Combinatorial synthesis of natural products | Request …
Initially, the field focused primarily on the synthesis of peptide and oligonucleotide libraries. H. Mario Geysen, distinguished research scientist at Glaxo Wellcome Inc., Research Triangle Park, N.C., helped jump-start the field in 1984 when his group developed a technique for synthesizing peptides on pin-shaped solid supports. At the Coronado conference, Geysen reported on his group's recent development of an encoding strategy in which molecular tags are attached to beads or linker groups used in solid-phase synthesis. After the products have been assayed, the tags are cleaved and determined by mass spectrometry (MS) to identify potential lead compounds.
Synthesis of natural-product-based compound libraries (2000) ..
Combinatorial Chemistry is used to synthesize large number of chemical compounds by combining sets of building blocks. Each newly synthesized compound's composition is slightly different from the previous one. A traditional chemist can synthesize 100-200 compounds per year. A combinatorial robotic system can produce in a year thousands or millions compounds which can be tested for potential drug candidates in a high-throughput screening process.
By accelerating the process of chemical synthesis, this method is having a profound effect on all branches of chemistry, but especially on drug discovery. Through the rapidly evolving technology of combi-chemistry, it is now possible to produce compound libraries to screen for novel bioactivities. This powerful new technology has begun to help pharmaceutical companies to find new drug candidates quickly, save significant money in preclinical development costs and ultimately change their fundamental approach to drug discovery 2.
Natural Product-like Combinatorial Libraries Based on Privileged ..
Boger, Total synthesis of vinblastine, related natural products, key analogues and development of inspired methodology suitable for the systematic study of their structure-function properties, Acc.
of libraries based on natural product ..
2) Some means of linking the substrate to this solid phase that permits selective cleavage of some or all of the product from the solid support during synthesis for analysis of the extent of reaction(s), and ultimately to give the final product of interest;
High-Throughput Synthesis of Natural Products | …
Boger, Isolation, total synthesis, and structure elucidation of chlorofusin, a natural product inhibitor of the p53-MDM2 protein-protein interaction Nat.
Natural product-like combinatorial libraries - SciELO
Finally, structural motifs from the biologically active parent molecule have been identified and have served for design of natural product mimicry, which facilitates the creation of combinatorial libraries.">
Journal of the Brazilian Chemical Society ..
Description :Traditionally, the search for new compounds from natural products has been a time- and resource-intensive process. The recent application of combinatorial methods and high-throughput synthesis has all...
synthesis, and screening of libraries ..
Synthesis of Combinatorial Library: Combinatorial synthesis on solid phase can generate very large numbers of products, using a method described as mix and split synthesis. This technique was pioneered by Furka and has been enthusiastically exploited by many others since its first disclosure. For example, Houghten has used mix and split on a macro scale in a "tea bag" approach for the generation of large libraries of peptides.
The Ulijn Group - Nanoscience at ASRC/CUNY
Abstract: Computer-based analysis revealed that natural products exhibit a remarkable structural diversity of molecular frameworks and scaffolds that could be systematically exploited for combinatorial synthesis.