659729-07-4Relevant academic research and scientific papers
Synthesis of novel substituted pyrimidine derivatives bearing a sulfamide group and their in vitro cancer growth inhibition activity
Lefebvre, Carole-Anne,Forcellini, Elsa,Boutin, Sophie,C?té, Marie-France,C.-Gaudreault, René,Mathieu, Patrick,Lagüe, Patrick,Paquin, Jean-Fran?ois
supporting information, p. 299 - 302 (2016/12/27)
The synthesis of two series of novel substituted pyrimidine derivatives bearing a sulfamide group have been described and their in vitro cancer growth inhibition activities have been evaluated against three human tumour cell lines (HT-29, M21, and MCF7). In general, growth inhibition activity has been enhanced by the introduction of a bulky substituent on the aromatic ring with the best compound having GI50??6?μM for all the human tumour cell lines. The MCF7 selective compounds were evaluated on four additional human invasive breast ductal carcinoma cell lines (MDA-MB-231, MDA-MB-468, SKBR3, and T47D) and were selective against T47D cell line in all cases except one, suggesting a potential antiestrogen activity.
Novel vanilloid receptor-1 antagonists: 1. Conformationally restricted analogues of trans-cinnamides
Norman, Mark H.,Zhu, Jiawang,Fotsch, Christopher,Bo, Yunxin,Chen, Ning,Chakrabarti, Partha,Doherty, Elizabeth M.,Gavva, Narender R.,Nishimura, Nobuko,Nixey, Thomas,Ognyanov, Vassil I.,Rzasa, Robert M.,Stec, Markian,Surapaneni, Sekhar,Tamir, Rami,Viswanadhan, Vellarkad N.,Treanor, James J. S.
, p. 3497 - 3514 (2008/02/11)
The vanilloid receptor-1 (VR1 or TRPV1) is a member of the transient receptor potential (TRP) family of ion channels and plays a role as an integrator of multiple pain-producing stimuli. From a high-throughput screening assay, measuring calcium uptake in
