Chemical and Pharmaceutical Bulletin p. 818 - 828 (1995)
Update date:2022-07-30
Topics:
Ohsumi
Ohishi
Morinaga
Nakagawa
Suga
Sekiyama
Akiyama
Tsuji
Tsuruo
New N-alkylated 1,4-dihydropyridine derivatives were synthesized and their ability to overcome multidrug resistance was examined in vincristine-resistant P388 cells (P388/VCR cells). Compounds that possessed an arylalkyl substituent on the dihydropyridine ring nitrogen were more potent than verapamil in potentiating the cytotoxicity of vincristine against P388/VCR cells. However, neither drug effectively enhanced the antitumor activity of vincristine in tumor-bearing mice. Introduction of basic nitrogen-containing substituents on the side chain of 1,4-dihydropyridines gave improved activity in vitro and in vivo. The piperazine derivative 12c and 12o were more than 10 times as potent as verapamil in vitro. Four compounds selected for in vivo testing showed superior antitumor activity in P388/VCR-bearing mice in combination with vincristine. The structure-activity relationships of the compounds are discussed.
View MoreShenzhen Sungening Medicine Co., Ltd
Contact:+86-871-65110906
Address:Room702, Building 2, 365 Dianchi Road, Kunming, Yunnan Province, P.R. China
Contact:+86-371-55981030
Address:Room 1571, Macalline Soho, No.1, Shangdu Road, Zhengzhou, Henan
Shanghai Massive Chemical Technology Co., Ltd.
website:http://www.massivechem.com/
Contact:+86 21 34943721
Address:Room 435, 4th floor, Building 9, No. 2568 Gudai Road,Minhang District, Shanghai,
Nanjing Qirui Material Co., Ltd.
Contact:+86-25-52320053
Address:F4-5, #17 Building, Chuang Yi Yuan, No.6 Guanghua East Street, Nanjing, 210007 P.R.China
Shandong Topscience Biotech Co., Ltd.
Contact:0633-2619278
Address:No. 98 Lanshan West Road, Lanshan District, Rizhao, Shandong Province, P.R. of China
Doi:10.1021/jm980567e
(1999)Doi:10.1021/ol800109s
(2008)Doi:10.1055/s-2008-1032086
(2008)Doi:10.1016/S0040-4039(01)80890-X
(1985)Doi:10.1002/adsc.201600786
(2017)Doi:10.1021/ol034471c
(2003)
