The enone motif of (+)-grandifloracin is not essential for 'anti-austerity' antiproliferative activity.

نویسندگان

  • Monika Ali Khan
  • Pauline J Wood
  • Natasha M Lamb-Guhren
  • Lorenzo Caggiano
  • Gabriele Kociok-Köhn
  • David Tosh
  • Simon E Lewis
چکیده

We report the synthesis and biological evaluation of three analogues of the natural product (+)-grandifloracin (+)-1. All three analogues exhibit enhanced antiproliferative activity against PANC-1 and HT-29 cells compared to the natural product. The retention of activity in an analogue lacking the enone functional group, 9, implies this structural element is not an essential part of the (+)-grandifloracin pharmacophore.

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عنوان ژورنال:
  • Bioorganic & medicinal chemistry letters

دوره 24 13  شماره 

صفحات  -

تاریخ انتشار 2014