Highly Efficient Semisynthesis of Biologically Active Epothilone Derivatives

2001 ◽  
pp. 97-111 ◽  
Author(s):  
Gregory D. Vite ◽  
Robert M. Borzilleri ◽  
Soong-Hoon Kim ◽  
Alicia Regueiro-Ren ◽  
W. Griffith Humphreys ◽  
...  
Keyword(s):  
Biologically Active ◽  
Highly Efficient

Nickel(0)-Catalyzed Linear-Selective Hydroarylation of Unactivated Alkenes and Styrenes with Arylboron Acids

2018 ◽  
Author(s):  
Honggui Lv ◽  
Li-Jun Xiao ◽  
Dongbing Zhao ◽  
Qi-Lin Zhou
Keyword(s):  
Butyric Acid ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Highly Efficient ◽  
Organoboronic Acids

Herein, we realized the first linear-selective hydroarylation of unactivated alkenes and styrenes with organoboronic acids by introducing directing groupon alkenes. Our method is highly efficient and scalable, and provides a modular route to assemble structurally diverse alkylarenes, especially for γ-aryl butyric acid derivatives, which have been widely utilized as chemical feedstocks to access multiple marketed drugs, and biologically active compounds.<br>

Triflic acid-catalyzed metal-free synthesis of (E)-2-cyanoacrylamides and 3-substituted azetidine-2,4-diones

2018 ◽  
Vol 42 (8) ◽  
pp. 6433-6440 ◽  
Author(s):  
Bapurao D. Rupanwar ◽  
Santosh S. Chavan ◽  
Anil M. Shelke ◽  
Gurunath M. Suryavanshi
Keyword(s):  
Biologically Active ◽  
Efficient Synthesis ◽  
Triflic Acid ◽  
Metal Free ◽  
Highly Efficient ◽  
Acid Catalyzed

A TfOH-catalyzed highly efficient synthesis of biologically active (E)-2-cyanoacrylamides and 3-substituted azetidine-2,4-diones has been reported with 64–94% yields under metal-free conditions.

scholarly journals Modular Synthesis of Trifunctional Peptide-oligonucleotide Conjugates via Native Chemical Ligation

2021 ◽  
Vol 9 ◽  
Author(s):  
Mohadeseh Dastpeyman ◽  
John A. Karas ◽  
Azin Amin ◽  
Bradley J. Turner ◽  
Fazel Shabanpoor
Keyword(s):  
Phase Conjugation ◽  
Cell Penetrating Peptides ◽  
Survival Motor Neuron ◽  
Biologically Active ◽  
Solution Phase ◽  
Cell Membrane Permeability ◽  
Native Chemical Ligation ◽  
High Yield ◽  
Chemical Ligation ◽  
Highly Efficient

Cell penetrating peptides (CPPs) are being increasingly used as efficient vectors for intracellular delivery of biologically active agents, such as therapeutic antisense oligonucleotides (ASOs). Unfortunately, ASOs have poor cell membrane permeability. The conjugation of ASOs to CPPs have been shown to significantly improve their cellular permeability and therapeutic efficacy. CPPs are often covalently conjugated to ASOs through a variety of chemical linkages. Most of the reported approaches for ligation of CPPs to ASOs relies on methodologies that forms non-native bond due to incompatibility with in-solution phase conjugation. These approaches have low efficiency and poor yields. Therefore, in this study, we have exploited native chemical ligation (NCL) as an efficient strategy for synthesizing CPP-ASO conjugates. A previously characterized CPP [ApoE(133–150)] was used to conjugate to a peptide nucleic acid (PNA) sequence targeting human survival motor neuron-2 (SMN2) mRNA which has been approved by the FDA for the treatment of spinal muscular atrophy. The synthesis of ApoE(133–150)-PNA conjugate using chemo-selective NCL was highly efficient and the conjugate was obtained in high yield. Toward synthesizing trifunctional CPP-ASO conjugates, we subsequently conjugated different functional moieties including a phosphorodiamidate morpholino oligonucleotide (PMO), an additional functional peptide or a fluorescent dye (Cy5) to the thiol that was generated after NCL. The in vitro analysis of the bifunctional CPP-PNA and trifunctional CPP-(PMO)-PNA, CPP-(peptide)-PNA and CPP-(Cy5)-PNA showed that all conjugates are cell-permeable and biologically active. Here we demonstrated chemo-selective NCL as a highly efficient and superior conjugation strategy to previously published methods for facile solution-phase synthesis of bi-/trifunctional CPP-ASO conjugates.

