BOC Sciences Blog

Design and discovery of 3-aryl-5-substituted-isoquinolin-1-ones as potent tankyrase inhibitors

Design and discovery of 3-aryl-5-substituted-isoquinolin-1-ones as potent tankyrase inhibitors

The ADP-ribosyltranferase diphtheria toxin-like (ARTD) or poly-ADP-ribose polymerase (PARP) protein superfamily comprises 17 proteins that contain a common catalytic domain. Those that are catalytically active use β-NAD+ as an essential […]

HPLC-DAD-MSn analysis and HPLC quantitation of chemical constituents in the traditional Chinese medicine formula Ya-tong-yi-li-wan

HPLC-DAD-MSn analysis and HPLC quantitation of chemical constituents in the traditional Chinese medicine formula Ya-tong-yi-li-wan

Ya-tong-yi-li-wan (YTYLW) is a well-known traditional Chinese medicine (TCM) formula composed of ChanSu (toad venom), licorice root, realgar, and cinnabaris in the ratio of 24 : 24 : 6 : […]

Recent advances in the synthesis of new glycopeptide antibiotics

Recent advances in the synthesis of new glycopeptide antibiotics

  Semi-synthetic glycopeptide antibiotics   Oritavancin, telavancin and dalbavancin   Early studies by Nagarajan et al. into the development of semi-synthetic glycopeptide antibiotics focused on utilizing vancomycin as a structural […]

Optimized Rhodamine B labeled mesoporous silica nanoparticles as fluorescent scaffolds for the immobilization of photosensitizers: a theranostic platform for optical imaging and photodynamic therapy

Optimized Rhodamine B labeled mesoporous silica nanoparticles as fluorescent scaffolds for the immobilization of photosensitizers: a theranostic platform for optical imaging and photodynamic therapy

Nanomaterials with easy surface functionalization and high biocompatibility have emerged as good candidates for theranostic applications. In particular the integration of multiple smart functions such as contrast agents (CA) and […]

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 […]