第二部分: Passerini reaction 為三個單元組成之反應，用含硼之酸或醛作為起始 物，於微波反應槽內反應，合成出α-acyloxyl amides 的化合物 (A1-A20,B1-B10)。此此方式進行合成，其操作簡單，且大量縮短反應時間。 另外只需以水做為反應溶劑，不需添加任何路易士酸進行催化，而在純化 上亦只需再沉澱即可得到乾淨的產物，達到綠色化學之裡想。 而後將所得之化合物進行一系列的藥物化學結構與活性關係，找出作 為後續藥物開發的領導藥物。 Part 1 Six of peptidyl boron-containing analogs were designed and successfully synthesized. Their anti-proliferative activities against hepatocellular carcinoma cells (HepG2) and human metastatic breast cancer cells (MDA-MB231) were evaluated by MTT assay. Unfortunately, none of the synthesized analogs were found active against the cancer cell lines. More analogs are being synthesized and the result will be reported in due course.
Part 2 In this report, a Passerini three-component reaction with a boron- containing carboxylic acid or a boron-containing aldehyde in water under microwave irradiation was developed. This methodology allows an efficient formation of a broad range of boron-containing a-acyloxy amides under mild condition in short reaction times. Two series of boron-containing a-acyloxy amides were synthesized and screened by MTT assay, and two potential lead compounds were found to be potent against HepG2 cancer cell.
