Organic Synthesis

ADCs

Several Ways of Thiol Coupling in ADCs

The popularity of thiol coupling in ADC preparation can be attributed to three factors: It is essential to note that a reduction step is always required before coupling to release […]

Covalent, Non-covalent, and Covalent Reversible Drug Design in Medicinal Chemistry

Covalent, Non-covalent, and Covalent Reversible Drug Design in Medicinal Chemistry

Chemical drugs can be classified into three categories based on their binding modes: covalent drugs, non-covalent drugs, and covalent reversible drugs. Covalent drugs have strong binding ability and high efficacy, […]

Design Ideas for FDA-Approved Small Molecule Drugs in the third quarter of 2023

Design Ideas for FDA-Approved Small Molecule Drugs in the third quarter of 2023

FDA approved the marketing of 14 drugs in the third quarter of 2023, including 6 small molecule drugs. This article mainly focuses on the drug design ideas of small molecule drugs, hoping […]

ligands in PROTACs

Thalidomide Analogs and Other CRBN Ligands in PROTACs

History of Thalidomide During the 1950s-1960s, thalidomide was widely used as an antiemetic for pregnant women, leading to a tragic outcome with thousands of cases of malformed babies. However, in 1965, […]

lab experiment

FDA-approved small molecule kinase inhibitors-Part 3

Fostamatinib is the precursor drug of active metabolite R406. It is a Syk inhibitor with an IC50 value of 41 nM. It strongly inhibits Syk but does not inhibit Lyn. […]

drug research

FDA-approved small molecule kinase inhibitors-Part 2

Dabrafenib (GSK2118436) is a mutant BRAFV600-specific inhibitor, with an IC50 of 0.7 nM in cell-free assays. It shows 7-fold and 9-fold lower potency against B-Raf(wt) and c-Raf, respectively. Synthetic route: […]

drug development

FDA-approved small molecule kinase inhibitors-Part 1

Kinase inhibitors can be divided into monoclonal antibodies (mAbs) and small molecule kinase inhibitors (SMKIs) based on their structure and size. Monoclonal antibodies have achieved great success in the development […]

Organic Chemistry Experiments

BOC Sciences Updates Helpful Q&As about Organic Chemistry Experiments

What are the methods of heating in an organic chemical reaction? Organic reactions are most commonly heated through the asbestos mesh and cannot be heated directly by fire. Otherwise, the instrument […]

linker design

Linker Design Impacts Drug Conjugate Pharmacokinetics and Efficacy

In recent years, antibody-drug conjugates (ADCs) have achieved substantial success in cancer therapy. Typically, an antibody or peptide in a conjugated drug acts as a precisely located “navigator” while a small-molecule […]

Monoaromatic Heterocyclic Chemistry: Applications and Synthesis

Monoaromatic Heterocyclic Chemistry: Applications and Synthesis

Summary Heterocyclic compounds with aromatic characteristics are called aromatic heterocyclic compounds, which can be classified into monoaromatic heterocycles and fused heterocycles. The common monoaromatic heterocycles are five-membered Furan, Pyrrole, Thiophene, Pyrazole, Imidazole, […]