1067880-31-2

Upstream product

• 1067880-35-6 tert-butyl(2-methoxy-5-(1-(3,4,5-trimethoxyphenyl)vinyl)phenoxy)dimethylsilane 
• 1192108-60-3 1-[1-(3-tert-butyldiphenylsiloxy-4-methoxyphenyl)vinyl]-3,4,5-trimethoxybenzene 
• 1136-86-3 methyl (3,4,5-trimethoxyphenyl) ketone 
• 186837-48-9 3-(tert-butyldimethylsilyloxy)-4-methyloxyphenyl iodide 
• 1170045-84-7 4-methyl-N′-(1-(3,4,5-trimethoxyphenyl)ethylidene)benzenesulfonohydrazide 
• 160257-85-2 5-iodo-2-methoxyphenol 
• 90-05-1 2-methoxy-phenol 
• 86-81-7 3,4,5-trimethoxy-benzaldehyde 
• 613-70-7 2-methoxyphenyl acetate 
• 183593-98-8 5-iodo-2-methoxyphenyl acetate 
• 53560-33-1 3,4,5-trimethoxyphenylacetylene 
• 77295-62-6 1,1-Dibromo-2-(3',4',5'-trimethoxyphenyl)ethene 
• 874812-62-1 2-methoxy-5-(3,4,5-trimethoxybenzoyl)phenyl 2-chloroacetate 
• 75-24-1 trimethylaluminum 

Downstream Products

• 1067880-43-6 C₃₂H₃₃O₈P 
• 1070196-11-0 C₄₀H₄₃NO₉ 
• 1070196-57-4 C₁₈H₂₁O₈P 
• 1339825-60-3 C₁₈H₁₈O₆ 
• 1070196-40-5 C₂₂H₂₇NO₆*ClH 
• 1070196-33-6 C₂₄H₂₃NO₆*ClH 
• 1070196-43-8 C₁₈H₁₉O₈S^(1-)*Na⁽¹⁺⁾ 
• 1070196-37-0 C₂₂H₂₃O₈^(1-)*Na⁽¹⁺⁾ 
• 1070196-30-3 isoCA-4S 
• 1070196-53-0 C₃₅H₃₂O₈ 
• 1070196-24-5 C₂₂H₂₇NO₆ 

Relevant academic research and scientific papers

Design and synthesis of silicon-containing tubulin polymerization inhibitors: Replacement of the ethylene moiety of combretastatin A-4 with a silicon linker

Silicon-containing combretastatin analogs were designed, synthesized and evaluated for stability and biological activities. Among them, compound 31 exhibited strong tubulin polymerization-inhibitory activity and very potent tumor cell growth-inhibitory ac

Origins of Internal Regioselectivity in Copper-Catalyzed Borylation of Terminal Alkynes

Installation of a boron functionality into a more substituted carbon of terminal alkynes has been a challenging issue in chemical synthesis, since inherently Lewis acidic boron moieties, in principle, favor their attachment to a terminal carbon. Herein, we report on the highly internal-selective borylation of terminal alkynes under copper catalysis, wherein diminishment of boron-Lewis acidity and ligand-derived steric bulk around a copper center are the key to the success. In particular, the use of an anthranilamide-substituted boron moiety [B(aam)] is of high synthetic significance, because its properly diminished Lewis acidity enabled the internal regioselectivity and the Suzuki-Miyaura cross-coupling activity to be compatibly achieved. This method provided a direct and universal approach to variously substituted branched alkenylboron compounds, regardless of electronic and steric properties of a substituent on terminal alkynes.

Toward a Greener Barluenga-Valdés Cross-Coupling: Microwave-Promoted C-C Bond Formation with a Pd/PEG/H2O Recyclable Catalytic System

A green Barluenga-Valdés cross-coupling reaction for the synthesis of 1,1-diarylethylenes using palladium catalysis has been developed. The new catalytic system based on Pd/Xphos-SO3Na or Pd/MeDavephos-CF3SO3 in PEG/H2O under microwave irradiation was found to be the best conditions for this transformation. The recyclability of the palladium catalyst system was also studied, and it was found to be active over nine runs without significant loss in its activity.

