3284-51-3Relevant articles and documents
A novel pyrrole synthesis: One-pot preparation of ethyl 5-methylpyrrole-2-carboxylate
Curran, Timothy P.,Keaney, Meghan T.
, p. 9068 - 9069 (1996)
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SYNTHESIS OF FURAN, THIOPHENE, AND PYRROLES FROM ACETOACETIC ESTERS
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Paragraph 0117-0120, (2016/11/07)
The present invention refers to using ester pgd2 alkylacetoacetoates furan, thiophene, method relates to synthesis of pyrrole, more particularly the acetohydroxy pgd2 ester compound alpha, beta unsaturated carbonyl compounds obtained is added to the 1,5-dicarbonyl compounds (II)/ cobalt manganese (III) method of silica glass by sol the reaction deacetylase with Neel step then alkali to thereby synthesize a compound 1,4-dicarboxylic, Paal-Knorr herein using synthesis on the furan, thiophene, pyrrole for synthesizing relates to method. According to the present invention, a necessary for synthesis of Paal-Knorr 1,4-dicarbonyl compounds efficiently mixed in the oxidation reaction from said 1,5-dicarbonyl compounds (deacetylase reaction) and a conjunction synthesis on the Paal-Knorr in the reaction vessel a are sequentially two reactors furan, thiophene, and of won-port synthesis method by using the mask pattern.. (by machine translation)
Synthesis and biological evaluation of novobiocin analogues as potential heat shock protein 90 inhibitors
Gunaherath, G.M. Kamal B.,Marron, Marilyn T.,Wijeratne, E.M. Kithsiri,Whitesell, Luke,Gunatilaka, A.A. Leslie
, p. 5118 - 5129 (2013/09/02)
Recent studies have shown that novobiocin (NB), a member of the coumermycin (CA) family of antibiotics with demonstrated DNA gyrase inhibitory activity, inhibits Heat shock protein 90 (HSP90) by binding weakly to a putative ATP-binding site within its C-terminus. To develop more potent HSP90 inhibitors that target this site and to define structure-activity relationships (SARs) for this class of compounds, we have synthesized twenty seven 3-amido-7- noviosylcoumarin analogues starting from NB and CA. These were evaluated for evidence of HSP90 inhibition using several biological assays including inhibition of cell proliferation and cell cycle arrest, induction of the heat shock response, inhibition of luciferase-refolding in vitro, and depletion of the HSP90 client protein c-erbB-2/HER-2/neu (HER2). This SAR study revealed that a substantial increase in biological activity can be achieved by introduction of an indole-2-carboxamide group in place of 4-hydroxy-isopentylbenzamido group at C-3 of NB in addition to removal/derivatization of the 4-hydroxyl group from the coumarin ring. Methylation of the 4-hydroxyl group in the coumarin moiety moderately increased biological activity as shown by compounds 11 and 13. Our most potent new analogue 19 demonstrated biological activities consistent with known HSP90-binding agents, but with greater potency than NB.
