|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  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.