81581-05-7Relevant academic research and scientific papers
4β-amidotriazole linked podophyllotoxin congeners: DNA topoisomerase-IIα inhibition and potential anticancer agents for prostate cancer
Reddy, V. Ganga,Bonam, Srinivasa Reddy,Reddy, T. Srinivasa,Akunuri, Ravikumar,Naidu,Nayak, V. Lakshma,Bhargava, Suresh K.,Kumar, H.M. Sampath,Srihari,Kamal, Ahmed
, p. 595 - 611 (2018/01/01)
Topoisomerases (topo-I and topo-II) have occupied a significant role in DNA replication, transcription, and are a promising set of antitumor targets. In the present approach, a series of new 4β-amidotriazole linked podophyllotoxin derivatives (10a-i and 1
N-Benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors
Atkinson, Karen A.,Beretta, Elena E.,Brown, Janice A.,Castrodad, Mayda,Chen, Yue,Cosgrove, Judith M.,Du, Ping,Litchfield, John,Makowski, Michael,Martin, Kelly,McLellan, Thomas J.,Neagu, Constantin,Perry, David A.,Piotrowski, David W.,Steppan, Claire M.,Trilles, Richard
scheme or table, p. 1621 - 1625 (2011/05/05)
A potent, small molecule inhibitor with a favorable pharmacokinetic profile to allow for sustained SCD inhibition in vivo was identified. Starting from a low MW acyl guanidine (5a), identified with a RapidFire High-Throughput Mass Spectrometry (RF-MS) assay, iterative library design was used to rapidly probe the amide and tail regions of the molecule. Singleton synthesis was used to probe core changes. Biological evaluation of a SCD inhibitor (5b) included in vitro potency at SCD-1 and in vivo modulation of the plasma desaturation index (DI) in rats on a low essential fatty acid (LEFA) diet. In addition to dose-dependent decrease in DI, effects on rodent ocular tissue were noted. Therefore, in rat, these SCD inhibitors only recapitulate a portion of phenotype exhibited by the SCD-1 knockout mouse.
PYRAZOLE DERIVATIVES AS CYTOCHROME P450 INHIBITORS
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Page/Page column 82, (2008/06/13)
The present invention provides compounds of formula (I), or pharmaceutically acceptable salts or solvates thereof, methods for their preparation, methods for their use, and pharmaceutical formulations comprising them.
Dipolar Cycloaddition Reactions of Organic Azides with some Acetylenic Compounds
Abu-Orabi, Sultan T.,Atfah, M. Adnan,Jibril, Ibrahim,Mari'i, Fakhri M.,Ali, Amer Al-Sheikh
, p. 1461 - 1468 (2007/10/02)
Phenyl azide 1 and several substituted benzyl azides 2a-o underwent 1,3-dipolar cycloaddition reactions with dimethyl acrtylenedicarboxylate 3, phenylacetylene 4 and ethyl propiolate 5 to afford the triazoles 6-13.The reactions of these azides with ethyl
Studies of v-Triazoles. Part 4. The 4-Methoxybenzyl Group, a Versatile N-Protecting Group for the Synthesis of N-Unsubstituted v-Triazoles
Buckle, Derek R.,Rockell, Caroline J.M.
, p. 627 - 630 (2007/10/02)
A series of readily prepared monocyclic N-(4-methoxybenzyl)-v-trizoles (1) have been converted into their N-unsubstituted derivatives (2) by treatment with trifluoroacetic acid at 65 deg C.The procedure allows the synthesis of a range of N-unsubstituted v
