USNIC ACID-DERIVATIVES AS POTENTIAL ANTI-NEOPLASTIC AGENTS

被引：105

作者：

TAKAI, M ^{[1
]}

UEHARA, Y ^{[1
]}

BEISLER, JA ^{[1
]}

机构：

[1] NCI, DIV CANC TREATMENT, MED CHEM & BIOL LAB, BETHESDA, MD 20014 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1979年 / 22卷 / 11期

关键词：

D O I：

10.1021/jm00197a019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Usnic acid, a lichen antibiotic, showed low-level activity in the Lewis lung carcinoma test system. In an effort to produce new agents of potential use in the treatment of lung cancer, derivatives of the natural product were synthesized and evaluated with a cytotoxicity assay. Structure-activity analysis of the cytotoxicity data indicated the importance of the lipophilicity and the ²-triketone moiety of usnic acid on cytotoxicity. No significant increases in survival of test animals over controls were shown by any of the synthetic compounds in the P388 leukemia or the Lewis lung carcinoma test systems. © 1979, American Chemical Society. All rights reserved.

引用

页码：1380 / 1384

页数：5

共 25 条

[1]

ASAHINA Y, 1938, CHEM BER, V71, P2260

[2]

ASAHINA Y, 1939, CHEM BER, V72, P1140

[3]

ASAHINA Y, 1937, CHEM BER, V70, P2462

[4] SOME OBSERVATIONS ON THE CONSTITUTION OF USNIC ACID [J].

BARTON, DHR ;

BRUUN, T .

JOURNAL OF THE CHEMICAL SOCIETY, 1953, (FEB) :603-609

[5] SYNTHESIS AND ANTI-TUMOR ACTIVITY OF DIHYDRO-5-AZACYTIDINE, A HYDROLYTICALLY STABLE ANALOG OF 5-AZACYTIDINE [J].

BEISLER, JA ;

ABBASI, MM ;

KELLEY, JA ;

DRISCOLL, JS .

JOURNAL OF MEDICINAL CHEMISTRY, 1977, 20 (06) :806-812

[6] METHYLATION AND RACEMISATION STUDIES ON USNIC ACID [J].

BERTILSSON, L ;

WACHTMEISTER, CA .

ACTA CHEMICA SCANDINAVICA, 1968, 22 (06) :1791-+

[7]

CONCHIE J, 1963, METHODS CARBOHYDRATE, V2, P332

[8] SPECTROSCOPIC STUDIES ON ENOLS .4. HYDROGEN BONDING IN USNIC ACID [J].

FORSEN, S ;

WACHTMEISTER, CA ;

NILSSON, M .

ACTA CHEMICA SCANDINAVICA, 1962, 16 (03) :583-&

[9]

GERAN RI, 1972, CANC CHEMOTHER REP, V3, P1

[10]

HALL LD, 1964, ADV CARBOHYD CHEM, V19, P51

← 1 2 3 →