77290-47-2Relevant academic research and scientific papers
Synthesis and biological evaluation of novel tryptoline derivatives as indoleamine 2,3-dioxygenase (IDO) inhibitors
Tanaka, Minoru,Li, Xin,Hikawa, Hidemasa,Suzuki, Takafumi,Tsutsumi, Katsuhiko,Sato, Masashi,Takikawa, Osamu,Suzuki, Hideharu,Yokoyama, Yuusaku
, p. 1159 - 1165 (2013/03/14)
Indoleamine 2,3-dioxygenase (IDO) plays a significant role in several disorders such as Alzheimer's disease, age-related cataracts and tumors. A series of novel tryptoline derivatives were synthesized and evaluated for their inhibitory activity against ID
Structure-activity relationship study of novel necroptosis inhibitors
Teng, Xin,Degterev, Alexei,Jagtap, Prakash,Xing, Xuechao,Choi, Sungwoon,Denu, Regine,Yuan, Junying,Cuny, Gregory D.
, p. 5039 - 5044 (2007/10/03)
Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling necrosis. It can be induced in a FADD-deficient variant of human Jurkat T cells treated with TNF-α. 5-(1H-Indol-3-ylmethyl)-2-thiohydantoins and 5-(1H-indol-3-ylmethyl)hydantoins were found to be potent necroptosis inhibitors (called necrostatins). A SAR study revealed that several positions of the indole were intolerant of substitution, while small substituents at the 7-position resulted in increased inhibitory activity. The hydantoin ring was also quite sensitive to structural modifications. A representative member of this compound class demonstrated moderate pharmacokinetic characteristics and readily entered the central nervous system upon intravenous administration.
Synthesis of 7-Chloro-L- and 7-Chloro-D-tryptophan; Biosynthesis of Pyrrolnitrin
Pee, Karl-Heinz van,Salcher, Olga,Lingens, Franz
, p. 233 - 239 (2007/10/02)
The article describes the synthesis of 7-chloro-DL-tryptophan (1 with R=Cl) via the intermediates 5, 6, 7 and 8.The separation of the optical antipodes was achieved by treatment of 7-chloro-N-chloroacetyl-DL-tryptophan (9) with carboxypeptidase.DL-Tryptophan (1 with R=H), 1 with R=Cl and its anomers, 1a with R=Cl and 1b with R=Cl, are substrates of L-tryptophan-2,3-dioxygenase from Pseudomonas aureofaciens.
