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Friday, August 29, 2014
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Microwave-Assisted Rapid Access to Bio-active Heterocycles
Vivek Polshettiwar and Rajender S. Varma

Environmentally benign protocols have been developed for the synthesis of various pharmaceutically active heterocycles namely 1,3,4-oxadiazoles, 1,3,4-thiadiazoles, 1,3-dioxanes, pyrazoles, hydrazones and 3,4-dihydropyrimidin-2(1H)-ones, which proceed under the influence of microwave irradiation and using eco-friendly conditions. These greener protocols were catalyzed efficiently by solid supported Nafion®NR50, phosphorus pentasulfide on alumina under solvent-free conditions.

Caveolin-1 Expression as a Possible Biomarker in Pancreatic Cancer Diagnosis
C. Tanase, E. Raducan, L. Albulescu, E. Codorean, M.I. Nicolescu, D.I. Popescu, M.L. Cruceru and A.C. Popa

Caveolin1 (Cav-1) function either as a tumor supressor or as a promoter of metastasis. Overexpresion of cav-1 was correlated with: tumoral grading, proliferration markers (Ki67, p53), serum tumor markers (CEA, CA19.9) and angiogenic markers (VEGF, bFGF).

New Accessories for High Throughput and Combinatorial Approach in a Microwave Batch Reactor
Alexander Stadler, Thomas Karner, Matthias Treu

A unique sealable well-plate system is introduced allowing screening reactions in a 8x6 well format with operation limits of 200°C and 20 bar and a reaction volume of 0.3 mL per well. An appropriate turntable enables to proceed up to 4 of these SiC well plates in one run resulting in 192 parallel reactions at a time. Reaction control is achieved by sensing the IR temperature of the plate surface.

Facile Synthesis of Hydrocarbon-Stapled Peptides
Wei Qiu, Ling Sheng, Peng Zou, Ke Yang, Anita Hong and Xiaohe Tong

This poster describes a versatile synthesis method for hydrocarbon-stapled peptides. Asymmetric synthesis of (S)-Fmoc-a-(2’-pentenyl)-alanine was successfully accomplished via an Ala-Ni (II)-BPB-complex [3] in three steps with a 40% total yield. The 12-mer peptide containing two a- pentenyl-alanines on positions 4 and 8 was synthesized by Fmoc solid phase synthesis method. After olefin metathesis and cleavage, the peptide was purified by HPLC to obtain the hydrocarbon-stapled peptide.

In silico Screening for Signalosome Inhibitors
Melanie Füllbeck, Wolfgang Dubiel, Cornelius Frömmel, Andrean Goede and Robert Preissner

The COP9 signalosome (CSN) is involved in cell cycle regulation, possesses kinase activity and is therefore an interesting therapeutic target for anti-tumor drugs. Known inhibitors of the kinase activity exhibit low binding constants. Using them a 3D similarity screening for our in-house database is performed. The superposition algorithm enables the explicit consideration of conformers reflecting the structural flexibility.

Design and Synthesis of Novel Thiazolidine and Pyrrolidine Derivatives as DPP-IV Inhibitors
Ramesh C. Gupta, Laxmikant Chhipa, A. B. Mandhare, Sunil S. Nadkarni, Deepa Joshi, Shital Zambad, Padmaja Pathak, Vijay C. Chauthaiwale and C. Dutt

DPP-IV inhibitors have many advantages like increasing insulin release and suppressing glucagon release in a glucose-dependent manner hence they pose less of a hypoglycemia risk and no weight gain than that observed with other antihyperglycemic agents. To develop a novel potent DPP-IV inhibitors we have synthesized and evaluated DPP-IV inhibiting activity and selectivity of various compounds. All these results would facilitate further development of Novel drugs for treatment of type 2 diabetes.

Pharmacophore Mapping of Flavone Derivatives for Aromatase Inhibiton
Shuchi Nagar, Md Ataul Islam, Arup Mukherjee and Achintya Saha

The study explores the structural requirements of flavones for inhibition of aromatase activity. The QSAR analysis generates the model that shows the importance of flavone ring and with molecular lipophilicity. Presence of additional aromatic ring and m-hydroxy substitution on that ring increases inhibitory activity. Space modeling study further adjudged the presence of hydrogen bond acceptor, hydrophobic and aromatic ring and critical distance among features for the inhibitory activity.

Solid Phase Synthesis of a Fluorescent Peptide: Comparison of Fmoc-Lys(5-FAM)-Resin and Fmoc-Lys[5-FAM(Trt)-Resin
Wenyu Fu, Ling Sheng, Anita Hong and Xiaohe Tong

We have prepared and performed comparison studies using two kinds of resins, Fmoc-Lys(5-FAM)-Rink Amide resin (I) and Fmoc-Lys[5-FAM(trt)]-Rink Amide resin (II), the latter contains a phenolic hydroxyl group protected with a trityl group. Syntheses were carried out under the same standard conditions and the peptides obtained showed no significant difference in purity. The results of these studies showed that resin (I) is adequate for synthesis of C-terminal fluorescent labeled peptide.

EasyBeacons™ - new Probes Ideal for Realtime PCR Detection of Methylation Status of Single CpG Duplets and SNPs
K. Skadhauge, C. Nielsen & U.B. Christensen

The EasyBeacons™ presented here are based on the novel technology Intercalating Nucleic Acid, INA®, linked to a fluorophore and a quencher. INA® is composed of normal DNA nucleotides and Intercalating Pseudo Nucleotides (IPNs). The fact that the EasyBeacons™ are mostly composed of normal DNA nucleotides means that in many respects EasyBeacons™ behave like DNA based probes, allowing use of standard buffers, primers and enzymes and hence reduces the optimisation efforts.

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Showing Results 81 - 90 of 142
Scientific News
Cancer-Fighting Drugs Might Also Stop Malaria Early
A number of compounds have been identified which could be used to fight malaria.
Collaboration Leads to Possible Shortcut to New Drugs
The reaction, reported in Science, demonstrates how a carboxylic acid can be transformed into a very reactive site through use of a novel photoredox catalyst.
Catalysts That Mimic Enzymes Could Revolutionize Pharmaceutical Manufacturing
Structures made of polymer chains allow the catalysts to work in water.
Discovery of How Taxol Works Could Lead to Better Anticancer Drugs
The drug’s interference with the normal function of microtubules could help in designing better anticancer drugs.
Chemists Discover Cancer Drug Candidate Structure
Chemists at The Scripps Research Institute have determined the correct structure of a highly promising anticancer compound approved by the U.S. FDA for clinical trials in cancer patients.
Novel Drug Targets for Allergy Identified
Researchers have identified several target molecules which are suitable for the development of new allergy drugs.
Drug Does Not Improve Set of Cardiovascular Outcomes for Diastolic Heart Failure
NIH-supported study finds drug does appear to reduce hospitalizations for diastolic heart failure.
Entirely Novel Strategy to Molecular Anticancer Therapy Tricks Malignant Cells
New drug prevents tumour growth by inhibiting the nucleotide sanitizing enzyme MTH1.
New Trial of Personalized Cancer Treatment Begins in Oxford
Phase I trial in Oxford will investigate a new drug, called CXD101.
Flow Microreactor Synthesis in Organo-Fluorine Chemistry
This review focuses on successful examples on synthesis and reactions of fluorine-containing molecules by the use of flow microreactor systems.
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