New 5-ylidene rhodanine derivatives based on the dispacamide A model

Mol Divers. 2014 May;18(2):375-88. doi: 10.1007/s11030-014-9509-7. Epub 2014 Mar 2.

Abstract

A practical approach for the preparation of (5Z) 5-ylidene rhodanine derivatives bearing the (4,5-dihalogeno-pyrrol-2-yl)carbamoyl fragment of dispacamide A is reported. The new compounds were obtained in good yields (19-88 %) by Knoevenagel condensation according to a solution-phase microwave dielectric heating protocol in the presence of organic bases (piperidine, TEA, and AcONa) from a set of N-substituted rhodanines 2(a-i). The ten synthetic products 3(a-j) have been synthesized with a Z-geometry about their exocyclic double bond and the structure of one of these compounds (3) was confirmed by a single X-ray diffraction analysis. The new (5Z) 5-ylidene rhodanine derivatives 3(a-j) were tested against eight protein kinases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chemistry Techniques, Synthetic
  • Protein Kinase Inhibitors / chemical synthesis*
  • Protein Kinase Inhibitors / chemistry*
  • Pyrroles / chemistry*
  • Rhodanine / analogs & derivatives*
  • Rhodanine / chemical synthesis*
  • Rhodanine / chemistry*

Substances

  • Protein Kinase Inhibitors
  • Pyrroles
  • Rhodanine