BOC Sciences Blog

Design, characterization and cellular uptake studies of fluorescence-labeled prototypic cathepsin inhibitors

Design, characterization and cellular uptake studies of fluorescence-labeled prototypic cathepsin inhibitors

The cathepsins comprise a family of lysosomal proteolytic enzymes. Eleven human cathepsins are cysteine proteases of the papain-like subfamily C1A and represent the best characterized group of cathepsins. Cysteine cathepsins […]

Perspectives on natural product epigenetic modulators in chemical biology and medicine

Perspectives on natural product epigenetic modulators in chemical biology and medicine

Epigenetic therapies from natural products in the clinic 1. Clinically approved natural product epigenetic modulators Despite an increasing number of synthetically-derived epigenetic modulators being taken into preclinical and clinical studies, […]

Synthesis, anticancer evaluation and docking study of vadimezan derivatives with carboxyl substitution

Synthesis, anticancer evaluation and docking study of vadimezan derivatives with carboxyl substitution

Xanthones with various substituents on the three-membered heterocyclic ring skeleton exhibit diverse biological activities, such as antihypertensive, antioxidative, antithrombotic and anticancer activities. Naturally existing xanthone analogues, including gentiakochianin, α-mangostin and […]

The use of environmental metrics to evaluate green chemistry improvements to the synthesis of (S,S)-reboxetine succinate

The use of environmental metrics to evaluate green chemistry improvements to the synthesis of (S,S)-reboxetine succinate

(±)-Reboxetine mesylate is a selective norepinephrine uptake (NRI) inhibitor which is marketed as the racemate, under the trade name EdronaxTM, for the treatment of depression, in more than 60 countries. […]

Validation of a HPLC-MS/MS assay for the determination of total and unbound concentration of temocillin in human serum

Validation of a HPLC-MS/MS assay for the determination of total and unbound concentration of temocillin in human serum

Temocillin is a β-lactam antibiotic active against gram-negative bacteria, including β-lactamase producers. It is currently indicated for the treatment of septicemia, urinary tract infections, and lower respiratory tract infections. In […]

Enantioselective Synthesis of Janus Kinase Inhibitor INCB018424 via an Organocatalytic Aza-Michael Reaction

Enantioselective Synthesis of Janus Kinase Inhibitor INCB018424 via an Organocatalytic Aza-Michael Reaction

Janus kinases (JAKs) are crucial signal transducers for a variety of cytokines, growth factors, and interferons. Inhibition of JAKs has advanced the basic and clinical studies of tyrosine kinase inhibitors […]

Peri- and Postnatal Developmental Toxicity of Salcaprozate Sodium (SNAC) in Sprague-Dawley Rats

Peri- and Postnatal Developmental Toxicity of Salcaprozate Sodium (SNAC) in Sprague-Dawley Rats

Salcaprozate sodium (SNAC) (sodium 8-((2-hydroxybenzoyl)amino) octanoate, CAS RN 203787-91-1) is classified as an oral absorption promoter. Although several clinical investigations have explored the potential therapeutic applications of Salcaprozate sodium (SNAC) as […]

Comparison of the Effects of Omapatrilat and Lisinopril on Circulating Neurohormones and Cytokines in Patients With Chronic Heart Failure

Comparison of the Effects of Omapatrilat and Lisinopril on Circulating Neurohormones and Cytokines in Patients With Chronic Heart Failure

A number of endogenous systems exist to counter the effects of vasoconstricting neurohormones that are increased in congestive heart failure (CHF). These include natriuretic peptides, nitric oxide, and prostaglandins. A […]

Labeled oxazaphosphorines for applications in mass spectrometry studies. 2. Synthesis of deuterium-labeled 2-dechloroethylcyclo-phosphamides and 2- and 3-dechloroethylifosfamides

Labeled oxazaphosphorines for applications in mass spectrometry studies. 2. Synthesis of deuterium-labeled 2-dechloroethylcyclo-phosphamides and 2- and 3-dechloroethylifosfamides

The prodrugs cyclophosphamide (CP) and ifosfamide (IF) each metabolize to an active alkylating agent through a cytochrome P450-mediated oxidation at the C-4 position. Competing with this activation pathway are enzymatic […]

Celastrol supports survival of retinal ganglion cells injured by optic nerve crush

Celastrol supports survival of retinal ganglion cells injured by optic nerve crush

Celastrol, a quinine methide triterpene extracted from the perennial vine Tripterygium wilfordii (Celastraceae), has been used in traditional Chinese medicine as a natural remedy for inflammation and a variety of […]