- A new method for the synthesis of chalcone derivatives promoted by PPh3/I2under non-alkaline conditions
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A straightforward and general method has been developed for the synthesis of chalcone derivatives by a Claisen-Schmidt reaction in the presence of PPh3/I2 in 1,4-dioxane under reflux temperatures. With the condensation of the aromatic ketone and aldehyde occurring at non-strongly alkaline conditions, our proposed method significantly expands the range of applicable substrates, especially for groups that are unstable under alkaline conditions.
- Xue, Kangsheng,Sun, Guoxiang,Zhang, Yanzhi,Chen, Xubing,Zhou, Yang,Hou, Jinjun,Long, Huali,Zhang, Zijia,Lei, Min,Wu, Wanying
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- Synthesis, Characterisation, Molecular Docking, Anti-microbial and Anti-diabetic Screening of Substituted 4-indolylphenyl-6-arylpyrimidine-2-imine Derivatives
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The purpose of the research is to synthesise a novel series of (E)-2-(4-(1H-indol-3-yl)-6-p-substituted phenylpyrimidin-2-yl)dimethylguanidine derivatives since 3-(1H-indol-3-yl)-1-p-substituted phenylprop-2-en-1-one and evaluate their molecular docking s
- Ramya, Veerasamy,Vembu, Santhirakasu,Ariharasivakumar, Ganesan,Gopalakrishnan, Manathusamy
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- Synthesis, docking, and evaluation of novel thiazoles for potent antidiabetic activity
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In this study, a series of novel substituted pyrazoles containing indole and thiazole motifs were synthesized and evaluated for their antihyperglycemic activity against α-amylase and α-glucosidase enzymes. Among them, 2-(5-(1H-indol-3-yl)-3-phenyl-1H-pyra
- Sravanthi,Sajitha Lulu,Vino,Jayasri,Mohanapriya,Manju
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- Synthesis and antioxidant activity of a new class of pyrazolyl indoles, thiazolyl pyrazolyl indoles
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A new class of bis and tris heterocycles–pyrazolyl indoles and thiazolyl pyrazolyl indoles were prepared from the Michael acceptor (E)-3-(1H-indol-3-yl)-1-arylprop-2-en-1-ones by ultrasound irradiation technique and tested for antioxidant activity. The th
- Ummadi, Nagarjuna,Gundala, Sravya,Venkatapuram, Padmavathi,Adivireddy, Padmaja
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- Synthesis and evaluation of chalcone derivatives as novel sunscreen agent
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Ultraviolet (UV) irradiation is a serious problem for skin health thus the interest in the research to develop sunscreen agent has been increasing. Chalcone is a promising compound to be developed as its chromophore absorbs in the UV region. Therefore, in
- Jumina, Jumina,Lee, Wonkoo,Swasono, Respati Tri,Wijayanti, Lucia Wiwid
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- Synthesis and carbonic anhydrase inhibition studies of sulfonamide based indole-1,2,3-triazole chalcone hybrids
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Sulfonamide is one of the most promising classes of classical carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. A novel series of indolylchalcones incorporating benzenesulfonamide-1,2,3-triazole (6a-q) has been synthesized by click chemistry reaction and in
- Angeli, Andrea,Arifuddin, Mohammed,Purnachander Yadav, P.,Sigalapalli, Dilep Kumar,Singh, Priti,Supuran, Claudiu T.,Swain, Baijayantimala,Thacker, Pavitra S.
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- Alpha,beta-unsaturated ketone derivatives, preparation method of derivatives and application of derivatives as medicines
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The invention relates to the technical field of medicine, and proposes alpha,beta-unsaturated ketone derivatives and a preparation method thereof. The derivatives have a structural general formula represented by a formula I shown in the specification, whe
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Paragraph 0135-0137
(2019/12/15)
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- Preheated fly-ash catalyzed aldol condensation: Efficient synthesis of chalcones and antimicrobial activities of some 3-thienyl chalcones
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In the present study we have prepared a series of some chalcones using solvent - free Aldol - condensation by microwave irradiation. The yields of the ketones are more than 60%. The synthesised chalcones were characterized by their analytical, physical and spectral data. The antimicrobial activities of substituted styryl 3-thienyl ketones have been studied using Bauer-Kirby method.
- Arulkumaran, Ranganathan,Vijayakumar, Sambandhamoorthy,Sakthinathan, S. Pazhanivel,Kamalakkannan, Dakshnamoorthy,Ranganathan, Kaliyaperumal,Suresh, Ramamoorthy,Sundararajan, Rajasekaran,Vanangamudi, Ganesan,Thirunarayanan, Ganesamoorthy
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p. 1684 - 1690
(2013/09/24)
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- An efficient method for the synthesis of isoxazolines under microwave irradiation and solvent-free conditions
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A facile method for the synthesis of new isoxazoline derivatives are being reported starting from substituted 1-(1H-indol-3-yl)-3-(substituted aryl)-prop-1-en-3-ones and hydroxylamine hydrochloride under solvent free conditions and microwave irradiation.
