- A conformational and structure-activity relationship study of cytotoxic 3,5-bis(arylidene)-4-piperidones and related N-acryloyl analogues
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A series of 3,5-bis(arylidene)-4-piperidones 1 and related N-acryloyl analogues 2 were prepared as candidate cytotoxic agents with a view to discerning those structural features which contributed to bioactivity. A number of the compounds were markedly cytotoxic toward murine P388 and L1210 leukemic cells and also to human Molt 4/C8 and CEM neoplasms. Approximately 40% of the IC50 values generated were lower than the figures obtained for melphalan. In virtually all cases, the N-acyl compounds were significantly more bioactive than the analogues 1. In general, structure - activity relationships revealed that the cytotoxicity of series 1 was correlated positively with the size of the aryl substituents, while in series 2, a -σ relationship was established. In particular, various angles and interatomic distances were obtained by molecular modeling, and the presence of an acryloyl group on the piperidyl nitrogen atom in series 2 affected the relative locations of the two aryl rings. This observation, along with some differences in distances between various atoms in series 1 and 2, may have contributed to the disparity in cytotoxicity between 1 and 2. The results obtained by X-ray crystallography of representative compounds were mainly in accordance with the observations noted by molecular modeling. Selected compounds interfered with the biosynthesis of DNA, RNA, and protein in murine L1210 cells, while others were shown to cause apoptosis in the human Jurkat leukemic cell line. This study has revealed the potential of these molecules for development as cytotoxic and anticancer agents.
- Dimmock,Padmanilayam,Puthucode,Nazarali,Motaganahalli,Zello,Quail,Oloo,Kraatz,Prisciak,Allen,Santos,Balzarini,De Clercq,Manavathu
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Read Online
- Design, synthesis and tumour-selective toxicity of novel 1-[3-{3,5-bis(Benzylidene)-4-oxo-1-piperidino}-3-oxopropyl]-4-piperidone oximes and related quaternary ammonium salts
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A novel series of 1-[3-{3,5-bis(benzylidene)-4-oxo-1-piperidino}-3-oxopropyl]-4-piperidone oximes 3a–h and related quaternary ammonium salts 4a–h were prepared as candidate antineoplastic agents. Evaluation against neoplastic Ca9-22, HSC-2 and HSC-4 cells
- Aguilera, Renato J.,Amano, Shigeru,Balderrama, Karol S.,Contreras, Lisett,Das, Umashankar,Dimmock, Jonathan R.,Roayapalley, Praveen K.,Sakagami, Hiroshi,Sharma, Rajendra K.
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- Application of monocarbonyl curcumin compound in preparation of medicine for preventing and treating periodontitis
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The invention belongs to the technical field of medicines, and particularly relates to application of a specific monocarbonyl curcumin analogue in preparation of a medicine for preventing and treating periodontitis. Experiments prove that the monocarbonyl curcumin analogues not only can play a better anti-oxidation protection role by activating an Nrf2/HO-1 signal channel, but also can play an anti-inflammatory role by inhibiting release of inflammatory factors TNF alpha and IL1-beta, so that the monocarbonyl curcumin analogues have a remarkable prevention and treatment effect on rat periodontitis, have good potential value and significance for prevention and treatment of periodontitis, and have a good research and development prospect.
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Paragraph 0024-0026; 0032
(2021/06/22)
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- Novel hybrid molecules of 3,5-bis(benzylidene)-4-piperidones and dichloroacetic acid which demonstrate potent tumour-selective cytotoxicity
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A novel class of hybrid molecules 2a-o was designed as candidate antineoplastic agents from dichloroacetic acid which is a known inhibitor of pyruvate dehydrogenase kinase and a number of cytotoxic 3,5-bis(benzylidene)-4-piperidones 1. In general these new hybrid molecules are potent cytotoxins towards human HCT116 colon cancer cells. A number of lead molecules emerged having the IC50 values in the double digit nanomolar range. Most of these compounds are less toxic to human CRL1790 non-malignant colon cells and hence the selectivity index (SI) figures for most of the compounds are huge; in the case of 2c-g, m, n, the SI values are in excess of 100. Compounds 2g, 2j, 2m and 2n displayed >100-fold higher potency than the reference drug 5-FU. Quantitative structure-activity relationships revealed that the potencies of the compounds in series 2 increase as the magnitude of the Hammett σ and Taft σ* values rise. X-ray crystallographic of a representative compound 2c revealed various structural features which may influence cytotoxic potencies. Several representative compounds lowered the mitochondrial membrane potential and increased the production of reactive oxygen species in HCT116 cells. A minimal effect was noted in altering the percentage of cells in different phases of the cell cycle. Some future directions have been outlined for analog development.
