STUDIES ON STEROIDS .54. RELATIONSHIP BETWEEN CHEMICAL-STRUCTURE AND ANTI-TUMOR ACTIVITY OF WITHAFERIN A ANALOGS

被引：23

作者：

YOSHIDA, M ^{[1
]}

HOSHI, A ^{[1
]}

KURETANI, K ^{[1
]}

ISHIGURO, M ^{[1
]}

IKEKAWA, N ^{[1
]}

机构：

[1] TOKYO INST TECHNOL,CHEM NAT PROD LAB,MIDORI KU,YOKOHAMA 227,JAPAN

来源：

JOURNAL OF PHARMACOBIO-DYNAMICS | 1979年 / 2卷 / 02期

关键词：

AB ring analogue of withaferin A; antitumor activity; leukemia L5178Y; ring opening of epoxide; withaferin A; withanolide;

D O I：

10.1248/bpb1978.2.92

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The relationship between chemical structure and antitumor activity of AB ring analogues of withaferin A was examined by cell growth inhibition in mouse leukemia L5178Y cells in vitro. The 5, 6β-epoxy-4β-ol (5) and 5, 6α-epoxy-4α-ol (6) with 1-keto-2-ene function and cholesterol side chain have antitumor activity. The 4, 5-epoxy-6-hydroxyl compounds (9-16) were found to be equally or more active than corresponding 5, 6-epoxy-4-hydroxyl analogues. The antitumor activities of the 4, 5-epoxides paralleled the reactivities in ring opening reaction with acid. For the antitumor activity of withanolides, the unsaturated lactone in the side chain is important, and 1-keto-2-ene and epoxide functions were essential to elicit the activity. © 1979, The Pharmaceutical Society of Japan. All rights reserved.

引用

页码：92 / 97

页数：6

共 14 条

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