肿瘤的化学治疗——ⅩⅩⅩⅤ.若干植物生长控制剂的衍生物的合成及其抗肿瘤作用

鉴于作者过去曾报道植物生长控制剂与肿瘤细胞的关系及其一些特点,合成了一系列带有强烈生物作用化合物为载体的植物生长控制剂衍生物(Ⅺ_a-d,Ⅻ_a-f,Ⅻ_a-e)和羟基萘乙酸(ⅩⅣ_a-l)羟基萘氧乙酸(ⅩⅤ_a-g)等化合物。药理试验结果Ⅺ_a,Ⅻ_s,b,Ⅻ_a,ⅩⅣ_f,h对肉瘤180或肉瘤37均有明显的抑制作用,其中化合物Ⅺ_a(代号AT-236)已作了初步临床试验,深入工作尚在进行中。

Tumour chemotherapy. XXXV. Syntheses of derivatives of some plant growth regulators and their antitumour activity (author's transl)

In continuation of our investigations of syntheses of derivatives of plant growth regulators for screening antitumour agents we report in this article the syntheses of the following series of compound, namely, the derivatives of naphthalene acetic acids and naphthalene glycolic acids both with a hydroxy substituent in the various positions of the aromatic rings, and the derivatives of some well known plant growth regulators carried by biologically active compound. The synthetic compounds have all been subjected to experimental antitumour tests. Preliminary results showed that Ⅺ_a. Ⅻ_a,b, ⅫⅠ_a and ⅪⅤ_f,h to be much stronger inhibitors against Sarcoma 180 or Sarcoma 37. Compound Ⅺ_a (designated as AT-236) has been submitted to clinical trials. Further research works are in progress.