Synthesis, biological evaluation, and modeling of dimeric PPI analogues as novel DNA minor groove binders.

Semi-automatic synthesis, antiproliferative activity and DNA-binding properties of new netropsin and bis-netropsin analogues.

A general route for the semi-automatic synthesis of some new potential minor groove binders was established. Six four-numbered sub-libraries of new netropsin and bis-netropsin analogues have been synthesized using a Syncore Reactor. The structures of the all new substances prepared in this investigation were fully characterized by NMR ((1)H, (13)C), HPLC and LC-MS. The antiproliferative activit...

The Analogues of DNA Minor-Groove Binders as Antineoplastic Compounds

Minor Groove of DNA as Target for Drug Design

Small minor groove binding molecules have been found to influence DNA-dependent processes. Their affinity is high enough to prevent transcription factors from interaction with the DNA. Some of the minor groove binders can be even designed to target only specific DNA sequences. Thereby, they are able to influence transcription, which provides the possibility to systematically regulate the synthe...

Novel Linezolid like Analogues: Synthesis, Characterization and Biological Evaluation

The synthesis of 4-(substituted benzylidene)-2-(pyrazin-2-yl) oxazol-5(4H)-one was achieved in two steps, In first step, pyrazine-2-carboxamide  dissolved in EtOH, 10% KOH solution with ClCH2COOH produced compound 2-(pyrazine-2-carboxamido) acetic acid (II) and in second step, compound (II) in (CH3CO)2O with aromatic aldehyde, and catalyst potassium ace...

Design, Synthesis and Biological Evaluation of Novel Peptide-Like Analogues as Selective COX-2 Inhibitors

A new series of peptide-like derivatives containing different aromatic amino acids andpossessing pharmacophores of COX-2 inhibitors as SO2Me or N3 attached to the para positionof an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2)inhibitors. The synthetic reactions were based on the solid phase peptide synthesis methodusing Wang resin. One of the analogues, i...