- Hossain, Mohammad,Das, Swagatika,Das, Umashankar,Doroudi, Alireza,Zhu, Jianfeng,Dimmock, Jonathan R.
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supporting information
(2020/01/03)
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- [Bmim]br accelerated one-pot three-component cascade protocol for the construction of spirooxindole?pyrrolidine heterocyclic hybrids
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Our synthetic approach for the assembly of structurally complex spirooxindole heterocyclic hybrids was based on an ionic liquid, [bmim]Br mediated one-pot three-component cascade reaction strategy involving 1,3-dipolar cycloaddition reaction of N-1-(2-pyridinylmethyl)-3, 5-bis[(E)-arylmethylidene]tetrahydro-4(1H)-pyridinones and azomethine ylide generated in situ from isatin and L-phenyl alanine, affording a series of spirooxindole–pyrrolidine heterocyclic hybrids in good-to-excellent yields. In addition to serving as the reaction medium, [bmim]Br also functioned as a catalyst in this cycloaddition reaction and hence accelerated the reaction rate affording the cycloadducts in short reaction time.
- Al-Thamili, Dhaifallah M.,Almansour, Abdulrahman I.,Arumugam, Natarajan,Dege, Necmi,Kumar, Raju Suresh
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- INHIBITORS OF THE WNT/BETA-CATENIN PATHWAY
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The present disclosure relates to compounds that are capable of modulating the WNT/Beta-Catenin pathway. The disclosure further relates to methods of treating colorectal cancer and other WNT/Beta-Catenin mediated cancers.
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Page/Page column 46
(2019/08/26)
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- Highly functionalized 2-amino-4H-pyrans as potent cholinesterase inhibitors
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Novel highly functionalized 2-amino-4H-pyrans were achieved in excellent yields under simple grinding at ambient temperature and were assessed for their potential for treating Alzheimer's disease (AD). The 2-amino-4H-pyran bearing nitro groups on both the aryl rings showed the highest activity, with an IC50 of 1.98 ± 0.09 μM against acetylcholinesterase (AChE) and 10.62 ± 0.21 μM against butyrylcholinesterase (BChE), the inhibition mechanisms on AChE and BChE receptors were revealed by means of molecular docking simulations.
- Kumar, Raju Suresh,Almansour, Abdulrahman I.,Arumugam, Natarajan,Al-thamili, Dhaifallah M.,Basiri, Alireza,Kotresha,Manohar, Thota Sai,Venketesh,Asad, Mohammad,Asiri, Abdullah M.
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p. 134 - 143
(2018/08/21)
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- Design and synthesis of new piperidone grafted acetylcholinesterase inhibitors
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Alzheimer's disease (AD) is a neurodegenerative disorder affecting 35?million people worldwide. A common strategy to improve the well-being of AD patients consists on the inhibition of acetylcholinesterase with the concomitant increase of the neurotransmitter acetylcholine at cholinergic synapses. Two series of unreported N-benzylpiperidines 5(a–h) and thiazolopyrimidines 9(a–q) molecules were synthesized and evaluated in vitro for their acetylcholinesterase (AChE) inhibitory activities. Among the newly synthesized compounds, 5h, 9h, 9j, and 9p displayed higher AChE enzyme inhibitory activities than the standard drug, galantamine, with IC50values of 0.83, 0.98, and 0.73?μM, respectively. Cytotoxicity studies of 5h, 9h, 9j, 9n and 9p on human neuroblastoma cells SH-SY5Y, showed no toxicity up to 40?μM concentration. Molecular docking simulations of the active compounds 5h and 9p disclosed the crucial role of π-π-stacking in their binding interaction to the active site AChE enzyme. The presented compounds have potential as AChE inhibitors and potential AD drugs.
