STRUCTURE-FUNCTION RELATIONSHIP OF YUEHCHUKENE .2. THE EFFECT OF C-6-INDOLE ROTATION ON ANTIIMPLANTATION ACTIVITY

被引：22

作者：

CHENG, KF ^{[1
]}

WONG, TT ^{[1
]}

CHAN, KP ^{[1
]}

KONG, YC ^{[1
]}

机构：

[1] CHINESE UNIV HONG KONG,DEPT BIOCHEM,SHA TIN,HONG KONG

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 27卷 / 02期

关键词：

YUEHCHUKENE (YCK); ANALOG SYNTHESES; ANTI-IMPLANTATION ACTIVITY; STERIC REQUIREMENT;

D O I：

10.1016/0223-5234(92)90100-F

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In a first attempts to define the structural requirements for the expression of anti-implantation activity in Yuehchukene (YCK), it was found that the relative position or planarity of the aromatic centres may be crucial. New synthetic routes leading to analogues with modification of C-7 substituents were established. Results indicated that a bulky group at C-7 that served to restrict the rotation of the C-6 indole was indispensable. Further steric hindrance by 2'-methyl would increase potency in all weak analogues. It was concluded that YCK required an optimal conformation that was defined by a narrowly-fixed angle between the, planes of the C-6 indole and the tetracyclic unit.

引用

页码：121 / 130

页数：10

共 8 条

[1] STRUCTURE-FUNCTION RELATIONSHIP STUDY OF YUEHCHUKENE .1. ANTI-IMPLANTATION AND ESTROGENIC ACTIVITIES OF SUBSTITUTED YUEHCHUKENE DERIVATIVES [J].