RELATIONSHIP OF HYPOLIPIDEMIC AND ANTINEOPLASTIC ACTIVITIES OF TRICYCLOHEXYLPHOSPHINE AND TRIPHENYLPHOSPHINE BORANES, CARBOXYBORANES, CYANOBORANES, AND RELATED DERIVATIVES

被引:32
作者
DAS, MK
MAITI, PK
ROY, S
MITTAKANTI, M
MORSE, KW
HALL, IH
机构
[1] UTAH STATE UNIV,DEPT CHEM & BIOCHEM,LOGAN,UT 84322
[2] UNIV N CAROLINA,SCH PHARM,DIV MED CHEM & NAT PROD,CHAPEL HILL,NC 27599
关键词
D O I
10.1002/ardp.19923250504
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of tricyclohexyl- and triphenylphosphine boranes, carboxyboranes and cyanoboranes were synthesized. These compounds have potent hypolipidemic effects, antineoplastic and antiinflammatory activities in rodents. Furthermore, they demonstrated potent cyctotoxicity against standard human tissue culture lines. The compounds which afforded the best hypolipidemic activity, i.e. greater than 40% reduction of serum cholesterol and triglyceride levels, were diphenyl-(4-methylphenyl)-phosphine borane and triphenylphosphine carboxyborane. Other derivatives demonstrated more potent antineoplastic activity against the Ehrlich ascites carcinoma growth including triphenylphosphine cyanoborane, 2-amino-4-methyl-pyridine cyanoborane and 2-amino-pyridine cyanoborane. Most of the derivatives showed good activity against murine L1210 lymphoid leukemia, Tmolt3 human leukemia, uterine HeLa(S) cells, and human glioma cell growth. Select compounds were active against colon adenocarcinoma, KB nasopharynx, lung bronchogenic and osteosarcoma cell growth. Tricyclohexyl- and triphenylphosphine boranes and the carboxy derivatives of the latter borane demonstrated good antiinflammatory activity.
引用
收藏
页码:267 / 272
页数:6
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