New Chemical Scaffold Starting Points for Targeting Inflammation Preferred, Novel and Neglected Scaffolds in a Drug Discovery Program
Mark A. O’Neil-Johnson Sequoia Sciences, Inc. 1912 Innerbelt Business Center Dr., Saint Louis, MO, USA
Abstract:
Plants have a history of producing compounds with antibacterial, cancer and CNS activities against multiple species for defensive purposes. Since homologous biological mechanisms exist across species, searching for compounds isolated from plants for novel anti-inflammatory activities warrants investigation. Sequoia has built an analytical process such that rapid isolation and structure elucidation of active compounds could be accomplished. Utilizing these advanced analytical techniques, Sequoia Sciences has identified preferred, novel and neglected drug-like scaffolds from its library containing extensively purified plant compounds. These compounds exhibit activities against bacteria, virus and tumor cells. Based upon these novel discoveries and the fact that Sequoia’s library has yet to be screened in anti-inflammatory assays, Sequoia believes that compounds with these biological activities are waiting to be discovered from its library and may inspire lead optimization programs. Some of the scaffolds Sequoia has identified have more chiral centers and non-aromatic rings when compared to synthetically inspired compounds. Since recent evidence from Lipkus and coworkers1 suggests that the majority of known scaffolds have been neglected in drug discovery programs, examining preferred, novel and neglected drug-like scaffolds from plants may inspire the anti-inflammatory drugs of 2020. Certain representative scaffolds and compounds identified from Sequoia’s library will be presented.