[reaction: see text] Highly efficient methodology for the construction of functionalized resins was presented involving 1,3-dipolar cycloaddition as the key reaction step. On the basis of this concept, the first series of click backbone amide linkers were synthesized and the application of the FIMT resin 3f to the parallel synthesis of putative dopaminergic agents was demonstrated leading to the selective receptor ligands 10i and 10s revealing high affinity to the D4 subtype.

Fused pyridine derivativesFused pyridine derivatives R 0450 Synthesis and Evaluation of 9-Anilinothiazolo[5,4-b]quinoline Derivatives as Potential Antitumorals. -Five new title derivatives, cf. (III), (VI), (IX), (XI) and (XIII), combining the general substitution pattern of potent antitumoral acridines with a thiazoloquinoline template are prepared and preliminarily evaluated for their antitumoral activity. Compounds (IX), (XI) and (XIII) are synthesized by coupling properly substituted anilines to the novel thiazoloquinoline (VII). All derivatives demonstrate DNA binding in the nanomolar range. Derivative (IX) forms the tightest intercalation complex without correlation to its cytotoxic activity. On the other hand, (VI) forms the weakest and most extensive complexes with DNA being highly cytotoxic. -(RODRIGUEZ-LOAIZA, P.; QUINTERO, A.; RODRIGUEZ-SOTRES, R.; SOLANO, J. D.; LIRA-ROCHA*, A.; Eur.

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