Design and synthesis of bioactive molecules
Prof. Fengzhi Zhang, Hangzhou Medical College
Prof. David R. Spring, University of Cambridge
The design and synthesis of bioactive molecules is of great importance in advancing drug development, understanding biological processes, and driving technological innovation. This thematic issue aims to cover a diverse range of topics related to the rational design, chemical synthesis, and biological evaluation of molecules with specific bioactivities:
- Design and synthesis of bioactive molecules that can interact with specific biological targets
- Bifunctional and multifunctional bioactive molecules such as PROTACs
- Novel green synthetic methodologies for the fast and efficient preparation of bioactive molecules
- Natural-product-inspired synthesis and evaluation
- Recent advances and trends, such as artificial intelligence and machine learning in bioactive molecule design and synthesis
Synthesis, biological and electrochemical evaluation of glycidyl esters of phosphorus acids as potential anticancer drugs
- Almaz A. Zagidullin,
- Emil R. Bulatov,
- Mikhail N. Khrizanforov,
- Damir R. Davletshin,
- Elvina M. Gilyazova,
- Ivan A. Strelkov and
- Vasily A. Miluykov
Beilstein J. Org. Chem. 2025, 21, 1909–1916, doi:10.3762/bjoc.21.148
Rhodium-catalysed connective synthesis of diverse reactive probes bearing S(VI) electrophilic warheads
- Scott Rice,
- Julian Chesti,
- William R. T. Mosedale,
- Megan H. Wright,
- Stephen P. Marsden,
- Terry K. Smith and
- Adam Nelson
Beilstein J. Org. Chem. 2025, 21, 1924–1931, doi:10.3762/bjoc.21.150
Efficient solid-phase synthesis and structural characterization of segetalins A–H, J and K
- Liangyu Liu,
- Wanqiu Lu,
- Quanping Guo and
- Zhaoqing Xu
Beilstein J. Org. Chem. 2025, 21, 2612–2617, doi:10.3762/bjoc.21.202
Synthesis of a HDAC inhibitor–nanogold probe for cryo-EM visualization in class I HDAC co-repressor complexes
- Wiktoria A. Pytel,
- John W. R. Schwabe and
- James T. Hodgkinson
Beilstein J. Org. Chem. 2026, 22, 480–485, doi:10.3762/bjoc.22.35
Design and synthesis of an erdafitinib-based selective FGFR2 degrader
- Yumeng Jin,
- Shidong Wang,
- Sihan Pan,
- Shuqi Huang,
- Weichen Zhou,
- Xiaohao Huang,
- Lei Zheng and
- Lingfeng Chen
Beilstein J. Org. Chem. 2026, 22, 583–591, doi:10.3762/bjoc.22.44
Towards the targeted protein degradation of CK2: design and synthesis of CAM4066-based PROTACs
- Sophie Day-Riley,
- Sona Krajcovicova,
- Aryaman Raj Sokhal,
- Jan L. Venne,
- Paul Brear,
- Marko Hyvönen,
- Benjamin C. Whitehurst,
- Jason S. Carroll and
- David R. Spring
Beilstein J. Org. Chem. 2026, 22, 611–619, doi:10.3762/bjoc.22.47
Advantages of PROTACs in achieving selective degradation of homologous protein families
- Luxi Yang,
- Xinfei Mao,
- Jingyi Zhang,
- Jing Shu,
- Wenhai Huang,
- Xiaowu Dong,
- Yinqiao Chen and
- Mingfei Wu
Beilstein J. Org. Chem. 2026, 22, 628–661, doi:10.3762/bjoc.22.49
Using generative AI to transform peptide hits into small molecule leads
- Joshua Mills and
- Yu Heng Lau
Beilstein J. Org. Chem. 2026, 22, 672–679, doi:10.3762/bjoc.22.51
