- Iron-Catalyzed Intramolecular C—H Amidation of N-Benzoyloxyureas
-
A redox-neutral Fe-catalyzed intramolecular C—H amidation of N-benzoyloxyureas is described. This methodology employs a simple iron complex in situ generated from Fe(OTf)2 and bipyridine as the catalyst and N-benzoyloxyureas as the nitrene prec
- Zhong, Dayou,Wu, Lin-Yang,Wang, Xing-Zhen,Liu, Wen-Bo
-
supporting information
p. 855 - 858
(2021/02/16)
-
- COMPOUNDS, PREPARATIONS AND USES THEREOF
-
The present invention provides novel compounds of the Formula (I), pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susc
- -
-
Page/Page column 128-129
(2011/07/09)
-
- Structure-based optimization of FDA-approved drug methylene blue as a c-myc G-quadruplex DNA stabilizer
-
G-quadruplexes are non-canonical DNA secondary structures putatively present in the promoter regions of oncogenes in the human genome. The targeting of promoter G-quadruplex structures to repress oncogene transcription represents a potential anticancer st
- Chan, Daniel Shiu-Hin,Yang, Hui,Kwan, Maria Hiu-Tung,Cheng, Zhen,Lee, Paul,Bai, Li-Ping,Jiang, Zhi-Hong,Wong, Chun-Yuen,Fong, Wang-Fun,Leung, Chung-Hang,Ma, Dik-Lung
-
experimental part
p. 1055 - 1064
(2012/03/22)
-
- Structure-activity correlations for β-phenethylamines at human trace amine receptor 1
-
A cell line in which RD-HGA16 cells were stably transfected with the hTAAR 1 receptor was created and utilized to carry out a systematic evaluation of a series of β-phenethylamines. Fair agreement was observed with data obtained for aryl and ethylene chain substituted analogs in an AV12-664 cell line in which hemagglutinin-tagged hTAAR 1 was stably co-expressed with rat Gαs. Analogs with multiple substituents as well as analogs with bulky groups were found to be partial agonists. Analogs in which the primary amino group was converted to a secondary or a tertiary amino group by N-methylation were also partial agonists. Comparative Molecular Field Analysis (CoMFA) using the potency data yielded a regression coefficient r2 of 0.824. The steric field contribution to the model was 61% with the balance (39%) contributed by the electrostatic field. The collective results suggest that increasing steric bulk both at the amino nitrogen, particularly by N-dimethylation, and at the 4-position of the aromatic ring leads to low efficacy ligands.
- Lewin, Anita H.,Navarro, Hernan A.,Wayne Mascarella
-
p. 7415 - 7423
(2008/12/22)
-
- MACROCYCLIC FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
-
The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, thereof, wherein the variables A, B, L, M, W, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.
- -
-
Page/Page column 130
(2008/06/13)
-