- Patil, Pravin O.,Bari, Sanjay B.
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p. 3588 - 3590
(2013/04/24)
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- Csp2-Csp2 bond formation via Lewis acid/ammonium salt cocatalyzed tandem addition and oxidative dehydrogenation strategy: Alkenylation of indoles with α,β-unsaturated ketones
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The alkenylation of indoles with α,β-unsaturated ketones through a tandem addition and oxidative dehydrogenation strategy has been developed. This method provides an alternative approach for C3 alkenylation of indoles with α,β-unsaturated ketones. Using inexpensive and readily available BF3·Et2O and an ammonium salt as the efficient cocatalyst constitutes the attractive advantage of this reaction.
- Xiang, Shi-Kai,Wu, Guolin,Zhang, Bo,Cui, Yuxin,Jiao, Ning
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supporting information; experimental part
p. 3802 - 3804
(2012/09/21)
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- Fly-ash:H2SO4 catalyzed solvent free efficient synthesis of some aryl chalcones under microwave irradiation
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Some 2E aryl chalcones have been synthesized using greener catalyst Fly-ash:H2SO4 assisted solvent free environmentally benign Crossed-Aldol reaction. The yields of chalcones are more than 90%. The synthesized chalcones are characterized by their physical constants and spectral data.
- Thirunarayanan,Mayavel,Thirumurthy
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experimental part
p. 18 - 22
(2012/05/05)
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- Synthesis and evaluation of indole-based chalcones as inducers of methuosis, a novel type of nonapoptotic cell death
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Methuosis is a novel caspase-independent form of cell death in which massive accumulation of vacuoles derived from macropinosomes ultimately causes cells to detach from the substratum and rupture. We recently described a chalcone-like compound, 3-(2-methyl-1H-indol-3-yl)-1-(4-pyridinyl)-2-propen-1- one (i.e., MIPP), which can induce methuosis in glioblastoma and other types of cancer cells. Herein, we describe the synthesis and structure-activity relationships of a directed library of related compounds, providing insights into the contributions of the two aryl ring systems and highlighting a potent derivative, 3-(5-methoxy, 2-methyl-1H-indol-3-yl)-1-(4-pyridinyl)-2-propen-1-one (i.e., MOMIPP) that can induce methuosis at low micromolar concentrations. We have also generated biologically active azide derivatives that may be useful for future studies aimed at identifying the protein targets of MOMIPP by photoaffinity labeling techniques. The potential significance of these studies is underscored by the finding that MOMIPP effectively reduces the growth and viability of Temozolomide-resistant glioblastoma and doxorubicin-resistant breast cancer cells. Thus, it may serve as a prototype for drugs that could be used to trigger death by methuosis in cancers that are resistant to conventional forms of cell death (e.g., apoptosis).
- Robinson, Michael W.,Overmeyer, Jean H.,Young, Ashley M.,Erhardt, Paul W.,Maltese, William A.
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experimental part
p. 1940 - 1956
(2012/05/20)
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- Solvent effect profiles of absorbance and fluorescence spectra of some indole based chalcones
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The photophysical properties of a series of 3-(1' H-Indol-3′-yl)-1- phenylprop-2-en-1-one and its derivatives (indole chalcones) were studied in different solvents. Solvent effects on the absorption and fluorescence spectra were quantified using Reichardt
- Saroj, Manju Kumari,Sharma, Neera,Rastogi, Ramesh C.
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experimental part
p. 2213 - 2227
(2012/06/15)
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- Enantioselective conjugate addition of alkenylboronic acids to indole-appended enones
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An enantioselective addition of alkenylboronic acids and alkynylboronic esters to unprotected indole-appended enones is reported. This transformation proceeds with high enantioselectivity and high product yields via the use of catalytic amounts of 3,3′-bis(pentafluorophenyl)-BINOL and Mg(Ot-Bu) 2. A range of α-branched indole derivatives are available from the transformation.
- Lundy, Brian J.,Jansone-Popova, Santa,May, Jeremy A.
