ANTITUMOR AGENTS .5. SYNTHESIS AND ANTILEUKEMIC ACTIVITY OF E-RING-MODIFIED (RS)-CAMPTOTHECIN ANALOGS

被引:24
作者
EJIMA, A
TERASAWA, H
SUGIMORI, M
OHSUKI, S
MATSUMOTO, K
KAWATO, Y
YASUOKA, M
TAGAWA, H
机构
[1] Exploratory Research Laboratories I, Daiichi Pharmaceutical Co., Ltd., Tokyo 134, 16–13, Kitakasai 1-chome, Edogawa-ku
关键词
CAMPTOTHECIN; AMINOCAMPTOTHECIN; FRIEDLANDER CONDENSATION; ANTITUMOR ACTIVITY;
D O I
10.1248/cpb.40.683
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Several E-ring-modified analogues of (RS)-camptothecin were synthesis via Friedlander condensation and evaluated for cytotoxicity and antitumor activity against P388 mouse leukemia cells. Among them, (RS)-20-deoxyamino-7-ethyl-10-methoxycamptothecin (25c) was found to be more active than (RS)-camptothecin (1) in the in vivo assay.
引用
收藏
页码:683 / 688
页数:6
相关论文
共 15 条
  • [1] BORSCHE W, 1943, CHEM BER, V76, P1099
  • [2] EIJMA A, 1989, CHEM PHARM BULL, V37, P2253
  • [3] ANTITUMOR AGENTS .1. ASYMMETRIC-SYNTHESIS OF (S)-CAMPTOTHECIN
    EJIMA, A
    TERASAWA, H
    SUGIMORI, M
    TAGAWA, H
    [J]. TETRAHEDRON LETTERS, 1989, 30 (20) : 2639 - 2640
  • [4] ANTITUMOUR AGENTS .2. ASYMMETRIC-SYNTHESIS OF (S)-CAMPTOTHECIN
    EJIMA, A
    TERASAWA, H
    SUGIMORI, M
    TAGAWA, H
    [J]. JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1990, (01): : 27 - 31
  • [5] PHOTOINDUCED NUCLEOPHILIC SUBSTITUTION OF 3-SUBSTITUTED 2,1-BENZISOXAZOLES (IN RING OPENING)
    GIOVANNINI, E
    ROSALES, J
    SOUZA, BD
    [J]. HELVETICA CHIMICA ACTA, 1971, 54 (07) : 2111 - +
  • [6] UBER DIE KONSTITUTION DES ARICINS
    GOUTAREL, R
    JANOT, MM
    LEHIR, A
    CORRODI, H
    PRELOG, V
    [J]. HELVETICA CHIMICA ACTA, 1954, 37 (06) : 1805 - 1814
  • [7] KINGSBURY MD, 1991, J MED CHEM, V34, P98
  • [8] SAWADA S, 1991, CHEM PHARM BULL, V39, P2574
  • [9] SAWADA S, 1991, CHEM PHARM BULL, V39, P1446
  • [10] CAMPTOTHECIN
    SCHULTZ, AG
    [J]. CHEMICAL REVIEWS, 1973, 73 (04) : 385 - 405