Combinatorial Chemistry & High Throughput Screening - Volume 6, Issue 5, 2003

Libraries of displayed antibodies have been increasingly used to select or screen antibodies. It is generally well recognized that large libraries provide high probability of finding a given antibody. In this review, the factors that limit the sizes of current in vivo and ribosome-based in vitro display libraries to be around 10 11 members are first discussed. An analysis resulting in a quantitative correlation between the library si Read More

The Nobel Prize in Chemistry 1902 was given to Hermann Emil Fischer “in recognition of the extraordinary services he had rendered by his work on sugar and purine synthesis”. This truly great chemist of all time named a group of bicyclic nitrogenous structures as purines, discovered the synthesis of glucose, fructose and mannose starting from glycerol, and further created the basis for glucoside-, amino acid-, and enzym Read More

High-throughput ligand-based proton NMR screening performed in the presence of a spy molecule and a control molecule is a valuable tool for identifying drug leads. A limitation of the technique is represented by the severe overlap encountered in the screening of large chemical mixtures. An approach for overcoming this overlap problem is the use of multi-selective R1 filtered and COSY or TOCSY experiments. Application Read More

In solid tumors the predominant genetic mechanism for oncogene activation is through amplification of genes. The HER-2 (also known as ErbB2 / c-erbB2 / HER-2 / neu) oncogene is the most frequently amplified oncogene in breast cancer and is also commonly amplified in other forms of cancer. Alongside its important role in tumor induction, growth and progression, HER-2 is also a target for a new form of chemotherapy. Read More

A solution phase strategy for the multiple parallel synthesis of a demonstration library of indazoles is described by which regio-selectivity problems inherent to previous syntheses of this nucleus are largely overcome. Synthesis of selected components proceeded satisfactorily indicating that a fully realized library of indazole analogs could readily be produced using this methodology. Simple modifications of the basic nucleophilic Read More

A biased chemical library containing 91 differentially substituted thiazolidinones was prepared in an effort to improve the pharmacology of a known anticonvulsant agent V102862. The collection was prepared in a single step multi-component condensation reaction that produced good yields and very high crude purity (75%-85%). Seven compounds, identified within the library were shown to be more potent than V102862, our par Read More