SYNTHESIS AND EVALUATION OF 1-(HYDROXYPHENYL)-1-NONEN-3-ONES AND RELATED COMPOUNDS FOR ANTI-NEOPLASTIC AND ANTI-MICROBIAL ACTIVITIES

被引:23
作者
DIMMOCK, JR [1 ]
NYATHI, CB [1 ]
SMITH, PJ [1 ]
机构
[1] UNIV SASKATCHEWAN, DEPT CHEM & CHEM ENGN, SASKATOON S7N 0W0, SASKATCHEWAN, CANADA
关键词
1‐Phenyl‐1‐nonen‐3‐one derivatives—synthesized; evaluated for antineoplastic and antimicrobial activities; Antimicrobial activity—various 1‐phenyl‐1‐nonen‐3‐one derivatives evaluated in vitro; Antineoplastic activity—various 1‐phenyl‐1‐nonen‐3‐one derivatives evaluated in mice; Structure‐activity relationships—various 1‐phenyl‐1‐nonen‐3‐one derivatives evaluated for antineoplastic activity in mice and antimicrobial activity in vitro;
D O I
10.1002/jps.2600671113
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Some 1‐(hydroxyphenyl)‐1‐nonen‐3‐ones, the corresponding Mannich bases, and O‐benzoyl esters were synthesized. Evaluation of these derivatives against murine P‐388 lymphocytic leukemia indicated that, while the hydroxyphenyl styryl ketones and related esters were devoid of significant anticancer activities, etherification of the nuclear hydroxyl group gave compounds with a discernible increase in mean survival time. The hydroxyphenyl styryl ketones showed marked potencies against two pathogenic fungi and one yeast, while the corresponding ethers had diminished activities and the related esters were virtually devoid of antimicrobial activities. Two Mannich bases showed similar spectra of antimicrobial activities as the phenols and, in particular, were active against Trichophyton mentagrophytes and Saccharomyces uvarum. Copyright © 1978 Wiley‐Liss, Inc., A Wiley Company
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页码:1543 / 1546
页数:4
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