[Studies on the synthesis and antitumor activities of howiinol A and its analogues].
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.
Sun
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Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050.
Yu
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D000818:Animals; D029061:Annonaceae / Q000737:chemistry*; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000494:pharmacology; D018922:HL-60 Cells / Q000187:drug effects; D006801:Humans; D007939:Leukemia L1210 / Q000473:pathology; D024301:Plant Bark / Q000737:chemistry; D011753:Pyrones / Q000138:chemical synthesis* / Q000302:isolation & purification / Q000494:pharmacology; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000972:Antineoplastic Agents, Phytogenic; D011753:Pyrones; C426486:howiinol A