- Basiri, Alireza,Xiao, Michelle,McCarthy, Alec,Dutta, Debashis,Byrareddy, Siddappa N.,Conda-Sheridan, Martin
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p. 228 - 231
(2016/12/27)
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- Synthesis and antiproliferative activity of cyclic arylidene ketones: a direct comparison of monobenzylidene and dibenzylidene derivatives
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Abstract To give further insight into the influence of the structural modifications of enones and dienones on their antiproliferative properties, 25 derivatives of enones: (E)-2-benzylidene-1-cyclohexanones, (E)-2-benzylidene-1-tetralones, (E)-2-benzylidene-1-indanone, and dienones: (E,E)-2,5- or 2,6-dibenzylidene-1-cyclanones, (E,E)-3,5-dibenzylidene-4-piperidones were synthesized using a newly developed "one-pot" synthetic method. Due to the fact that all of them have the same aryl substituents (phenyl or 4-chlorophenyl) in the arylidene moiety, it is possible to compare the relevant contribution of the single-point structural modifications (type of ring or N-substitution) on their potency on the basis of their IC 50 values. Their antiproliferative activity was evaluated against the following four human adherent cancer cell lines: HeLa, A431, A2780, and MCF7. The cytotoxicity screen has revealed that the dibenzylidene dienones in general dominate the monobenzylidene enones in this respect. The nitrogen-containing heterocyclic dienones at the same time displayed higher inhibitory properties toward these human carcinoma cell lines compared with their homocyclic dienone analogs. One of the eight newly prepared 4-piperidone derivatives, N-(γ-oxobutyl)-(E,E)-3,5-bis(p-chlorobenzylidene)-4-piperidone is as potent a cell growth inhibitor (IC 50 of 0.438-1.409 μM) as the N-methyl-(E,E)-3,5-bis(p-chlorobenzylidene)-4-piperidone (IC 50 of 0.447-1.048 μM), one of the most active among the previously described compounds in this series. Catalytic hydrogen-transfer isomerization of compounds with two exocyclic benzylidene double bonds to derivatives with endocyclic double bonds results in the complete loss of antiproliferative activity. The structural modifications and 50 % inhibitory concentration (IC 50) values resulted in correlations which can promote the design of more potent derivatives of the 4-piperidone dienones.
- Huber, Imre,Zupk, Istvn,Kovcs, Ida J.,Minorics, Renta,Gulys-Fekete, Gergely,Masz, Gbor,Perjsi, Pl
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p. 973 - 981
(2015/02/19)
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- An expedient synthesis, acetylcholinesterase inhibitory activity, and molecular modeling study of highly functionalized hexahydro-1,6-naphthyridines
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A series of hexahydro-1,6-naphthyridines were synthesized in good yields by the reaction of 3,5-bis[(E)-arylmethylidene] tetrahydro-4(1H)-pyridinones with cyanoacetamide in the presence of sodium ethoxide under simple mixing at ambient temperature for 6-10 minutes and were assayed for their acetylcholinesterase (AChE) inhibitory activity using colorimetric Ellman's method. Compound 4e with methoxy substituent at ortho-position of the phenyl rings displayed the maximum inhibitory activity with IC50 value of 2.12 μM. Molecular modeling simulation of 4e was performed using three-dimensional structure of Torpedo californica AChE (TcAChE) enzyme to disclose binding interaction and orientation of this molecule into the active site gorge of the receptor.
- Almansour, Abdulrahman I.,Kumar, Raju Suresh,Arumugam, Natarajan,Basiri, Alireza,Kia, Yalda,Ali, Mohamed Ashraf
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- Ionic liquid mediated synthesis of mono- and bis-spirooxindole- hexahydropyrrolidines as cholinesterase inhibitors and their molecular docking studies
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One pot, three-component reaction of 1-acryloyl-3,5- bisarylmethylidenepiperidin-4-ones with isatin and sarcosine in molar ratios of 1:1:1 and 1:2:2 furnished to mono- and bis-spiropyrrolidine heterocyclic hybrids comprising functionalized piperidine, pyrrolidine and oxindole structural motifs. Both mono and bis-spiropyrrolidines displayed good inhibitory activity against acetylcholinesterase (AChE) with IC50 values of 2.36-9.43 μM. For butyrylcholinesterase (BChE), mono-cycloadducts in series 8 with IC50 values of lower than 10 μM displayed better inhibitory activities than their bis-cycloadduct analogs in series 9 with IC50 values of 7.44-19.12 μM. The cycloadducts 9j and 8e were found to be the most potent AChE and BChE inhibitors with IC50 values of 2.35 and 3.21 μM, respectively. Compound 9j was found to be competitive inhibitor of AChE while compound 8e was a mixed-mode inhibitor of BChE with calculated K i values of 2.01 and 6.76 μM, respectively. Molecular docking on Torpedo californica AChE and human BChE showed good correlation between IC 50 values and free binding energy values of the synthesized compounds docked into the active site of the enzymes.
