Bioorganic and Medicinal Chemistry p. 421 - 439 (2017)
Update date:2022-08-15
Topics:
Shelton, Kerri L.
DeBord, Michael A.
Wagers, Patrick O.
Southerland, Marie R.
Williams, Travis M.
Robishaw, Nikki K.
Shriver, Leah P.
Tessier, Claire A.
Panzner, Matthew J.
Youngs, Wiley J.
A series of N,N′-bis(arylmethyl)benzimidazolium salts have been synthesized and evaluated for their in vitro anti-cancer activity against select non-small cell lung cancer cell lines to create a structure activity relationship profile. The results indicate that hydrophobic substituents on the salts increase the overall anti-proliferative activity. Our data confirms that naphthylmethyl substituents at the nitrogen atoms (N1(N3)) and highly lipophilic substituents at the carbon atoms (C2and C5(C6)) can generate benzimidazolium salts with anti-proliferative activity that is comparable to that of cisplatin. The National Cancer Institute's Developmental Therapeutics Program tested 1, 3–5, 10, 11, 13–18, 20–25, and 28–30 in their 60 human tumor cell line screen. Results were supportive of data observed in our lab. Compounds with hydrophobic substituents have higher anti-cancer activity than compounds with hydrophilic substituents.
View MoreNanjing Norris Pharm Technology Co., Ltd.
Contact:+86-13901585132
Address:2 Qiande Road, Jiangning sciencepark Hi-Tech Zone, Nanjing, P.R.China
Zhejiang Hoshine Silicon Industry Co., Ltd.
Contact:86-573-89179966
Address:Zhapu Town, Pinghu City, Zhejiang, China
HANGZHOU ZHONGCHANG SCIENTIFIC CO.,LTD
Contact:+86-571-88932183
Address:Hangzhou
Beijing Greenchem Technology Co.,Ltd. ( Panjin Greenchem Technology Co.Ltd .)
website:http://www.bjgreenchem.com/
Contact:+86-427-6515887
Address:301,302, 3rd Floor, Building C-7, Dongsheng Science Park, Northern Territory, Zhongguancun, No. 66, Xixiaokou Road, Haidian District, Beijing
Hangzhou Gangjin Chemical Co.,Ltd.
Contact:+86-571-85109780
Address:707 Zhejiang Minhang Bldg., No.290 Zhongshan North Road, Hangzhou 310003, China
Doi:10.1007/s10870-005-3884-y
(2005)Doi:10.1016/j.bmcl.2004.11.049
(2005)Doi:10.1080/00397911.2020.1799010
(2020)Doi:10.1021/jo401134c
(2013)Doi:10.1021/ac00257a003
(1983)Doi:10.1021/jo00306a006
(1990)