Diversity-oriented synthesis articles within Nature

Featured

• Article | 15 December 2021

  Synthon-based ligand discovery in virtual libraries of over 11 billion compounds

  V-SYNTHES, a scalable and computationally cost-effective synthon-based approach to compound screening, identified compounds with a high affinity for CB2 and CB1 in a hierarchical structure-based screen of more than 11 billion compounds.

  • Arman A. Sadybekov
  • , Anastasiia V. Sadybekov
  •  & Vsevolod Katritch

• Article | 30 September 2019

  Metal-free directed sp²-C–H borylation

  A method for the site-selective C–H borylation of arenes and heteroarenes is described, in which BBr₃ acts as both a reagent and a catalyst.

  • Jiahang Lv
  • , Xiangyang Chen
  •  & Zhuangzhi Shi

• News & Views Forum | 02 February 2011

  A question of library design

  Two approaches have emerged for creating libraries of compounds for use in biological screening assays for drug discovery — fragment-based ligand design and diversity-oriented synthesis. Advocates of each approach discuss their favoured strategy.

  • Philip J. Hajduk
  • , Warren R. J. D. Galloway
  •  & David R. Spring