Synthesis and biological evaluation of structurally diverse α-conformationally restricted chalcones and related analogues

Cyclic chalcones and structural analogues evaluated as cytotoxic agents.

Tailored therapeutics based on 1,2,3-1H-triazoles: a mini review

Contemporary drug discovery approaches rely on library synthesis coupled with combinatorial methods and high-throughput screening to identify leads.

Synthesis and antitumor activity of fluorouracil – oleanolic acid/ursolic acid/glycyrrhetinic acid conjugates

Due to the obvious adverse effects of 5-fluorouracil and considering the diverse biological activities of pentacyclic triterpenes, twelve pentacyclic triterpene-5-fluorouracil conjugates were synthesized and their antitumor activities were evaluated.

Synthesis of N-acyl amide natural products using a versatile adenylating biocatalyst

TamA is the enzyme that controls the acyl chain length of the tambjamine natural products. Here we show that the catalytic ANL domain of TamA can be used to prepare a range of N-acyl amides.

Synthesis, conformational preferences, and biological activity of conformational analogues of the microtubule-stabilizing agents, (−)-zampanolide and (−)-dactylolide

Zampanolide and dactylolide are microtubule-stabilizing polyketides possessing potent cytotoxicity towards a variety of cancer cell lines.

Design, synthesis and biological evaluation of tryptamine salicylic acid derivatives as potential antitumor agents

According to the combination principle, target compounds were designed, and compound E20 might be a promising anti-tumor agent targeting gastric cancer.

Targeted metabolomics approach for identification of relapsing–remitting multiple sclerosis markers and evaluation of diagnostic models

Relapsing–remitting multiple sclerosis markers determined (a) and multivariate models for early diagnosis were evaluated (b).

Aurantiamide-related dipeptide derivatives are formyl peptide receptor 1 antagonists

Aurantiamide is a useful scaffold to develop promising FPR1 antagonists capable of inhibiting neutrophil chemotaxis.

Synthesis of DNA-coupled isoquinolones and pyrrolidines by solid phase ytterbium- and silver-mediated imine chemistry

A solid phase-based strategy gave access to DNA-tagged heterocycles by metal-mediated imine chemistry, exemplified by Cushman- and 1,3-dipolar cycloaddition reactions.

Synthesis of an α-phosphono-α,α-difluoroacetamide analogue of the diphosphoinositol pentakisphosphate 5-InsP7

A synthetic, fluorinated analogue of 5-InsP7binds to the kinase domain of PPIP5K2, suggesting new strategies for designing diphosphoinositol phosphate mimics.