Nickel(0)-Catalyzed Linear-Selective Hydroarylation of Unactivated Alkenes and Styrenes with Arylboron Acids

2018 ◽  
Author(s):  
Honggui Lv ◽  
Li-Jun Xiao ◽  
Dongbing Zhao ◽  
Qi-Lin Zhou
Keyword(s):  
Butyric Acid ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Highly Efficient ◽  
Organoboronic Acids

Herein, we realized the first linear-selective hydroarylation of unactivated alkenes and styrenes with organoboronic acids by introducing directing groupon alkenes. Our method is highly efficient and scalable, and provides a modular route to assemble structurally diverse alkylarenes, especially for γ-aryl butyric acid derivatives, which have been widely utilized as chemical feedstocks to access multiple marketed drugs, and biologically active compounds.<br>

Engineering a noncarrier to a highly efficient carrier peptide for noncovalently delivering biologically active proteins into human cells

2007 ◽  
Vol 365 (2) ◽  
pp. 215-221 ◽  
Author(s):  
Eric Mahlum ◽  
Deendayal Mandal ◽  
Chandralekha Halder ◽  
Avudaiappan Maran ◽  
Michael J. Yaszemski ◽  
...  
Keyword(s):  
Human Cells ◽  
Biologically Active ◽  
Highly Efficient

scholarly journals Asparagine-EDTA MNPs: A Highly Efficient And Recyclable Magnetic Multifunctional Core-Shell Nanocatalyst For Green Synthesis of Biologically-Active 3,4-Dihydropyrimidin-2(1H)-One Compounds

2021 ◽  
Author(s):  
Negin Rostami ◽  
Mohammad G Dekamin ◽  
Ehsan Valiey ◽  
Hamidreza FaniMoghadam
Keyword(s):  
Biginelli Reaction ◽  
Biologically Active ◽  
Catalyst Loading ◽  
Core Shell ◽  
Environmental Friendliness ◽  
Green Protocol ◽  
Highly Efficient ◽  
Solvent Free Conditions ◽  
Wide Range ◽  
Magnetic Stability

Abstract In this study, the new asparagine grafted on the EDTA-modified Fe3O4@SiO2 core-shell (Fe3O4@SiO2-APTS-EDTA-asparagine) magnetic nanoparticles were prepared and their structures were properly confirmed using different spectroscopic, microscopic and magnetic methods or techniques such as FT-IR, EDX, XRD, FESEM, TEM, TGA and VSM. The Fe3O4@SiO2-APTS-EDTA-asparagine core-shell nanomaterial was examined, as a highly efficient multifunctional and recoverable nanocatalyst, for the synthesis of a wide range of nitrogen-containing heterocycles and biologically-active 3,4-dihydropyrimidin-2(1H)-one derivatives under solvent-free conditions. It was proved that Fe3O4@SiO2-APTS-EDTA-asparagine MNPs, as a catalyst having excellent thermally and magnetic stability, specific morphology and acidic sites, can activate the Biginelli reaction components. Moreover, environmental-friendliness and nontoxic nature properties of the catalyst, cost effectiveness, low catalyst loading, easy separation of the catalyst from products and short time of reaction are some of the remarkable advantages of this green protocol.

Polyoxometalate-based supramolecular porous frameworks with dual-active centers toward highly-efficient synthesis of functionalized p-benzoquinones

2021 ◽  
Author(s):  
Shenzhen Chang ◽  
Yanhong Chen ◽  
Haiyan An ◽  
Qingshan Zhu ◽  
Huiyun Luo ◽  
...  
Keyword(s):  
Selective Oxidation ◽  
Raw Materials ◽  
Biologically Active ◽  
Efficient Synthesis ◽  
Substituted Phenols ◽  
Active Centers ◽  
Highly Efficient ◽  
Ideal Method

Selective oxidation of substituted phenols is an ideal method for preparing functionalized p-benzoquinones (p-BQs), which are served as versatile raw materials for the synthesis of a variety of biologically active...

