Sun S, Yu D
Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050.
Yao Xue Xue Bao. 1998 Jul;33(7):502-11.
Howiinol A(1), one of the active antitumor constituents from the root and stem bark of Goniothamus howii Meer. (Annonaceae) has been synthesized in nine steps from alpha-D-glucoheptonic gamma-lactone with an over all yield of 13.3%. It shows that all data of the synthetic product are identical to those of the natural howiinol A, thus the absolute configuration of natural howiinol A is further confirmed as 1. In the search for new antitumor compounds with high potency, 26 analogues have been synthesized. In pharmacological tests most of them showed antitumor activities in vitro, some of them are significant.
厚壳桂醇A(1)是厚壳桂（番荔枝科）根和茎皮中的活性抗肿瘤成分之一，已由α-D-葡庚糖酸γ-内酯经九步合成，总产率为13.3%。结果表明，合成产物的所有数据与天然厚壳桂醇A的数据一致，从而进一步确认天然厚壳桂醇A的绝对构型为1。在寻找高效新抗肿瘤化合物的过程中，已合成了26个类似物。药理试验表明，其中大多数在体外具有抗肿瘤活性，有些活性显著。
