Bioisosteres of the phenyl ring: recent strategic applications in lead optimization and drug design
MAM Subbaiah, NA Meanwell - Journal of Medicinal Chemistry, 2021 - ACS Publications
The benzene moiety is the most prevalent ring system in marketed drugs, underscoring its
historic popularity in drug design either as a pharmacophore or as a scaffold that projects …
historic popularity in drug design either as a pharmacophore or as a scaffold that projects …
Nanomedicine for increasing the oral bioavailability of cancer treatments
Oral administration is an appealing route of delivering cancer treatments. However, the
gastrointestinal tract is characterized by specific and efficient physical, chemical, and …
gastrointestinal tract is characterized by specific and efficient physical, chemical, and …
[HTML][HTML] Trends in oral small-molecule drug discovery and product development based on product launches before and after the Rule of Five
S Stegemann, C Moreton, S Svanbäck, K Box… - Drug Discovery …, 2023 - Elsevier
Highlights•Orally delivered drug products gradually continue to exceed the Rule-of-five on
Molecular Weight and clogP.•New predictive descriptors and tools, advanced chemistry and …
Molecular Weight and clogP.•New predictive descriptors and tools, advanced chemistry and …
Drug-drug interactions that alter the exposure of glucuronidated drugs: Scope, UDP-glucuronosyltransferase (UGT) enzyme selectivity, mechanisms (inhibition and …
Drug-drug interactions (DDIs) arising from the perturbation of drug metabolising enzyme
activities represent both a clinical problem and a potential economic loss for the …
activities represent both a clinical problem and a potential economic loss for the …
Supporting gut health with medicinal cannabis in people with advanced cancer: potential benefits and challenges
HR Wardill, LT Wooley, OM Bellas, K Cao… - British Journal of …, 2024 - nature.com
The side effects of cancer therapy continue to cause significant health and cost burden to the
patient, their friends and family, and governments. A major barrier in the way in which these …
patient, their friends and family, and governments. A major barrier in the way in which these …
Inhibition of human UDP-glucuronosyltransferase enzymes by lapatinib, pazopanib, regorafenib and sorafenib: implications for hyperbilirubinemia
Kinase inhibitors (KIs) are a rapidly expanding class of drugs used primarily for the treatment
of cancer. Data relating to the inhibition of UDP-glucuronosyltransferase (UGT) enzymes by …
of cancer. Data relating to the inhibition of UDP-glucuronosyltransferase (UGT) enzymes by …
Electronic medical record‐integrated pharmacogenomics and related clinical decision support concepts
PJ Caraballo, SJ Bielinski, JL St. Sauver… - Clinical …, 2017 - Wiley Online Library
Advances in pharmacogenomics (PGx) have the potential to transform healthcare by
allowing precision medicine to become a reality. However, PGx knowledge is new, complex …
allowing precision medicine to become a reality. However, PGx knowledge is new, complex …
CORAL: Monte Carlo based global QSAR modelling of Bruton tyrosine kinase inhibitors using hybrid descriptors
Global QSAR modelling was performed to predict the pIC50 values of 233 diverse
heterocyclic compounds as BTK inhibitors with the Monte Carlo algorithm of CORAL …
heterocyclic compounds as BTK inhibitors with the Monte Carlo algorithm of CORAL …
Role of extracellular vesicles in the pathophysiology, diagnosis and tracking of non-alcoholic fatty liver disease
Non-alcoholic fatty liver disease (NAFLD) is the most common chronic liver disease,
affecting approximately one-third of the global population. Most affected individuals …
affecting approximately one-third of the global population. Most affected individuals …
Solid lipid nanoparticles for efficient oral delivery of tyrosine kinase inhibitors: a nano targeted cancer drug delivery
S Satapathy, CS Patro - Advanced pharmaceutical bulletin, 2021 - pmc.ncbi.nlm.nih.gov
Tyrosine kinase inhibitors (TKIs) are used as targeted therapy for cancer by inhibiting the
signaling pathway and tumor growth. Many TKIs got approved by FDA in recent times for the …
signaling pathway and tumor growth. Many TKIs got approved by FDA in recent times for the …