60129-33-1Relevant academic research and scientific papers
Synthesis and pharmacological in vitro investigations of novel shikonin derivatives with a special focus on cyclopropane bearing derivatives
Kretschmer, Nadine,Hufner, Antje,Durchschein, Christin,Popodi, Katrin,Rinner, Beate,Lohberger, Birgit,Bauer, Rudolf
, p. 1 - 25 (2021/03/15)
Melanoma is the deadliest form of skin cancer and accounts for about three quarters of all skin cancer deaths. Especially at an advanced stage, its treatment is challenging, and survival rates are very low. In previous studies, we showed that the constitu
Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR
Basu, Debjit,Richters, André,Rauh, Daniel
, p. 2767 - 2780 (2015/06/08)
The clinical success of covalent kinase inhibitors in the treatment of EGFR-dependent non-small cell lung cancer (NSCLC) has rejuvenated the appreciation of reactive small molecules. Acquired drug resistance against first-line EGFR inhibitors remains the
TiCl4-mediated olefination of aldehydes with acetic acid and alkyl acetates: A stereoselective approach to (E)-α,β-unsaturated carboxylic acids and esters
Augustine, John Kallikat,Boodappa, Chandrakantha,Venkatachaliah, Srinivasa,Mariappan, Ayyampillai
, p. 3503 - 3506 (2014/06/10)
A new method has been developed for the preparation of α,β- unsaturated carboxylic acids and corresponding esters with (E)-stereoselectivity via the TiCl4-mediated olefination of aldehydes. The method, which uses readily available acetic acid or its alkyl esters as active methylene partners, is more flexible and complementary to conventional routes in the preparation of (E)-cinnamic acid derivatives.
N-HETEROARYL COMPOUNDS
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Page/Page column 85-86, (2012/04/17)
This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to novel N-heteroaryl compounds and the preparation of said compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.
3-cyclopropyl and 3-cyclobutyl pyrrolidine modulators of chemokine receptor activity
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, (2008/06/13)
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4fare defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
Tungsten(0) alkylidene complexes stabilized as pyridinium ylides: New aspects of their synthesis and reactivity
Rudler, Henri,Durand-Réville, Thomas
, p. 571 - 587 (2007/10/03)
The interaction of dihydropyridines with alkoxycarbene complexes of tungsten has been shown to lead to pyridinium ylid complexes: this transformation has now been applied to the synthesis of a hydroxyl-containing ylid complex by ring-opening of the pentacarbonyl (2-oxacyclopentylidene) tungsten(0) complex and to the synthesis of a series of chiral ylid complexes both from chiral and non-chiral carbene complexes by the use of dihydropyridines and dihydronicotines, respectively. The transfer of the alkylidene moiety of these complexes to nucleophilic olefins will be outlined and discussed. Especially relevant is the interaction of these pyridinium ylid complexes with unsaturated substrates such as dihydropyridines, enamines, and β-alkoxy bis(trimethyl-silyl) ketene acetals. This latter reaction leads to conjugated carboxylic acids, and has been be applied to a new synthesis of a honey bee pheromone, the queen substance.
Vinylcyclopropylacyl Radicals. Intramolecular Ketene Additions leading to Concise Syntheses of Cyclohexenones
Herbert, Nicola,Pattenden, Gerald
, p. 69 - 70 (2007/10/03)
Treatment of a range of vinylcyclopropyl selenyl esters with Bu3SnH-AIBN produces cyclohexenone products (50-60%) via 6-exo-dig radical cyclisations involving ketene intermediates.
Asymmetric dipolar cycloaddition reactions: A practical, convergent synthesis of chiral pyrrolidines
Ma, Zhenkun,Wang, Sanyi,Cooper, Curt S.,Fung, Anthony K. L.,Lynch, John K.,Plagge, Frederick,Chu, Daniel T. W.
, p. 883 - 887 (2007/10/03)
Chiral trans-3,4-disubstituted pyrrolidines were obtained from the 1,3-dipolar cycloaddition of chiral α,β-unsaturated N-acyloxazolidinones and azomethine ylide.
TRIAZOLO-1,4-DIAZEPINE DERIVATIVES AND THEIR USE IN PHARMACEUTICALS
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, (2008/06/13)
A triazolo-1,4-di-azepine compound of the below given formulas and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. STR1 in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 is hydrogen or an alkyl, X is--OCO--,--NHCO--,--CO--or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.
Control of Acarina by esters of cyclopropane acids
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, (2008/06/13)
Methods and compositions for the control of Acarina employing esters of cyclopropane carboxylic acids described herein.
