38202-27-6Relevant articles and documents
Fsp3-rich and diverse fragments inspired by natural products as a collection to enhance fragment-based drug discovery
Hanby, Abigail R.,Kidd, Sarah L.,Mortensen, Kim T.,Osberger, Thomas J.,Spring, David R.,Troelsen, Nikolaj S.
supporting information, p. 2280 - 2283 (2020/03/04)
Herein, we describe the natural product inspired synthesis of 38 complex small molecules based upon 20 unique frameworks suitable for fragment-based screening. Utilising an efficient strategy, two key building block diastereomers were harnessed to generate novel, three-dimensional fragments which each possess numerous synthetically accessible fragment growth positions.
SUBSTITUTED TETRAHYDROISOQUINOLINE ETHYLBENZAMIDE ANTI-CANCER AGENTS
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Paragraph 031, (2019/04/18)
The compounds herein disclosed are N-substituted tetrahydroisoquinoline ethylbenzamide compounds that have modifications on the phenyl rings by introducing groups with various electronic properties. These derivatives of N-substituted tetrahydroisoquinoline ethylbenzamide compounds have been shown to have anti-proliferative activity against cells. In particular, the compounds have been found to be effective in inhibiting the proliferation of cancer cells, such as cancer cells that originated in breast tissue. Additionally, it has been shown that the novel compounds have IC50 values against the breast cancer cells that are 6- to 10-fold less than the IC50 of Tamoxifen.
Ammonia-free synthesis of 3-trifluoromethyl-3-phenyldiaziridine
Kumar, Arun Babu,Manetsch, Roman
supporting information, p. 626 - 631 (2018/02/26)
An ammonia-free synthesis of 3-trifluoromethyl-3-phenyldiaziridine, an important intermediate in the synthesis of a widely used photolabel 3-trifluoromethyl-3-phenyldiazirine, is described. By avoiding the use of volatile, corrosive, and toxic anhydrous ammonia, the major hazard involved in the synthesis of this widely used photolabel is eliminated. Furthermore, this synthesis is convenient compared to the conventional route, since it is significantly less time consuming and, due to the absence of liquid ammonia, this method does not require the maintenance of low temperature for prolonged periods.
