52085-14-0Relevant academic research and scientific papers
Choline chloride based eutectic solvent for the efficient synthesis of 2-amino-4H-chromen-4-yl phosphonate derivatives via multicomponent reaction under mild conditions
Krishnammagari, Suresh Kumar,Cho, Byung Gwon,Jeong, Yeon Tae
, p. 306 - 316 (2018)
Synthesis of 2-amino-4H-chromen-4-ylphosphonate derivatives has been accomplished by the one-pot three-component reaction of salicylaldehyde, malononitrile/ethylcyanoacetate and dialkyl phosphites in the presence of reusable deep eutectic solvent (DES) under mild conditions. The advantages of this method are mild reaction conditions, simple work-up procedure, use of DES as a green solvent and an economical protocol for the preparation of important biologically active phosphorus-containing compounds.
A simple and efficient approach for the preparation of dihydroxanthyletin, xanthyletin, decursinol and marmesin
Kommera, Rajkumar,Bhimapaka, China Raju
supporting information, p. 3204 - 3211 (2020/08/05)
A simple and efficient approach has been developed for the preparation of coumarin natural products such as dihydroxanthyletin, xanthyletin, decursinol and marmesin starting from commercially available 2,4-dihydroxybenzaldehyde with very good yields. Wittig homologation and Claisen rearrangement are the protocols used to achieve these molecules.
Semicarbazone derivatives bearing phenyl moiety: Synthesis, anticancer activity, cell cycle, apoptosis-inducing and metabolic stability study
Ma, Junjie,Ni, Xin,Gao, Yali,Huang, Kun,Wang, Yu,Liu, Jiaan,Gong, Guowei
, p. 351 - 360 (2019/05/07)
A series of semicarbazone derivatives bearing phenyl moiety were synthesized and evaluated for the vitro anticancer activities in four human cancer cell lines (human colon cancer (HT29), human neuroblastoma (SK-N-SH), human breast cancer (MDA-MB-231), and human gastric cancer (MKN45)). Biological evaluation led to the identification of 11q and 11s, which showed excellent anticancer activities against tested cancer cell lines with IC50 values ranging from 0.32 to 1.57μM, respectively, while exhibiting weak cytotoxicity on the normal cells (human umbilical vein endothelial cell (HUVEC)). Flow cytometric assay for cell cycle and apoptosis revealed that 11q and 11s caused an arrest in the Sub-G1 cell cycle and inhibited proliferation of cancer cells by inducing apoptosis in a dose-dependent manner. Further enzymatic assay suggested that 11q and 11s could significantly activated procaspase-3 to caspase-3. Metabolic stability study indicated that 11q and 11s showed moderate stability in vitro in human and rat liver microsomes. In view of promising pharmacological activities of 11q and 11s, which had emerged as the valuable lead for further development in the treatment for cancer.
5-FLUORO-C-(ARYL OR HETEROCYCLYL)-GLYCOSIDE DERIVATIVES USEFUL AS DUAL SGLT1 / SGLT2 MODULATORS
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Paragraph 0405, (2019/02/28)
The present invention is directed to 5-fluoro-C-(aryl or hetercyclyl)-glycoside derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by SGLT activity, more particularly dual SGLT1/2 activity.
Choline hydroxide: An efficient and biodegradable catalyst for the synthesis of 2-amino-3-nitro-4H-chromene derivatives in an aqueous medium
Krishnammagari, Suresh Kumar,Lim, Kwon Taek,Cho, Byung Gwon,Tae Jeong, Yeon
supporting information, p. 574 - 581 (2018/09/25)
An expedient, eco-friendly and efficient procedure for the synthesis of novel 2-amino-3-nitro-4H-chromene derivatives has been developed through the reaction of various 2-hydroxybenzaldehydes and (E)-N-methyl-1-(methylthio)-2-nitroethenamine in the presence of the basic ionic liquid catalyst (choline hydroxide (ChOH)) at room temperature an aqueous medium. The advantageous of this method is a biodegradable and recyclable catalyst, mild, environmentally friendly and high products yields (83-96%) in short reaction times.