- Kia, Yalda,Osman, Hasnah,Kumar, Raju Suresh,Basiri, Alireza,Murugaiyah, Vikneswaran
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p. 1318 - 1328
(2014/03/21)
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- Cholinesterase inhibitory activity versus aromatic core multiplicity: A facile green synthesis and molecular docking study of novel piperidone embedded thiazolopyrimidines
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Novel thiazolopyrimidine derivatives have been synthesized via microwave assisted, domino cascade methodology in ionic liquid and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. Among the newly synthesized compounds 6d, 6a, 6e and 6b displayed higher AChE inhibitory activity than standard drug, galanthamine, with IC 50 values of 0.53, 1.47, 1.62 and 2.05 μM, respectively. Interestingly, all the compounds except for 6m-r and 6x displayed higher BChE inhibitory potentials than galanthamine with IC50 values ranging from 1.09 to 18.56 μM. Molecular docking simulations for 6d possessing the most potent AChE and BChE inhibitory activities, disclosed its binding interactions at the active site gorge of AChE and BChE enzymes.
- Basiri, Alireza,Murugaiyah, Vikneswaran,Osman, Hasnah,Kumar, Raju Suresh,Kia, Yalda,Hooda, Alysha,Parsons, Richard B.
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p. 906 - 916
(2014/01/23)
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- An efficient ionic liquid mediated synthesis, cholinesterase inhibitory activity and molecular modeling study of novel piperidone embedded α,β-unsaturated ketones
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A series of hitherto unreported piperidone embedded α,β- unsaturated ketones were synthesized efficiently in ionic solvent and evaluated for cholinesterase inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Most of the synthesized compounds displayed good enzyme inhibition; therein compounds 7i and 7f displayed significant activity against AChE with IC50 values of 1.47 and 1.74 μM, respectively. Compound 6g showed the highest BChE inhibitory potency with IC50 value of 3.41 μM, being 5 times more potent than galanthamine. Molecular modeling simulation was performed using AChE and BChE receptors extracted from crystal structure of human AChE and human BChE to determine the amino acid residues involved in the binding interaction of synthesized compounds and their relevant receptors.
- Kia, Yalda,Osman, Hasnah,Kumar, Raju Suresh,Murugaiyah, Vikneswaran,Basiri, Alireza,Khaw, Kooi Yeong,Rosli, Mohd. Mustaqim
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p. 512 - 520
(2014/06/23)
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- C5-curcuminoid-dithiocarbamate based molecular hybrids: Synthesis and anti-inflammatory and anti-cancer activity evaluation
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A series of C5-curcumin bearing morpholine based dithiocarbamates was synthesized. Molinspiration and Osiris software were used for theoretical prediction of physico-chemical properties of these molecules and the majority of the hybrids showed theoretical physico-chemical properties similar or better than curcumin. These hybrids (4a-4v) were evaluated for in vitro cytotoxicity on chronic myeloid leukemia (KBM5) and colon cancer (HCT116) cell lines, and down modulation of TNF-α-induced NF-κB activation at 5 μM. Most of the hybrids exhibit higher cytotoxicity against KBM5 cells compared to HCT116 cell lines. Further, all the hybrids showed potential to suppress the TNF-α-induced NF-κB activation at 5 μM KBM5 cells and seventeen hybrids have shown higher potential to inhibit NF-κB activation in comparison to curcumin.
