Highly Stereoselective Synthesis of a Compound Collection Based on the Bicyclic Scaffolds of Natural Products
Acquiring chemotypes beholding structural features of natural products, for instance high sp3 character, the synthesis of compound collections based on core-scaffolds of natural products presents a promising strategy in drug discovery research.
Due to their vast structural and chemical diversity, natural products (NPs) have been a rich source of bioactive small molecules to fuel the drug discovery process. Herein, we report a natural product inspired syntheses of six different chemotypes – novel bicyclic hetero- and carbocyclic frameworks, exhibiting high three-dimensional complexity and drug-like physicochemical properties. Moreover, two of the presented scaffolds were further diversified at Taros Chemicals through parallel synthesis, affording compound libraries (ca 350 molecules each) which would be exposed to various biological screenings within the European Lead Factory consortium.
About Taros Chemicals
Taros is a privately owned discovery chemistry company, working with global pharmaceutical, biotech and chemical companies since 1999. Alongside our performance chemicals and material science division, Taros’ drug discovery mission is to create drug candidates as potential new medicines. Taros has a strong scientific track record on many biomolecular targets in all main therapeutic areas and thereby adding considerable value to collaborations from target validation and hit identification to lead generation and optimization. Taros’ core expertise ranges from custom synthesis and process development to modern medicinal and computational chemistry, as well as compound library design and production.
Taros was heading the chemistry efforts of the EUR 196 million funded European Lead Factory (2013-2018) and is currently heading its EUR 36.5 million funded continuation (2019-2022). Moreover, Taros is deeply engaged in other research alliances like the EUR 11 million funded Drug Discovery Hub Dortmund.
Youri R. Mesmoudi, Executive Vice President, e-mail: innovation |at| taros.de
As a leading contract research organization in discovery chemistry and custom synthesis, Taros provides comprehensive solutions to meet our clients’ needs from diverse branches and applications
Our experienced chemists practice a pragmatic culture and customer-centric approach in order to exceed project expectations, despite challenges, bridging very narrow timelines. They are trained to consider economic, safety and ecological boundaries and conditions laid out for all stages of the project, starting from the development of synthetic routes to…