Design, synthesis and biological activity of a pyrrolo[2,1-c][1,4]benzodiazepine (PBD)-distamycin hybrid

被引:32
作者
Baraldi, PG [1 ]
Cacciari, B
Guiotto, A
Leoni, A
Romagnoli, R
Spalluto, G
Mongelli, N
Howard, PW
Thurston, DE
Bianchi, N
Gambari, R
机构
[1] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy
[2] Pharmacia & Upjohn Inc, Oncol, Preclin Res, Milan, Italy
[3] Portsmouth Polytech, Sch Pharm & Biomed Sci, CRC, Gene Targeted Drug Design Res Grp, Portsmouth PO1 2DT, Hants, England
[4] Univ Ferrara, Dipartmento Biochim & Biol Mol, I-44100 Ferrara, Italy
关键词
D O I
10.1016/S0960-894X(98)00544-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
We report the synthesis of a new hybrid 13 which is a combination of the naturally occurring antitumor agent distamycin A 1 and the pyrrolo[2,1-c][1,4]benzodiazepine 11, related to the naturally occurring anthramycin 2. The antitumor activity of the hybrid 13 was tested in vitro and compared to the natural product distamycin 1 and the PBD 11. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:3019 / 3024
页数:6
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