- Anthwal, Amit,Singh, Kundan,Rawat,Tyagi, Amit K.,Aggarwal, Bharat B.,Rawat, Diwan S.
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p. 28756 - 28764
(2014/07/22)
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- Facile, regio- And diastereoselective synthesis of spiro-pyrrolidine and pyrrolizine derivatives and evaluation of their antiproliferative activities
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A number of novel spiro-pyrrolidines/pyrrolizines derivatives were synthesized through [3+2]-cycloaddition of azomethine ylides with 3,5-bis[(E)- Arylmethylidene]tetrahydro-4(1H)-pyridinones 2a-n. Azomethine ylides were generated in situ from the reaction of 1H-indole-2,3-dione (isatin, 3) with N-methylglycine (sarcosine), phenylglycine, or proline. All compounds (50 μM) were evaluated for their antiproliferative activity against human breast carcinoma (MDA-MB-231), leukemia lymphoblastic (CCRF-CEM), and ovarian carcinoma (SK-OV-3) cells. N-α-Phenyl substituted spiro-pyrrolidine derivatives (5a-n) showed higher antiproliferative activity in MDA-MB-231 than other cancer cell lines. Among spiro-pyrrolizines 6a-n, a number of derivatives including 6a-c and 6i-m showed a comparable activity with doxorubicin in all three cell lines. Among all compounds in three classes, 6a, 6b, and 6m, were found to be the most potent derivatives showing 64%, 87%, and 74% antiproliferative activity in MDA-MB-231, SK-OV-3, and CCRF-CEM cells, respectively. Compound 6b showed an IC50 value of 3.6 μM in CCRF-CEM cells. These data suggest the potential antiproliferative activity of spiro-pyrrolidines/pyrrolizines.
- Almansour, Abdulrahman I.,Kumar, Raju Suresh,Beevi, Farzana,Shirazi, Amir Nasrolahi,Osman, Hasnah,Ismail, Rusli,Choon, Tan Soo,Sullivan, Brian,McCaffrey, Kellen,Nahhas, Alaa,Parang, Keykavous,Ali, Mohamed Ashraf
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p. 10033 - 10055
(2014/08/05)
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- Synthesis and discovery of novel piperidone-grafted mono- and bis-spirooxindole-hexahydropyrrolizines as potent cholinesterase inhibitors
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Three-component reaction of a series of 1-acryloyl-3,5- bisbenzylidenepiperidin-4-ones with isatin and l-proline in 1:1:1 and 1:2:2 molar ratios in methanol afforded, respectively the piperidone-grafted novel mono- and bisspiro heterocyclic hybrids comprising functionalized piperidine, pyrrolizine and oxindole ring systems in good yields. The in vitro evaluation of cholinesterase enzymes inhibitory activity of these cycloadducts disclosed that monospiripyrrolizines (8a-k), are more active with IC50 ranging from 3.36 to 20.07 μM than either the dipolarophiles (5a-k) or bisspiropyrrolizines (9a-k). The compounds, 8i and 8e with IC50 values of 3.36 and 3.50 μM, respectively showed the maximum inhibition of acethylcholinesterase (AChE) and butrylylcholinestrase (BuChE). Molecular modeling simulation, disclosed the binding interactions of the most active compounds to the active site residues of their respective enzymes. The docking results were in accordance with the IC50 values obtained from in vitro cholinesterase assay.
- Kia, Yalda,Osman, Hasnah,Kumar, Raju Suresh,Murugaiyah, Vikneswaran,Basiri, Alireza,Perumal, Subbu,Wahab, Habibah A.,Bing, Choi Sy
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p. 1696 - 1707
(2013/05/08)
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- A facile chemo-, regio- and stereoselective synthesis and cholinesterase inhibitory activity of spirooxindole-pyrrolizine-piperidine hybrids
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A series of novel hybrid spiro heterocycles comprising pyrrolizine, spiroxindole and piperidine moieties was synthesized chemo-, regio- and stereoselectively in good yields from 1,3-dipolar cycloaddition reaction of a series of 1-acryloyl-3,5-bisarylmethylidenepiperidin-4-ones with azomethine ylides generated in situ from 5-choloroisatin and l-proline in methanol. These cycloadducts displayed significant cholinesterase inhibitory activity. Among the compounds screened, 8g and 8e, showed maximum inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinestrase (BChE) with IC50 values of 3.33 and 3.13 μM, respectively.
