Journal of Medicinal Chemistry p. 234 - 240 (1995)
Update date:2022-09-26
Topics:
Houlihan, William J.
Munder, Paul G.
Handley, Dean A.
Cheon, Seung H.
Parrino, Vincent A.
A series of 5-aryl-2,3-dihydroimidazo<2,1-a>isoquinolines previously reported to be platelet activating factor (PAF) receptor antagonist were evaluated for potential antitumor activity.Several compounds, such as the 5-(4'-tert-butylphenyl) (65), 5-<4'-(trimethylsilyl)phenyl> (69), and 5-(4'-cyclohexylphenyl) (71) analogs showed very good cytotoxicity against several tumor cell lines. 5-<4'-(Piperidinomethyl)phenyl>-2,3-dihydroimidazo<2,1-a>isoquinoline (SDZ 62-434, 53) was more effective on a milligram per kilogram basis than the clinical cytostatic agent edelfosine (1) in increasing survivors and decreasing tumor volume in the oral mouse Meth A fibrosarcoma assay.It was selected for further development and is currently in phase I clinical trials in cancer patients.
View MoreNINGBO PANGS CHEM INT’L CO., LTD.
Contact:+86-0574-27666801
Address:Floor 21, Building 11, Xintiandi, No. 689, Shijiroad, Ningbo, Zhejiang, China
NIGNXIA XINDACHANG TECHNOLOGY CO.,LTD
Contact:86-0951-7815345
Address:North side of Qiyuan Road, west side of Yuanfeng Highway, New Material Park, Ningdong Energy and Chemical Industry Base, Ningxia,China
Taizhou Elitechemie MediPharma Technology Co.,Ltd.
Contact:+86-523-86810021
Address:Building G14,NO.1 Avenue,China Medical City, Taizhou, Jiangsu,China
Shandong LuZhou Amino Acid Co., Ltd
Contact:86-539-2218025
Address:yishui economic and technical development zone zhenxing south road
HEZE KINGVOLT CHEMICAL CO., LTD
Contact:86-573-82118911
Address:Juancheng Industry Park
Doi:10.1021/jo00310a014
(1990)Doi:10.1016/j.chempr.2017.10.007
(2017)Doi:10.1021/acs.jmedchem.0c00566
(2020)Doi:10.1246/bcsj.59.1277
(1986)Doi:10.1016/j.ejmech.2011.01.051
(2011)Doi:10.1021/ja2026882
(2011)
