- Ammonium [11C]thiocyanate: revised preparation and reactivity studies of a versatile nucleophile for carbon-11 radiolabelling
-
Herein we report the preparation of ammonium [11C]thiocyanate via the reaction of [11C]CS2 with ammonia. The [11C]SCN- ion is demonstrated as a potent nucleophile that can be used to readily generate a range of 11C-labelled thiocyanate molecules in high conversions. Furthermore, novel 11C-labelled thiazolone molecules can be easily prepared from the intermediate α-thiocyanatophenones via an acid mediated cyclisation reaction.
- Haywood, Tom,Cesarec, Sara,Kealey, Steven,Plisson, Christophe,Miller, Philip W.
-
supporting information
p. 1311 - 1314
(2018/08/28)
-
- COLORED CURABLE RESIN COMPOSITION
-
PROBLEM TO BE SOLVED: To provide a colored curable resin composition capable of forming a color filter excellent in lightness. SOLUTION: The colored curable resin composition contains a colorant, a resin, a polymerizable compound, and a polymerization ini
- -
-
Paragraph 0165
(2018/11/27)
-
- Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain
-
Recognizing acetyllysine of histone is a vital process of epigenetic regulation that is mediated by a protein module called bromodomain. To contribute novel scaffolds for developing into bromodomain inhibitors, we utilize a fragment-based drug discovery approach. By successively applying docking and X-ray crystallography, we were able to identify 9 fragment hits from diffracting more than 60 crystals. In the present work, we described four of them and carried out the integrated lead optimization for fragment 8, which bears a 2-thiazolidinone core. After several rounds of structure guided modifications, we assessed the druggability of 2-thiazolidinone by modulating in vitro pharmacokinetic studies and cellular activity assay. The results showed that two potent compounds of 2-thiazolidinones have good metabolic stability. Also, the cellular assay confirmed the activities of 2-thiazolidinones. Together, we hope the identified 2-thiazolidinone chemotype and other fragment hits described herein can stimulate researchers to develop more diversified bromodomain inhibitors.
- Zhao, Lele,Cao, Danyan,Chen, Tiantian,Wang, Yingqing,Miao, Zehong,Xu, Yechun,Chen, Wuyan,Wang, Xin,Li, Yanlian,Du, Zhiyan,Xiong, Bing,Li, Jian,Xu, Chunyan,Zhang, Naixia,He, Jianhua,Shen, Jingkang
-
p. 3833 - 3851
(2013/07/11)
-
- Inhibitory effect of 4-aryl 2-substituted aniline-thiazole analogs on growth of human prostate cancer LNCap cells
-
Androgen receptor (AR) is ligand-inducible nuclear hormone receptor which has been focused on key molecular target in growth and progression of prostate cancer. We synthesized a series of 4-aryl 2-substituted aniline-thiazole analogs and evaluated their anti-cancer activity in AR-dependent human prostate cancer LNCap cells. Among them, the compound 6 inhibited the tumor growth in LNCap-inoculated xenograft model.
- Baek, Seung-Hwa,Kim, Nakjeong,Kim, Seong Hwan,Park, Kwang Hwa,Jeong, Kyung-Chae,Park, Bae Keun,Kang, Nam Sook
-
p. 111 - 114
(2012/03/26)
-