Indolo[3,2-c]cinnolines with antiproliferative, antifungal, and antibacterial activity

被引:62
作者
Barraja, P
Diana, P
Lauria, A
Passannanti, A
Almerico, AM
Minnei, C
Longu, S
Congiu, D
Musiu, C
La Colla, P
机构
[1] Univ Studi Cagliari, Dipartimento Biol Sperimentale, Sez Microbiol, I-09124 Cagliari, Italy
[2] Univ Studi Palermo, Ist Farmacochim, I-90123 Palermo, Italy
关键词
polycyclic heterocyclic compounds; antiproliferative agents; antibacterials;
D O I
10.1016/S0968-0896(99)00096-6
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A series of indolo[3,2-c]cinnoline derivatives was prepared and tested to evaluate their biological activity. Most of them inhibited the proliferation of leukemia, lymphoma and solid tumor-derived cell lines at micromolar concentrations, whereas none of the compounds were active against HIV-1. With the exception of 7g, all title compounds showed antibacterial activity against grampositive bacteria, being up to 200 times more potent than the reference drug streptomycin. Some of the indolo[3,2-c]cinnolines were also endowed with good antifungal activity, particularly against Cryptococcus neoformans. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1591 / 1596
页数:6
相关论文
共 8 条
[1]  
Cirrincione G, 1995, FARMACO, V50, P849
[2]  
CIRRINCIONE G, IN PRESS J MED CHEM
[3]   RAPID COLORIMETRIC ASSAY FOR CELL-GROWTH AND SURVIVAL - MODIFICATIONS TO THE TETRAZOLIUM DYE PROCEDURE GIVING IMPROVED SENSITIVITY AND RELIABILITY [J].
DENIZOT, F ;
LANG, R .
JOURNAL OF IMMUNOLOGICAL METHODS, 1986, 89 (02) :271-277
[4]   INTERACTIONS OF ANTITUMOR DRUGS WITH NATURAL DNA - H-1-NMR STUDY OF BINDING MODE AND KINETICS [J].
FEIGON, J ;
DENNY, WA ;
LEUPIN, W ;
KEARNS, DR .
JOURNAL OF MEDICINAL CHEMISTRY, 1984, 27 (04) :450-465
[5]   Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: Novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series [J].
Mai, A ;
Artico, M ;
Sbardella, G ;
Quartarone, S ;
Massa, S ;
Loi, AG ;
DeMontis, A ;
Scintu, F ;
Putzolu, M ;
LaColla, P .
JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (10) :1447-1454
[6]  
MYERS CE, 1990, CANC CHEMOTHERAPY PR, P356
[7]   RAPID AND AUTOMATED TETRAZOLIUM-BASED COLORIMETRIC ASSAY FOR THE DETECTION OF ANTI-HIV COMPOUNDS [J].
PAUWELS, R ;
BALZARINI, J ;
BABA, M ;
SNOECK, R ;
SCHOLS, D ;
HERDEWIJN, P ;
DESMYTER, J ;
DECLERCQ, E .
JOURNAL OF VIROLOGICAL METHODS, 1988, 20 (04) :309-321
[8]  
Wakelin L. P. G., 1990, COMPREHENSIVE MED CH, V2, P703