BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis, and biological evaluation of novel pyrrolo[1,2-a]pyrazine derivatives.

Synthesis and evaluation of a novel quinoline-triazole analogs for antitubercular properties via molecular hybridization approach.

Design, synthesis, evaluation and molecular modeling study of 4-N-phenylaminoquinolines for Alzheimer disease treatment.

Triazolopyrimidine and triazolopyridine scaffolds as TDP2 inhibitors.

Discovery of novel 2,3-dihydro-1H-inden-1-amine derivatives as selective monoamine oxidase B inhibitors.

Design, synthesis and biological evaluation of benzimidazole derivatives as novel human Pin1 inhibitors.

Essential ingredients for rational drug design.

Peptides conjugated to 2-alkoxy-8-oxo-adenine as potential synthetic vaccines triggering TLR7.

Novel M4 positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands.

Synthesis and in vitro activity of asymmetric indole-based bisamidine compounds against Gram-positive and Gram-negative pathogens.

Discovery of small molecule inhibitors of human uridine-cytidine kinase 2 by high-throughput screening.

Biotinylated-spiperone ligands for quantum dot labeling of the dopamine D2 receptor in live cell cultures.

19-Hydroxyeicosatetraenoic acid analogs: Antagonism of 20-hydroxyeicosatetraenoic acid-induced vascular sensitization and hypertension.

Diarylcarbonates are a new class of deubiquitinating enzyme inhibitor.

Structure-based design, synthesis and biological evaluation of a novel series of isoquinolone and pyrazolo[4,3-c]pyridine inhibitors of fascin 1 as potential anti-metastatic agents

Structure-based design and discovery of potent and selective lysine-specific demethylase 1 (LSD1) inhibitors.

Synthesis and antitumor activity of daunorubicin conjugates with of 3,4-methylendioxybenzaldehyde.

Synthesis and antileishmanial evaluation of thiazole orange analogs.

Incorporation of privileged structures into 3-O-β-chacotriosyl ursolic acid can enhance inhibiting the entry of the H5N1 virus.

Novel sulfonamides against Botrytis cinerea with no positive cross-resistance to commercial fungicides: Design, synthesis and SAR study.

Evaluation of quinoxaline compounds as ligands of a site adjacent to S2 (AS2) of cruzain.

Upregulation of p53 through induction of MDM2 degradation: Amino acid prodrugs of anthraquinone analogs.

2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.

Discovery and optimization of covalent Bcl-xL antagonists.

Microwave-assisted synthesis and in vitro stability of N-benzylamide non-steroidal anti-inflammatory drug conjugates for CNS delivery.

Functional expression of a highly-reducing polyketide synthase of Emericella variecolor IFM42010, an asteltoxin-producing strain, resulted in production of two polyenoic β-ketolactones with opposite stereochemistry.

Chemically synthesized LYRM03 could inhibit the metastasis of human breast cancer MDA-MB-231 cells in vitro and in vivo.

Synthesis, fungicidal activity and SAR of 3,4-dichloroisothiazole-based cycloalkylsulfonamides.

Serendipitous discovery of aryl boronic acids as β-lactamase inhibitors.

Prodrugs of the cancer cell selective anti-cancer agent (Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)acrylonitrile (A131) are orally efficacious in a mouse model of resistant colon cancer.

Synthesis and biological evaluation of 3-amino-, 3-alkoxy- and 3-aryloxy-6-(hetero)arylpyridazines as potent antitumor agents.

Identification of BR101549 as a lead candidate of non-TZD PPARγ agonist for the treatment of type 2 diabetes: Proof-of-concept evaluation and SAR.

Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927.

Discovery of 1,8-disubstituted-[1,2,3]triazolo[4,5-c]quinoline derivatives as a new class of Hippo signaling pathway inhibitors.

Further exploration of the structure-activity relationship of imidazoquinolines; identification of potent C7-substituted imidazoquinolines.

Structure-based design of guanosine analogue inhibitors targeting GTP cyclohydrolase IB towards a new class of antibiotics.

Synthesis and evaluation of thieno[3,2-d]pyrimidine derivatives as novel FMS inhibitors.

Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M4 positive allosteric modulator (PAM) chemotype.

SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs.

Design, synthesis and biological evaluation of mogrol derivatives as a novel class of AMPKα2β1γ1 activators.

Development of the binding molecules for the RNA higher-order structures based on the guanine-recognition by the G-clamp.

Synthesis of 2-arylhydrazinylidene-3-oxo-4,4,4-trifluorobutanoic acids as new selective carboxylesterase inhibitors and radical scavengers.

Synthesis and biological evaluation of Vinpocetine derivatives.

Facile synthesis of carbon-11-labeled sEH/PDE4 dual inhibitors as new potential PET agents for imaging of sEH/PDE4 enzymes in neuroinflammation.

Targeting TRAIL.

Synthesis and antitumor activity of bis(arylsulfonyl)dihydroimidazolinone derivatives.

The role of N-terminal heterocycles in hydrogen bonding to α-chymotrypsin.