Synthesis of Analogues of NSC73306 to Circumvent Multidrug Resistance in Cancer

最近，在一名暑期学生（李家阳）的帮助下，我根据我们第一批的经验和中间体的商业可用性，合成了另外23种化合物。经过一番努力，终于制备出了对二甲胺取代衍生物，并如预期的那样，发现其可溶于稀酸，但由于样品的碱性较弱，在进一步稀释样品进行测试时，产生了沉淀。因此，一种涉及碱性强得多的对二甲氨基甲基衍生物的新合成方法被开发出来，其合成已接近完成。

More recently with the help of a summer student (Jiayang Li), I have synthesized an additional twenty-three compounds based on our experiences with the first set and the commercial availability of intermediates. The p-dimethylamino substituted derivative was finally prepared after much labor and, as expected, found to be soluble in dilute acid, but as the sample was diluted even further for testing, precipitation occurred due to its weak basicity. Therefore a new synthesis involving the much more strongly basic p-dimethylaminomethyl derivative was developed and its synthesis is nearing completion. I also continue to examine the structures of related proteins in the GFP series by digestion and LC/MS (J.-R. Gillet). The synthesized compounds are being tested for its selectivity in killing cancer cells. In particular, cancel cells that are showing multidrug-resistance.