"MULTI-TARGET" COMPOUNDS WITH INHIBITORY ACTIVITY TOWARDS HISTONE DEACETYLASES AND TUBULIN POLYMERISATION, FOR USE IN THE TREATMENT OF CANCER

The present invention relates to the design of novel molecules, referred to as “multi-target” molecules, having a double pharmacophore and acting both as inhibitors of histone deacetylases (HDACs) and as inhibitors of tubulin polymerisation. The invention also describes the method for synthesising the “multi-target” molecules and their use in the treatment of cancer, a pharmaceutical composition comprising at least one “multi-target” molecule, and the use of such compositions in the treatment of cancer.

Design and Synthesis of Tubulin and Histone Deacetylase Inhibitor Based on iso-Combretastatin A-4

Designing multitarget drugs have raised considerable interest due to their advantages in the treatment of complex diseases such as cancer. Their design constitutes a challenge in antitumor drug discovery. The present study reports a dual inhibition of tub

Constructing novel dihydrofuran and dihydroisoxazole analogues of isocombretastatin-4 as tubulin polymerization inhibitors through [3+2] reactions

[3+2] reactions play a key role in constructing various pharmaceutical moleculars. In this study, using Mn(OAc)3 mediated and 1,3-dipolar [3+2] cyclization reactions, 38 novel dihydrofuran and dihydroisoxazole analogues of isoCA-4 were synthesized as inhibitors of tubulin polymerization. Among them, compound 6g was found to be the most potent cytotoxic agents against PC-3 cells with IC50 value of 0.47 μM, and compound 5p exhibted highest activity on HeLa cells with IC50 vaule of 2.32 μM. Tubulin polymerization assay revealed that 6g was a dose-dependent and effective inhibitor of tubulin assembly. Immunohistochemistry studies and cell cycle distribution analysis indicated that 6g severely disrupted microtubule network and significantly arrested most cells in the G2/M phase of the cell cycle in PC-3 cells. In addition, molecular docking studies showed that two chiral isomers of 6g can bind efficiently and similarly at colchicine binding site of tubulin.

α,α-Diarylethylene Glycols as Valuable Precursor for Synthesis of 1,1-Diarylethenes and α,α-Diaryl Acetaldehydes

Towards assembling of diarylmethine unit present in biologically important molecules, we have developed a new Weinreb Amide (WA) based building block derived from glycolic acid. The WA functionality present in this building block permits the sequential addition of various arylmagnesium bromide reagents in a controlled manner that enables assembly of a diarylmethine unit. The developed synthetic route provides easy access to important diarylethenes and α,α-diarylethylene glycols. The synthesized α,α-diarylethylene glycols provide access to synthetically important symmetrical and unsymmetrical α,α-diaryl acetaldehydes as valuable intermediates.

Efficient synthesis of polysubstituted olefins using stable palladium nanocatalyst: Applications in synthesis of tamoxifen and isocombretastatin A4

A phosphine-free stable palladium nanocatalyst was used for an efficient synthesis of polysubstituted olefins from N-tosylhydrazones and aryl iodides. This methodology was successfully utilized in the synthesis of biologically important tamoxifen and isocombretastatin A4. The nanocatalyst was easily recovered and reused without any apparent loss in size and catalytic activity.

Negishi cross-coupling reaction as a route to isocombretastatins

A series of isocombretastatins A has been synthesized by a new method based on the Negishi cross-coupling reaction in 19-84% yields. Five of the synthesized compounds exhibit high cytotoxic activity in nanomolar concentrations (IC50 = 1-100 n) towards Jurkat, K562, Colo357, and A549 cell lines. Georg Thieme Verlag Stuttgart · New York.

DIHYDRO-ISO-CA-4 AND ANALOGUES: POTENT CYTOTOXICS, INHIBITORS OF TUBULIN POLYMERIZATION

The present invention relates to compounds of formula (I) below in which: —R1 and R3 represent, independently of one another, a methoxy group optionally substituted by one or more fluorine atoms, —R2 and R4 repr