex polyketides isolated from the myxobacterium Archangium gephyra and are potent inhibitors of vacuolar type ATPases. Herein, we report the first total synthesis of archazolid A, which establishes unequivocally the relative and ab
