70946-17-7Relevant academic research and scientific papers
Inhibitors of protein activity for the treatment of angiogenesis and SOX18/or lymphangiogenesis-related diseases
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Paragraph 0152; 0160; 0163, (2020/01/04)
Disclosed are compounds of a formula provided herein that show efficacy in the inhibition of SOX18 protein activity, and in particular with respect to the ability of SOX18 to bind DNA and/or particular protein partners. Further, methods of treating angiog
INHIBITORS OF SOX18 PROTEIN ACTIVITY FOR TREATING ANGIOGENESIS-AND/OR LYMPHANGIOGENESIS-RELATED DISEASES
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Paragraph 0157; 0162, (2019/11/19)
Disclosed are compounds of a formula provided herein that show efficacy in the inhibition of SOX18 protein activity, and in particular with respect to the ability of SOX18 to bind DNA and/or particular protein partners. Further, methods of treating angiog
Selective Oxidative Dearomatization of Angular Tetracyclic Phenols by Controlled Irradiation under Air: Synthesis of an Angucyclinone-Type Double Peroxide with Anticancer Properties
Cabrera-Afonso, María J.,Lucena, Silvia R.,Juarranz, ángeles,Urbano, Antonio,Carreno, M. Carmen
supporting information, p. 6094 - 6098 (2018/09/27)
Angular tetracyclic p-peroxyquinols, p-quinols, and a pentacyclic double peroxide, showing anticancer properties, were synthesized from the corresponding phenols by an environmentally friendly solvent- and wavelength-controlled irradiation under air in th
Synthesis of the griseusin B framework via a one-pot annulation- methylation-double deprotection-spirocyclization sequence
Naysmith, Briar J.,Brimble, Margaret A.
supporting information, p. 2006 - 2009 (2013/06/04)
A highly convergent synthesis of the griseusin B scaffold is described. The key step involves an efficient one-pot Hauser-Kraus annulation-methylation- double deprotection-spirocyclization sequence that directly affords the target parent tetracyclic ring system.
Efficient synthesis of anacardic acid analogues and their antibacterial activities
Mamidyala, Sreeman K.,Ramu, Soumya,Huang, Johnny X.,Robertson, Avril A.B.,Cooper, Matthew A.
supporting information, p. 1667 - 1670 (2013/04/10)
Anacardic acid derivatives exhibit a broad range of biological activities. In this report, an efficient method for the synthesis of anacardic acid derivatives was explored, and a small set of salicylic acid variants synthesised retaining a constant hydrophobic element (a naphthyl tail). The naphthyl side chain was introduced via Wittig reaction and the aldehyde installed using directed ortho-metalation reaction of the substituted o-anisic acids. The failure of ortho-metalation using unprotected carboxylic acid group compelled us to use directed ortho-metalation in which a tertiary amide was used as a strong ortho-directing group. In the initial route, tertiary amide cleavage during final step was challenging, but cleaving the tertiary amide before Wittig reaction was beneficial. The Wittig reaction with protected carboxylic group (methyl ester) resulted in side-products whereas using sodium salt resulted in higher yields. The novel compounds were screened for antibacterial activity and cytotoxicity. Although substitution on the salicylic head group enhanced antibacterial activities they also enhanced cytotoxicity.
Probing the reactivity of o-phthalaldehydic acid/methyl ester: Synthesis of N-isoindolinones and 3-arylaminophthalides
Mamidyala, Sreeman K.,Cooper, Matthew A.
supporting information, p. 8407 - 8409 (2013/09/23)
A new method for the synthesis of N-substituted isoindolinones and 3-arylaminophthalides was developed through aza-Wittig/cyclisation. The reaction of o-phthalaldehydic acid methyl ester with benzylic, aromatic and aliphatic azides gave N-isoindolinones w
Total synthesis of (+)-varitriol and (+)-6′-epi-varitriol
Vamshikrishna,Srihari
experimental part, p. 1540 - 1546 (2012/02/17)
Total synthesis of (+)-varitriol and its C6′-epimer have been achieved starting from commercially available d-(-)-ribose and o-anisic acid. The key steps involved are Corey Chaykovsky reaction, triethylamine mediated epimerization, and an olefin cross-met
Regiocontrolled rearrangement of isobenzofurans
Egan, Ben A.,Paradowski, Michael,Thomas, Lynne H.,Marquez, Rodolfo
experimental part, p. 2086 - 2089 (2011/06/25)
Regioselective alkylation and oxidative rearrangement of isobenzofurans has been achieved to generate substituted 4,8- ihydroxyisochromanones in good yields and with complete regiocontrol.
Rational design of inhibitors of VirA-VirG two-component signal transduction
Maresh, Justin,Zhang, Jin,Tzeng, Yih-Ling,Goodman, Nora A.,Lynn, David G.
, p. 3281 - 3286 (2008/02/08)
VirA-VirG two-component system regulates the vir (virulence) operon in response to specific host factors (xenognosins) in the plant pathogen Agrobacterium tumefaciens. Using whole cell assays, stable inhibitors inspired by the labile natural benzoxazinone inhibitor HDMBOA are developed. It is found that aromatic aldehydes represent a minimal structural unit for activity. In particular, 3-hydroxy-4,6-dimethoxy-3H-isobenzofuran-1-one (HDI) was found to have the highest activity, making it the most potent developed inhibitor of virulence gene expression in Agrobacterium.
A short enantioselective synthesis of the topoisomerase II inhibitor (+)-eleutherin
Gibson, Jennifer S.,Andrey, Olivier,Brimble, Margaret A.
, p. 2611 - 2613 (2008/02/13)
A Hauser-Kraus annulation was used as a key step for the concise enantioselective synthesis of the topoisomerase II inhibitor (+)-eleutherin. Georg Thieme Verlag Stuttgart.
