The 3<sup>rd</sup> International Conference on Drug Discovery & Therapy: Dubai, February 7 - 11, 2011

Hot topic in Natural Products (Track)



High-Throughput Natural Products Chemistry for Drug Discovery: Is it Possible

Mark O’Neil-Johnson
Sequoia Sciences, Inc. 1912 Innerbelt Business Center Drive Saint Louis, MO 63119, USA

Abstract:

Sequoia Sciences identifies novel chemistry from its library of structurally diverse small molecules isolated from plants.  The proprietary design of this library allows for the biological screening of these compounds at optimal HTS concentrations without non-drug-like interferences.  Sequoia built this analytical process such that rapid isolation and structure elucidation of active compounds could be accomplished.  Using the extremely sensitive TCI MicroCryoProbe, structure elucidation of active compounds is completed on samples of limited mass.  Relative to synthetic library HTS, the question remains, is it really high-throughput natural products chemistry?  Can the rate limiting step, structure elucidation process, be a higher throughput process?

The scientific strategy that Sequoia employs in order to rapidly uncover the chemical diversity contained in plant natural products will be outlined.  This presentation will expand upon the ground breaking cryoprobe introduced by Bruker BioSpin, the TCI 1.7mm MicroCryoProbe.  For the structure elucidation process, this advanced capillary scale NMR cryoprobe acquires complete NMR data sets on micrograms (10 micrograms) of material.  The Bruker TCI 1.7mm MicroCryoProbe has now extended the high-throughput process to include NMR data acquisition.

This talk outlines sample loading and data acquisition ease of the 1.7mm probe, presenting data on biologically active compounds isolated from preparative HPLC fractions from Sequoia’s library.  Sequoia’s inclusion of the TCI 1.7mm MicroCryoProbe compliments its current platform technologies for high-throughput natural products research for drug discovery.

Keywords: Sequoia Sciences has a natural product library of structurally diverse small molecules from plants, Bruker TCI 1.7mm MicroCryoProbe, an advanced capillary scale cryoprobe, Rapid acquisition of NMR data for structure elucidation