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2000
Volume 13, Issue 7
  • ISSN: 1871-5206
  • E-ISSN: 1875-5992

Abstract

Novel 5,6-disubstituted pyridazin-3(2H)-one derivatives were designed and synthesized as combretastatin A-4 analogues. Our objective was to overcome the spontaneous cis to trans isomerization of the compound. We therefore replaced the cis-double bond with a pyridazine ring. The antiproliferative activity of the novel analogues was evaluated against four human cancer cell lines (HL-60, MDAMB- 435, SF-295 and HCT-8). We found that the analogues had little activity either against selected cell lines or against purified tubulin. Molecular modeling studies may account for their inactivity.

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/content/journals/acamc/10.2174/1871520611313070018
2013-09-01
2025-05-07
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