The increasing value of biomass: moving from C6 carbohydrates to multifunctionalized building blocks via 5‐(hydroxymethyl) furfural

KI Galkin, VP Ananikov - ChemistryOpen, 2020 - Wiley Online Library
Recent decades have been marked by enormous progress in the field of synthesis and
chemistry of 5‐(hydroxymethyl) furfural (HMF), an important platform chemical widely …

The European Lead Factory: a blueprint for public–private partnerships in early drug discovery

A Karawajczyk, KM Orrling, JSB De Vlieger… - Frontiers in …, 2017 - frontiersin.org
The European Lead Factory (ELF) is a public–private partnership (PPP) that provides
researchers in Europe with a unique platform for translation of innovative biology and …

Access to a structurally complex compound collection via ring distortion of the alkaloid sinomenine

A Garcia, BS Drown, PJ Hergenrother - Organic letters, 2016 - ACS Publications
Many compound collections used in high-throughput screening are composed of members
whose structural complexity is considerably lower than that of natural products. We …

Limonin as a starting point for the construction of compounds with high scaffold diversity

L Furiassi, EJ Tonogai… - Angewandte Chemie …, 2021 - Wiley Online Library
Structurally complex natural products have been a fruitful source for the discovery and
development of new drugs. In an effort to construct a compound collection populated by …

Copper-catalyzed Aza-Michael addition of 2-aminobenzoate to β-substituted α, β-unsaturated ketones: one-pot synthesis of 3-carbonyl-2-substituted quinolin-4 (1 H) …

S Kang, S Park, K Kim, C Song… - The Journal of Organic …, 2018 - ACS Publications
We present a new and straightforward one-pot process for the synthesis of 3-carbonyl-4-
quinolone derivatives through highly efficient Cu-catalyzed aza-Michael addition of 2 …

Synthesis and evaluation of the performance of a small molecule library based on diverse tropane-related scaffolds

RA Lowe, D Taylor, K Chibale, A Nelson… - Bioorganic & Medicinal …, 2020 - Elsevier
A unified synthetic approach was developed that enabled the synthesis of diverse tropane-
related scaffolds. The key intermediates that were exploited were cycloadducts formed by …

Intermolecular Diels–Alder Cycloaddition/Cross-Coupling Sequences of 2-Bromo-1, 3-butadienes

H Choi, HJ Shirley, HRM Aitken, T Schulte… - Organic …, 2020 - ACS Publications
2-Bromo-1, 3-butadienes are demonstrated to be effective substrates for tandem Diels–
Alder/transition metal cross-coupling reaction sequences. Intermolecular cycloaddition of a 2 …

Translation of innovative chemistry into screening libraries: an exemplar partnership from the European Lead Factory

R Morgentin, M Dow, A Aimon, G Karageorgis… - Drug discovery today, 2018 - Elsevier
Highlights•Partnership translated academic chemistry into screening libraries.•Many
molecular scaffolds were sp 3-rich and natural-product-like.•A blueprint for exploiting …

Alkaloid diversification in the genus Palicourea (Rubiaceae: Palicoureeae) viewed from a (retro-)biogenetic perspective

A Berger, K Valant-Vetschera, J Schinnerl… - Phytochemistry …, 2022 - Springer
The species-rich genus Palicourea (Rubiaceae: Palicoureeae) is source of an intriguing
diversity of alkaloids derived from tryptamine and its precursor tryptophan. So far simple …

An IMDAF approach to annellated 1, 4: 5, 8-diepoxynaphthalenes and their metathesis reaction leading to novel scaffolds displaying an antiproliferative activity toward …

EA Kvyatkovskaya, KK Borisova, PP Epifanova… - New Journal of …, 2021 - pubs.rsc.org
A series of 1, 4: 5, 8-diepoxynaphthalenes, annellated with six-membered carbo-and
heterocycles, was obtained via the intramolecular Diels–Alder furan (IMDAF) cycloaddition …