Highly Efficient and Economical Baculovirus Expression System for Preparing Human Papillomavirus Type16 Virus-like Particle

2004 ◽  
Vol 36 (8) ◽  
pp. 548-552 ◽  
Author(s):  
Jin Zheng ◽  
Jun Ma ◽  
Xiao-Feng Yang ◽  
Hong-Li Liu ◽  
Hong-Wei Cheng ◽  
...  
Keyword(s):  
Human Papillomavirus ◽  
Expression System ◽  
Recombinant Baculovirus ◽  
Biologically Active ◽  
Native Protein ◽  
Highly Efficient ◽  
His Tag ◽  
Virus Like Particle ◽  
Purification System

Abstract To improve the existing human papillomavirus type16 (HPV16) virus-like particle (VLP) preparation, a highly efficient, economical and timesaving system was established. Sf-9 cells were infected with recombinant baculovirus containing the target gene encoding HPV16L1 protein with 6×His tag, and harvested 72 h postinfection (p.i.) at 27 °C. The ProBondTM purification system was used for protein purification. The molecular weight of expressed HPV16L1 protein was 58 kD as revealed by SDS-PAGE, and confirmed by Western blot. The purity of denatured and native HPVL1 proteins that were prepared were 91.9% and 71.5%, respectively, which corresponded to a yield of 2.26 mg denatured protein and 1.84 mg native protein per 2×107 cells. The proteins were further analyzed by mouse erythrocyte hemagglutination assay and hemagglutination inhibition assay, and there effects on VLP formation were also visualized by transmission electron microscopy. Results showed that the native protein purified was biologically active as natural HPVL1 protein, inducing the murine erythrocyte agglutination and VLP formation. In addition, the purified recombinant HPV16L1 native protein with 6×His tag could self-assemble into virions in vitro. Hopefully, the present expression and purification system is promising to be convenient, timesaving and economical for preparation of HPV16 VLP vaccine.

Oxygen mediated highly efficient cobalt(ii) porphyrin-catalyzed reduction of functional chromones: experimental and computational studies

2019 ◽  
Vol 43 (13) ◽  
pp. 5228-5238 ◽  
Author(s):  
Poonam Poonam ◽  
Pratibha Kumari ◽  
Maria Grishina ◽  
Vladimir Potemkin ◽  
Abhishek Verma ◽  
...  
Keyword(s):  
Sodium Borohydride ◽  
Biologically Active ◽  
Computational Studies ◽  
Highly Efficient ◽  
Mediated Reduction

The highly efficient oxygen mediated reduction of functional chromones with sodium borohydride (NaBH4) catalyzed by cobalt(ii) porphyrins afforded biologically active chroman-4-ols as the reduction products in 80–98% yields.

Characterization of photosystem II with the atomic-force microscope

1992 ◽  
Vol 50 (2) ◽  
pp. 1146-1147
Author(s):  
Kathleen M. Marr ◽  
Mary K. Lyon
Keyword(s):  
Photosystem Ii ◽  
Atomic Force Microscope ◽  
Three Dimensional ◽  
Biologically Active ◽  
Atomic Force ◽  
Freeze Etching ◽  
Image Averaging ◽  
Oxygen Evolving ◽  
Averaging Techniques

Photosystem II (PSII) is different from all other reaction centers in that it splits water to evolve oxygen and hydrogen ions. This unique ability to evolve oxygen is partly due to three oxygen evolving polypeptides (OEPs) associated with the PSII complex. Freeze etching on grana derived insideout membranes revealed that the OEPs contribute to the observed tetrameric nature of the PSIl particle; when the OEPs are removed, a distinct dimer emerges. Thus, the surface of the PSII complex changes dramatically upon removal of these polypeptides. The atomic force microscope (AFM) is ideal for examining surface topography. The instrument provides a topographical view of individual PSII complexes, giving relatively high resolution three-dimensional information without image averaging techniques. In addition, the use of a fluid cell allows a biologically active sample to be maintained under fully hydrated and physiologically buffered conditions. The OEPs associated with PSII may be sequentially removed, thereby changing the surface of the complex by one polypeptide at a time.

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