Journal of Medicinal Chemistry p. 2279 - 2291 (1993)
Update date:2022-07-30
Topics:
Pendergast
Johnson
Dickerson
Dev
Duch
Ferone
Hall
Humphreys
Kelly
Wilson
The synthesis and thymidylate synthase (TS) inhibitory activity of a series of simple benzo[f]-quinazolin-1(2H)-ones are described. Fully aromatic 3-amino compounds with compact lipophilic substituents in the 9-position were found to have I50 values as low as 20 nM on the isolated enzyme, and represent the first examples of potent, folate-based TS inhibitors that completely lack any structural feature corresponding to the (p- aminobenzoyl)glutamate moiety of the cofactor. A number of the compounds also showed moderate growth inhibitory activity against a human colon adenocarcinoma cell line (SW480), with IC50 values as low as 2 μM.
View MoreRugao Jinling Chemical Co., Ltd.
Contact:0086-513-68005586
Address:Lianluo new village huangshi town Rugao city Jiangsu Province.
Jiangsu Fengshan Group Co., Ltd.
Contact:86-25-86558671
Address:1903,Central International Mansion 105-6 North Zhongshan Road, Nanjing, China
Contact:0086 371 65711996
Address:Jalan 4/3, Kawasan Perindustrian Serendah, 48000 Rawang,
Hangzhou Dawn Ray Pharmaceutical Co.,Ltd
website:http://www.dawnraypharma.com/
Contact:+86-571-85335020
Address:1018 Guangyin Building,No.42 E.Fengqi Road,Hangzhou,310012 China
Contact:86 513 85512619
Address:Rm.1306, Building A, Wenfeng Mansion,168 Gongnong Road, Nantong Jiangsu China
Doi:10.1016/j.bmcl.2007.04.082
(2007)Doi:10.1002/hlca.19380210118
(1938)Doi:10.1021/acs.joc.0c00469
(2020)Doi:10.1002/anie.201108139
(2012)Doi:10.1246/bcsj.45.3586
(1972)Doi:10.1021/ja00777a014
(1972)