Development of noviomimetics that modulate molecular chaperones and manifest neuroprotective effects
Forsberg, Leah K.,Anyika, Mercy,You, Zhenyuan,Emery, Sean,McMullen, Mason,Dobrowsky, Rick T.,Blagg, Brian S.J.
, p. 1428 - 1435 (2017/11/17)
Heat shock protein 90 (Hsp90) is a chaperone under investigation for the treatment of cancer and neurodegenerative diseases. Neuroprotective Hsp90 C-terminal inhibitors derived from novobiocin (novologues) include KU-32 and KU-596. These novologues modulate molecular chaperones and result in an induction of Heat Shock Protein 70 (Hsp70). “Noviomimetics” replace the synthetically complex noviose sugar with a simple cyclohexyl moiety to maintain biological efficacy as compared to novologues KU-596 and KU-32. In this study, we further explore the development of noviomimetics and evaluate their efficacy using a luciferase refolding assay, immunoblot analysis, a c-jun assay, and an assay measuring mitochondrial bioenergetics. These new noviomimetics were designed and synthesized and found to induce Hsp70 and improve biological activity. Noviomimetics 39e and 40a were found to induce Hsp70 and exhibit promising effects in cellular assays.
SPIRO-COMPOUNDS AS S1P MODULATORS
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Page/Page column 48; 49, (2018/05/24)
The invention relates to heterocyclic compounds of formula (I) as SIP modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment or alleviation of diseases or disorders mediated by an SIP receptor.
Functional group manoeuvring for tuning stability and reactivity: Synthesis of cicerfuran, moracins (D, E, M) and chromene-fused benzofuran-based natural products
Rao, Maddali L. N.,Murty, Venneti N.,Nand, Sachchida
, p. 9415 - 9423 (2017/11/23)
The protecting group manoeuvring as a strategy was applied for tuning the stability and reactivity of 4-(2,2-dibromovinyl)benzene-1,3-diol (12a) and 6-(2,2-dibromovinyl)-2,2-dimethylchroman-7-ol (22) in the domino synthesis of benzofuran-based natural products (1-8). The functional group demands and their impact on the reactivity driven by electronic effects were successfully managed by varying the protecting groups with substituted gem-dibromovinylphenols in domino couplings and triarylbismuth reagents under palladium-catalyzed conditions. This approach paved the way for the synthesis of moracin M (1) and cicerfuran (2), and the first time synthesis of moracin D (3) and moracin E (4) along with chromene-fused benzofuran-based natural products (5-8) in overall good yields.
Semicarbazone derivatives and use thereof
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Paragraph 0437; 0438; 0439; 0440, (2017/08/14)
The invention belongs to the technical field of medicine, and relates to semicarbazone derivatives disclosed as general formula I, and geometrical isomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein the substituent groups M, R1, R2, R and n are defined in the specification. The invention also relates to a method for preparing compounds disclosed as Formula I, a pharmaceutical composition containing the compounds and application of the compounds and pharmaceutical composition in preparing drugs for treating and/or preventing cancers and other hyperplastic diseases.
Benzofuran compound and its preparation, use (by machine translation)
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Paragraph 0054-0055, (2017/08/18)
The invention relates to a benzofuran compound and its preparation, use, its structural formula such as formula (I) as shown: Wherein R1 , R2 , R4 Are selected from hydrogen, C1 - C5 Alkyl, nitro, halogen, ester, hydroxy, amino, amide base or alkoxyl; R3 Hydrogen, C1 - C5 Alkyl, benzyl, aromatic or heteroaromatic group. The invention also relates to the benzofuran compounds in inhibiting the application of gram-positive to be used repeatedly. The invention relates to 3 - oxime substituted benzene and furan structure aromatic ring as the center, the establishment and optimize the preparation method of the compound, and on the preparation of novel compound of the bacteriostatic screening experiment, through initial bacteriostatic test to confirm that preparation compound has broad-spectrum bacteriostatic activity. (by machine translation)
