European Journal of Medicinal Chemistry (2021)
Update date:2022-08-15
Topics: Synthesis Design Structure-Activity Relationship Urea compounds FGFR1 inhibitors Metastatic triple-negative breast cancer
Akwii, Racheal
Alvina, Karina
Ashraf-Uz-Zaman, Md
Farshbaf, Mohammad Jodeiri
German, Nadezhda A.
Kallem, Raja Reddy
Mikelis, Constantinos M.
Putnam, William
Sajib, Md Sanaullah
Shahi, Sadisna
Trippier, Paul C.
Wang, Wei
Zhang, Ruiwen
Triple-negative breast cancer (TNBC) is an aggressive type of cancer characterized by higher metastatic and reoccurrence rates, where approximately one-third of TNBC patients suffer from the metastasis in the brain. At the same time, TNBC shows good responses to chemotherapy, a feature that fuels the search for novel compounds with therapeutic potential in this area. Recently, we have identified novel urea-based compounds with cytotoxicity against selected cell lines and with the ability to cross the blood-brain barrier in vivo. We have synthesized and analyzed a library of more than 40 compounds to elucidate the key features responsible for the observed activity. We have also identified FGFR1 as a molecular target that is affected by the presence of these compounds, confirming our data using in silico model. Overall, we envision that these compounds can be further developed for the potential treatment of metastatic breast cancer.
View MoreContact:0512-63006287
Address:no.88.YISHENG Road,etdz-WUJIANG,SUZHOU,CHINA
VanderArk International Limited
Contact:86-10-82437576
Address:Qing He
Zibo Ocean International Trade Co.,Ltd
Contact:+86 533 5160706
Address:1117, Hongtai Bld., Songling rd, Zichuan,Zibo,Shandong,China
Beijing Green Guardee Technology CO,.LTD
Contact:+86-10-69706062
Address:F2 BLdj,5 No.37 Chaoqian Road
WUXI KINGHAN BIO-MEDICAL&CHEMICAL INC.
Contact:13861062998
Address:Room 1316,No.1619 Huishan Avenue,Wuxi,China
Doi:10.1021/jo502002w
(2015)Doi:10.1055/s-2006-942449
(2006)Doi:10.1246/bcsj.62.3567
(1989)Doi:10.1002/jccs.201190031
(2011)Doi:10.1021/ja01100a507
(1953)Doi:10.1021/ja01206a051
(1946)