在持續尋找維甲酸對HL-60細胞之分化活性之增強劑中，著者合成了數個以??-3-醋酸為先導化合物的類緣物。在測試這些標的化合物對於HL-60細胞的分化及增殖能力後，建立了初步的結構與活性關係。發現大部分的標的化合物能有效的加強維甲酸之作用。其中以化合物1-benzylindole-3-acetamide (4), N-methyl-1- benzylindole-3-acetamide (5), N-ethyl-1-benzylindole-3-acetamide (6), N-n-propyl-1-benzylindole-3-acetamide (7),以及N-methyl-1- benzylindole-3- carboxamide (13)具有最強的協同活性並選擇作進一步的評估。; As part of our continuing search for novel potentiators of the activity of retinoic acid in inducing differentiation of HL-60 cells, I have synthesized several analogs of the lead compound, indole-3-acetic acid. After testing the target compounds on HL-60 cells for differentiation and proliferation capability, a preliminary SAR was established.Most of the target compounds were found to be effective to potentiate the iuduction of different by retinoic acid.Among them, compound 1-benzylindole-3- acetamide (4), N-methyl-1-benzylindole-3-acetamide (5), N-ethyl-1- benzylindole-3-acetamide (6), N-n-propyl-1-benzylindole-3-acetamide (7),and N-methyl-1-benzylindole-3- carboxamide (13)showed most potent synesgistic activity and were selected for further evaluation.
