Expanding the medicinal chemistry synthetic toolbox

J Boström, DG Brown, RJ Young… - Nature Reviews Drug …, 2018 - nature.com
The key objectives of medicinal chemistry are to efficiently design and synthesize bioactive
compounds that have the potential to become safe and efficacious drugs. Most medicinal …

Design, Synthesis, and Phenotypic Profiling of Pyrano‐Furo‐Pyridone Pseudo Natural Products

A Christoforow, J Wilke, A Binici, A Pahl… - Angewandte …, 2019 - Wiley Online Library
Natural products (NPs) inspire the design and synthesis of novel biologically relevant
chemical matter, for instance through biology‐oriented synthesis (BIOS). However, BIOS is …

Diversity oriented clicking (DOC): divergent synthesis of SuFExable pharmacophores from 2‐substituted‐alkynyl‐1‐sulfonyl fluoride (SASF) hubs

CJ Smedley, G Li, AS Barrow, TL Gialelis… - Angewandte …, 2020 - Wiley Online Library
Abstract Diversity Oriented Clicking (DOC) is a unified click‐approach for the modular
synthesis of lead‐like structures through application of the wide family of click …

Water‐soluble non‐classical benzene mimetics

VV Levterov, Y Panasyuk, VO Pivnytska… - Angewandte …, 2020 - Wiley Online Library
A new generation of saturated benzene mimetics, 2‐oxabicyclo [2.1. 1] hexanes, was
developed. These compounds were designed as analogues of bicyclo [1.1. 1] pentane with …

Chromopynones are pseudo natural product glucose uptake inhibitors targeting glucose transporters GLUT-1 and-3

G Karageorgis, ES Reckzeh, J Ceballos… - Nature …, 2018 - nature.com
The principles guiding the design and synthesis of bioactive compounds based on natural
product (NP) structure, such as biology-oriented synthesis (BIOS), are limited by their partial …

The 3F Library: Fluorinated Fsp3‐Rich Fragments for Expeditious 19F NMR Based Screening

NS Troelsen, E Shanina… - Angewandte …, 2020 - Wiley Online Library
Fragment‐based drug discovery (FBDD) is a popular method in academia and the
pharmaceutical industry for the discovery of early lead candidates. Despite its wide‐spread …

Synthesis of Indomorphan pseudo‐natural product inhibitors of glucose transporters GLUT‐1 and‐3

J Ceballos, M Schwalfenberg… - Angewandte …, 2019 - Wiley Online Library
Bioactive compound design based on natural product (NP) structure may be limited because
of partial coverage of NP‐like chemical space and biological target space. These limitations …

Combination of pseudo‐natural product design and formal natural product ring distortion yields stereochemically and biologically diverse pseudo‐sesquiterpenoid …

J Liu, J Flegel, F Otte, A Pahl, S Sievers… - Angewandte …, 2021 - Wiley Online Library
We describe the synthesis and biological evaluation of a new natural product‐inspired
compound class obtained by combining the conceptually complementary pseudo‐natural …

Phenotyping reveals targets of a pseudo‐Natural‐product autophagy inhibitor

DJ Foley, S Zinken, D Corkery, L Laraia… - Angewandte Chemie …, 2020 - Wiley Online Library
Abstract Pseudo‐natural‐product (NP) design combines natural product fragments to
provide unprecedented NP‐inspired compounds not accessible by biosynthesis, but …

Ring‐Expansion Approach to Medium‐Sized Lactams and Analysis of Their Medicinal Lead‐Like Properties

LG Baud, MA Manning, HL Arkless… - … A European Journal, 2017 - Wiley Online Library
Medium‐sized rings are widely considered to be under‐represented in biological screening
libraries for lead identification in medicinal chemistry. To help address this, a library of …