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supporting information; experimental part
p. 4958 - 4961
(2011/11/29)
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- Synthesis, antioxidant and DNA cleavage activities of novel indole derivatives
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A new series of novel indole derivatives containing barbitone moiety (5a-i) are synthesized by simple and efficient condensation of chalcones (3a-i) with barbituric acid (4). The synthesized compounds are screened for their antioxidant (free radical scave
- Biradar,Sasidhar,Parveen
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scheme or table
p. 4074 - 4078
(2010/09/18)
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- Design and synthesis of 3-[3-(substituted phenyl)-4-piperidin-1-ylmethyl/- 4-morpholin-4-ylmethyl-4,5-dihydro-isoxazol-5-yl]-1H-indoles as potent anti-inflammatory agents
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The synthesis of new indole derivatives bearing isoxazoline moiety (3a-d and 4a-d) has been described. IR, 1H NMR, and mass spectral data supported the structures of synthesized compounds. The compounds were tested in vivo for their anti-inflam
- Amir, Mohammad,Javed, Sadique Akhtar,Kumar, Harish
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scheme or table
p. 299 - 310
(2011/01/12)
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- 3,5-Diphenylpent-2-enoic acids as allosteric activators of the protein kinase PDK1: Structure-activity relationships and thermodynamic characterization of binding as paradigms for PIF-binding pocket-targeting compounds
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The modulation of protein kinase activities by low molecular weight compounds is a major goal of current pharmaceutical developments. In this line, important efforts are directed to the development of drugs targeting the conserved ATP binding site. Howeve
- Stroba, Adriana,Schaeffer, Francis,Hindie, Valerie,Lopez-Garcia, Laura,Adrian, Iris,Fr?hner, Wolfgang,Hartmann, Rolf W.,Biondi, Ricardo M.,Engel, Matthias
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supporting information; experimental part
p. 4683 - 4693
(2010/02/28)
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- Synthesis of new 2-(5-substituted-3-phenyl-2-pyrazolinyl)-1,3-thiazolino[5,4-b]quinoxaline derivatives and evaluation of their antiamoebic activity
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In an effort to develop potent antiamoebic agents, we have synthesized chalcones (1-8), amino-5-substituted-(3-phenyl(2-pyrazolinyl))methane-1-thione derivatives (1a-8a) and 2-(5-substituted-3-phenyl-2-pyrazolinyl)-1,3-thiazolino[5,4-b]quinoxaline derivat
- Budakoti, Asha,Bhat, Abdul Roouf,Azam, Amir
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experimental part
p. 1317 - 1325
(2009/09/27)
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- Aryl azoles with neuroprotective activity-Parallel synthesis and attempts at target identification
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A parallel synthesis of aryl azoles with neuroprotective activity is described. All compounds obtained were evaluated in an in vitro assay using a NMDA toxicity paradigm showing a neuroprotective activity between 15% and 40%. The potential biological target of the active compounds was investigated by extensive literature searches based around similar scaffolds with reported neuroprotective activity. The most interesting molecules active in the NMDA toxicity assay (3a and 2g) showed moderate but significant activity in the inhibition of the Site 2 Sodium Channel binding assay at 10 μM. To confirm our hypothesis compounds 3a, c, f and 2g were tested in the Veratridine assay which is one of the excitotoxicity assays of revelance to NaV channels. The compounds tested showed an activity between 40% and 70%. The identification of neuroprotective small molecules and the identification of NaV channels as the potential site of action were the most important goals of this work.
- Cocconcelli, Giuseppe,Diodato, Enrica,Caricasole, Andrea,Gaviraghi, Giovanni,Genesio, Eva,Ghiron, Chiara,Magnoni, Letizia,Pecchioli, Elena,Plazzi, Pier Vincenzo,Terstappen, Georg C.
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p. 2043 - 2052
(2008/09/21)
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- Synthesis of substituted indole derivatives as a new class of antimalarial agents
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A series of substituted indole derivatives were synthesized and evaluated for their in vitro antimalarial activity against P. falciparum. Out of the 24 compounds synthesized six compounds have shown MIC of 1 μg/mL. These compounds are in vitro several fol
- Agarwal, Anu,Srivastava, Kumkum,Puri,Chauhan, Prem M.S.
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p. 3133 - 3136
(2007/10/03)
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- Substituted pyrazolines and their cardiovascular activity
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1-Thiocarbamoyl-3, 5-diphenyl-2-pyrazolines 4 and 5 have been prepared by cyclization of 1,3-diphenyl-2-propene-1 ones (chalcones) 3 with thiosemicarbazide in the presence of sodium hydroxide. Reaction of 3 with hydrazine hydrate followed by condensation with aryl isothiocyanates yields 1-N-substituted thiocarbamoyl-3, 5-diphenyl-2-pyrazolines 5. These compounds have been characterized on the basis of elemental analysis, IR, 1H NMR and MS. Compounds have been evaluated for their cardio-vascular activity and toxicity.
- Malhotra, Vineet,Pathak, Seema,Nath, Rajendra,Mukerjee, Devashis,Shanker, Kirpa
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p. 1310 - 1313
(2007/10/03)
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- Nitrones and Oxaziridines. XLII Synthesis of Indol-3-yl Substituted 1-Pyrroline 1-Oxides
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The 1-pyrroline 1-oxides (13), (14), (16) and (18) with indol-3-yl substituents attached to the 2- or 4-positions have been synthesized by reductive cyclization of the related γ-nitro ketones.The corresponding 1-pyrrolines (15), (17) and (19) have also be
- Black, David St.C.,Deb-Das, Renu B.,Kumar, Naresh
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p. 611 - 621
(2007/10/02)
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- SYNTHESIS OF SOME INDOLYL-TRIAZOLYL-PROPANONE AND -PROPANOL DERIVATIVES, I
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3-(3-Indolyl)-3-(1,2,4-triazolyl)-1-phenylpropan-1-ones and -1-ols were synthesized for tests as herbicides.
- Foeldeak, Sandor,Hegyes, Peter,Dombi, Gyoergy
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p. 275 - 280
(2007/10/02)
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