120-43-4Relevant articles and documents
L-selectride as a convenient reagent for the selective cleavage of carbamates
Coop, Andrew,Rice, Kenner C.
, p. 8933 - 8934 (1998)
L-Selectride(R) was shown to selectively cleave methyl carbamates in the presence of more sterically demanding carbamates, including the selective cleavage of a methyl carbamate in the presence of an N-Boc group.
Synthesis, mechanistic studies, and anti-proliferative activity of glutathione/glutathione S-transferase-activated nitric oxide prodrugs
Chakrapani, Harinath,Kalathur, Ravi C.,Maciag, Anna E.,Citro, Michael L.,Ji, Xinhua,Keefer, Larry K.,Saavedra, Joseph E.
, p. 9764 - 9771 (2008)
Nitric oxide (NO) prodrugs such as O2-(2,4-dinitrophenyl) 1-[(4-ethoxycarbonyl)piperazin-1-yl]diazen-1-ium-1,2-diolate (JS-K) are a growing class of promising NO-based therapeutics. Nitric oxide release from the anti-cancer lead compound, JS-K, is proposed to occur through a nucleophilic aromatic substitution by glutathione (GSH) catalyzed by glutathione S-transferase (GST) to form a diazeniumdiolate anion that spontaneously releases NO. In this study, a number of structural analogues of JS-K were synthesized and their chemical and biological properties were compared with those of JS-K. The homopiperazine analogue of JS-K showed anti-cancer activity that is comparable with that of JS-K but with a diminished reactivity towards both GSH and GSH/GST; both the aforementioned compounds displayed no cytotoxic activity towards normal renal epithelial cell line at concentrations where they significantly diminished the proliferation of a panel of renal cancer cell lines. These properties may prove advantageous in the further development of this class of nitric oxide prodrugs as cancer therapeutic agents.
Heteroaryl substituted dihydro pyrimidine compounds and their use in medicine
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Paragraph 0465-0469, (2017/08/14)
The invention relates to heteroaryl-substituted dihydropyrimidine compounds and application thereof in medicines, particularly application in medicines for treating and preventing hepatitis B. Particularly, the invention relates to compounds disclosed as general formula (I) or (Ia), or enantiomers, diastereoisomers, hydrates, solvates or pharmaceutically acceptable salts thereof, wherein the variables are defined in the specification. The invention also relates to application of the compounds disclosed as general formula (I) or (Ia), or enantiomers, diastereoisomers, hydrates, solvates or pharmaceutically acceptable salts thereof, especially application in medicines for treating and preventing hepatitis B.
BENZOPIPERIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND HEMOGLOBINOPATHIES
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Page/Page column 52, (2017/09/27)
A compound of formula I: (I) wherein: n is 1 or 2; p is 0 or 1; R1a, R1b, R1c and R1d are independently selected from H, halo, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, C1-4 alkyloxy, NH-C1-4 alkyl and cyano; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2e is H or Me; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (IIa), where R7a is selected from N-linked N-containing C5-7 heterocycyl and (A); or (ii) (IIb), where X is selected from CH2, N H and O, one of R8a and R8b is selected from CI and ethoxy and the other of R8a and R8b is H.