A5042315492- Protein Degradation and Inhibitors
- X-ray Diffraction in Crystallography
- Ubiquitin and proteasome pathways
- Crystallization and Solubility Studies
- Asymmetric Hydrogenation and Catalysis
- Asymmetric Synthesis and Catalysis
- PARP inhibition in cancer therapy
- Organoboron and organosilicon chemistry
- Catalytic Cross-Coupling Reactions
- Peptidase Inhibition and Analysis
- Chemical Synthesis and Analysis
- Crystallography and molecular interactions
- Synthetic Organic Chemistry Methods
- Prostate Cancer Treatment and Research
- Synthesis and biological activity
- Quinazolinone synthesis and applications
- Cancer therapeutics and mechanisms
- Cancer, Lipids, and Metabolism
- Multiple Myeloma Research and Treatments
- Hormonal and reproductive studies
- Integrated Circuits and Semiconductor Failure Analysis
- Histone Deacetylase Inhibitors Research
- Advanced Synthetic Organic Chemistry
Tsinghua University
2022
Center for Life Sciences
2022
Sichuan University
2016-2020
West China Hospital of Sichuan University
2020
State Key Laboratory of Biotherapy
2016-2019
Here we report an iridium-catalyzed asymmetric umpolung allylation of imines as a general approach to prepare 1,4-disubstituted homoallylic amines, fundamental class compounds that are hitherto not straightforward obtain. This transformation proceeds by cascade involving intermolecular regioselective 2-azaallyl anions and following 2-aza-Cope rearrangement, utilizes easily available reagents catalysts, tolerates substantial scope substrates, readily leads various enantioenriched, primary amines.
Described here is an enantioselective approach of making chiral, β-substituted homoallylic organoboronic esters. In the presence LiOtBu and a catalytic amount silver salt, commercial bis[(pinacolato)boryl]methane participated in iridium-catalyzed asymmetric allylation reactions, delivered "CH2B(pin)" group, yielded title compounds from allylic carbonates. The synthetic utility prepared chiral organoboronates was demonstrated by their conversion to other important classes compounds.
The nuclear protein poly(ADP-ribose) polymerase-1 (PARP1) has a well-established role in the signaling and repair of DNA is validated therapeutic target for cancers other human diseases. Here, we have designed, synthesized, evaluated series small-molecule PARP1 degraders based on proteolysis-targeting chimera (PROTAC) concept. Our efforts led to discovery highly potent degraders, as exemplified by compound 18 (SK-575). SK-575 potently inhibits growth cancer cells bearing BRCA1/2 mutations...
A method to prepare chiral β3-amino esters from methyl 3-aminopropanoate was described. This capitalized on a sequence involving an Ir-catalyzed asymmetric allylation of 2-azaallyl anions and 2-aza-Cope rearrangement. β3-Amino containing versatile alkene group were prepared.