Solution-phase synthesis and biological evaluation of triostin A and its analogues

2016 ◽  
Vol 14 (6) ◽  
pp. 2090-2111 ◽  
Author(s):  
Kozo Hattori ◽  
Kota Koike ◽  
Kensuke Okuda ◽  
Tasuku Hirayama ◽  
Masahiro Ebihara ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Biological Evaluation ◽  
Solution Phase ◽  
Phase Synthesis ◽  
Total Syntheses ◽  
Solution Phase Synthesis ◽  
Triostin A ◽  
Inhibitory Activities ◽  
High Yields ◽  
Synthesis And Biological Evaluation

We have accomplished preparative solution-phase total syntheses of triostin A (17.5% in 13 steps) and its analogues with high yields to demonstrate their significant inhibitory activities on HIF-1 activation and cell proliferation.

Solid and Solution Phase Synthesis and Biological Evaluation of Combinatorial Sarcodictyin Libraries

1998 ◽  
Vol 120 (42) ◽  
pp. 10814-10826 ◽  
Author(s):  
K. C. Nicolaou ◽  
N. Winssinger ◽  
D. Vourloumis ◽  
T. Ohshima ◽  
S. Kim ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Solution Phase ◽  
Phase Synthesis ◽  
Solution Phase Synthesis ◽  
Synthesis And Biological Evaluation

scholarly journals Solution phase synthesis of short oligoribonucleotides on a precipitative tetrapodal support

2014 ◽  
Vol 10 ◽  
pp. 2279-2285 ◽  
Author(s):  
Alejandro Gimenez Molina ◽  
Amit M Jabgunde ◽  
Pasi Virta ◽  
Harri Lönnberg
Keyword(s):  
Building Block ◽  
Rna Synthesis ◽  
Building Blocks ◽  
Solution Phase ◽  
Dipolar Cycloaddition ◽  
Proof Of Concept ◽  
Phase Synthesis ◽  
Solution Phase Synthesis ◽  
High Yields

An effective method for the synthesis of short oligoribonucleotides in solution has been elaborated. Novel 2'-O-(2-cyanoethyl)-5'-O-(1-methoxy-1-methylethyl) protected ribonucleoside 3'-phosphoramidites have been prepared and their usefulness as building blocks in RNA synthesis on a soluble support has been demonstrated. As a proof of concept, a pentameric oligoribonucleotide, 3'-UUGCA-5', has been prepared on a precipitative tetrapodal tetrakis(4-azidomethylphenyl)pentaerythritol support. The 3'-terminal nucleoside was coupled to the support as a 3'-O-(4-pentynoyl) derivative by Cu(I) promoted 1,3-dipolar cycloaddition. Couplings were carried out with 1.5 equiv of the building block. In each coupling cycle, the small molecular reagents and byproducts were removed by two quantitative precipitations from MeOH, one after oxidation and the second after the 5'-deprotection. After completion of the chain assembly, treatment with triethylamine, ammonia and TBAF released the pentamer in high yields.

Synthesis of Casein-Related Peptides and Phosphopeptides. I. Solution-Phase Synthesis and 13C N.M.R.-Spectroscopy of the N-α-Acetyl Octapeptide N-Methylamide Corresponding to Region 14-21 of Bovine β-Casein A2

1987 ◽  
Vol 40 (2) ◽  
pp. 257 ◽  
Author(s):  
JW Perich ◽  
PF Alewood ◽  
RB Johns
Keyword(s):  
Solution Phase ◽  
Phase Method ◽  
Peptide Fragments ◽  
Mixed Anhydride ◽  
Phase Synthesis ◽  
Solution Phase Synthesis ◽  
Coupling Procedure ◽  
Fragment Condensation ◽  
High Yields ◽  
Solution Phase Method

The octapeptide, Ac-Glu-Ser-Leu-Ser-Ser-Ser-Glu-Glu-NHMe (I), was synthesized by the solution-phase method by using the mixed anhydride coupling procedure for the fragment condensation of the Nα-acetyl tripeptide, Ac-Glu(OBut)-Ser(But)-Leu-OH, with the pentapeptide N-methylamide hydrochloride, Cl.H2-Ser(But)-Ser(But)-Ser(But)-Glu(OBzl)-Glu(OBzl)-NHMe, followed by palladium-catalysed hydrogenolysis of Ac-Glu(OBut)-Ser(But)-Leu-Ser(But)-Ser(But)- Ser(But) Glu(OBzl)Glu(OBzl NHMe in trifluoroacetic acid. The synthesis of the two peptide fragments was accomplished in high yields and purity by using the repetitive excess mixed anhydride procedure and the isobutoxycarbonyl mixed anhydride of acetic acid for the rapid and high yielding N-acetylation of the tripeptide fragment. 13C n.m.r. spectroscopy was routinely used to monitor the efficiency of the coupling steps and to confirm the structure of octapeptide (1), signal assignments being possible for both the protected tri- and penta-peptides.

A Low Temperature, Solution Phase Synthesis of III-V Semiconductor Nanocrystals

1994 ◽  
Vol 351 ◽  
Author(s):  
Shreyas S. Kher ◽  
Richard L. Wells
Keyword(s):  
Semiconductor Nanocrystals ◽  
Solution Phase ◽  
High Yield ◽  
Group V ◽  
Phase Synthesis ◽  
Group Iii ◽  
Wide Range ◽  
Solution Phase Synthesis ◽  
Temperature Solution ◽  
High Yields

ABSTRACTNanocrystalline materials have been intensely investigated in the recent past due to the novel properties associated with size-quantized particles. We have developed a new method for high yield, solution phase synthesis of nanocrystalline III-V semiconductors which eliminates the use of substituted or unsubstituted Group V hydrides and Group III alkyls. Our approach consists of in situ syntheses of (Na/K)3E (E = P, As, Sb) in aromatic solvents and subsequent reactions of these pnictides with Group III halide solutions in coordinating solvents. The nanocrystalline III-V semiconductors GaP, GaAs, GaSb, InP, InAs and InSb are readily prepared in a wide range of particle sizes (4–36 nm) and in high yields. The resultant Ill-V materials have been characterized by XRD, EDXA, TEM and elemental analyses.

Solution phase synthesis of oligonucleotides by the phosphoramidite method using solid supported reagents

2005 ◽  
Author(s):  
François Morvan ◽  
Aude-Emmanuelle Navarro ◽  
Cécile Dueymes ◽  
Ilaria Adamo ◽  
Andreas Schoenberger ◽  
...  
Keyword(s):  
Solution Phase ◽  
Phase Synthesis ◽  
Solution Phase Synthesis
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