62235-59-0Relevant academic research and scientific papers
POLYMORPHIC COMPOUNDS AND USES THEREOF
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Paragraph 00596; 00598; 0603, (2020/11/13)
The present invention relates to free-base and salt forms, and compositions thereof of small molecule therapeutics acting as a scavenger for toxic aldehydes. The present invention further relates to use of the free-base and salt forms, and compositions thereof for treating diseases, disorders, or conditions in which aldehyde toxicity is implicated in their pathogenesis.
Synthesis and Antiproliferative Activity Evaluation of the Disulfide-Containing Cyclic Peptide Thiochondrilline C and Derivatives
Vippila, Mohana Rao,Ly, Phuong Kim,Cuny, Gregory D.
, p. 2398 - 2404 (2015/11/09)
Thiochondrilline C (4) was previously isolated from Verrucisispora sp. and reported to have moderate cytotoxicity against human lung adenocarcinoma cells. Herein, we report the synthesis of thiochondrilline C by N-terminal peptide extension, oxidative disulfide bond formation, and heterocycle installation as key steps. Antiproliferative activities for the prepared natural product and several derivatives against the NCI 60 cancer cell line panel are also described. Derivative 22 was identified as a moderately potent antiproliferative agent (50% growth inhibition (GI50) = 0.2-12.2 μM) with leukemia (average GI50 = 1.8 ± 0.1 μM) and colon (average GI50 = 2.4 ± 0.3 μM) cells being most sensitive.
Novel approach to synthesis of substituted 3-aminoquinolines from nitroarenes and protected ethyl aminocrotonate
Bujok, Robert,Kwast, Andrzej,Cmoch, Piotr,Wróbel, Zbigniew
experimental part, p. 698 - 708 (2010/09/05)
The addition of mono- and dianions of ethyl N-pivaloyl-3-aminocrotonate to substituted nitroarenes, followed by action of silylating or acylating agent, leads to 3-aminoquinoline carboxylic acid derivatives. Hydrolysis and decarboxylation of the latter, carried out efficiently under relatively mild conditions, afford 3-aminoquinolines diversely substituted in the benzo-fused ring.
Design, synthesis, and structure-activity relationship studies of new phenolic DNA gyrase inhibitors
Luebbers, Thomas,Angehrn, Peter,Gmuender, Hans,Herzig, Silvia
, p. 4708 - 4714 (2008/02/10)
Starting from a biased needle screening hit 3a, we report herein the design and synthesis of a series of novel 2,3-dihydroisoindol-1-ones structurally related to cyclothialidine 2 with DNA gyrase inhibitory activity. In this series, some compounds exhibit
CETP INHIBITORS
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Page/Page column 49, (2008/06/13)
Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B is a cyclic group other than phenyl, and B has a cyclic substituent at a position that is ortho to the position at which B is connected to the remainder of the structure of Formula (I). The 5-membered ring of Formula (I) has a second cyclic substituent in addition to B.
A facile one-pot synthesis of 2-substituted-3-aminoquinolines: Preparation of benzo[b]naphthyridine-3-carbonitriles
Wang, Yanong D.,Boschelli, Diane H.,Johnson, Steven,Honores, Erick
, p. 2937 - 2942 (2007/10/03)
A facile one-pot synthesis of 3-aminoquinolines from ortho- aminobenzaldehydes was developed. Ethyl 6,7-dimethoxy-3-aminoquinoline-2- carboxylate, a key intermediate for the preparation of a 4-anilino-benzo[b][1,5] -naphthyridine-3-carbonitrile, was efficiently prepared by this method. Synthetic routes to 4-anilino-benzo[b][1,5]-naphthyridine-3-carbonitrile and 4-anilino-benzo[b][1,8]-naphthyridine-3-carbonitrile are described.