- Kia, Yalda,Osman, Hasnah,Kumar, Raju Suresh,Murugaiyah, Vikneswaran,Basiri, Alireza,Perumal, Subbu,Razak, Ibrahim Abdul
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p. 2979 - 2983
(2013/06/26)
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- Bis[3,5-bis(benzylidene)-4-oxo-1-piperidinyl]amides: A Novel Class of Potent Cytotoxins
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The principal objective of this study was the examination of the theory of cytotoxic synergism. In this exploratory study, we tested the hypothesis that doubling the number of sites available for thiol alkylation in a series of candidate cytotoxins increases potency more than two-fold. This concept was verified in one-third of our comparisons using human Molt 4/C8 and CEM T-lymphocytes and murine L1210 cells. In addition, the significant potencies of various members of our compound series justified further studies. Molecular modeling revealed that relative locations of the amidic groups correlate with cytotoxicity. A potent cytotoxic compound, 1,2-bis(3,5-dibenzylidene-4-oxo-piperidin-1-yl)ethane-1,2-dione (1a) inhibited the growth of a large number of human tumor cell lines and displayed greater toxicity toward certain non-adherent cells than toward adherent neoplasms or fibroblasts. The mode of action of 1a includes induction of apoptosis and necrosis.
- Das, Swagatika,Das, Umashankar,Varela-Ramirez, Armando,Lema, Carolina,Aguilera, Renato J.,Balzarini, Jan,DeClercq, Erik,Dimmock, Stephen G.,Gorecki, Dennis K. J.,Dimmock, Jonathan R.
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scheme or table
p. 1892 - 1899
(2012/07/03)
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- A facile three-component [3+2]-cycloaddition/annulation domino protocol for the regio- and diastereoselective synthesis of novel penta- and hexacyclic cage systems, involving the generation of two heterocyclic rings and five contiguous stereocenters
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An expedient, three-component, [3+2]-cycloaddition/annulation domino protocol for the synthesis of a series of cage penta- and hexacyclic compounds in good to excellent yields is described. The ring systems thus generated contain as structural elements bridged, fused and spiro rings and were obtained with complete selectivity through the creation of two C-C and two C-N bonds, which led to the generation of two azaheterocyclic rings, four carbon and one nitrogen adjacent stereocentres, three of which are quaternary.
- Suresh Kumar, Raju,Osman, Hasnah,Perumal, Subbu,Menéndez, J. Carlos,Ashraf Ali, Mohamed,Ismail, Rusli,Soo Choon, Tan
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body text
p. 3132 - 3139
(2011/05/06)
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- Curcumin analogues as possible anti-proliferative & anti-inflammatory agents
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A series of novel curcumin analogues has been designed, synthesized and tested in vitro/in vivo as potential multi-target agents. Their anti-proliferative and anti-inflammatory activities were studied. Compounds 1b and 2b were stronger inhibitors of soybean lipoxygenase (LOX) than curcumin. Analogue 1b was also the most potent aldose reductase (ALR2) inhibitor. Two compounds, (1a and 1f) exhibited in vivo anti-inflammatory activity comparable to that of indomethacin, whereas derivative 1i exhibited even higher activity. The derivatives were also tested for their anti-proliferative activity using three different human cancer cell lines. Compounds 1a, 1b, 1d and 2b exhibited significant growth inhibitory activity as compared to curcumin, against all three cancer cell lines. Lipophilicity was determined as RM values using RPTLC and theoretically. The results are discussed in terms of the structural characteristics of the compounds. Docking simulations were performed on LOX and ALR2 inhibitor 1b and curcumin. Compound 1b is well fitted in the active site of ALR2, binding to the ALR2 enzyme in a similar way to curcumin. Allosteric interactions may govern the LOX-inhibitor binding.
- Katsori,Chatzopoulou,Dimas,Kontogiorgis,Patsilinakos,Trangas,Hadjipavlou-Litina
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experimental part
p. 2722 - 2735
(2011/07/29)
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- A highly efficient method for solvent-free synthesis of bis(arylmethylidene)piperidinones
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(Chemical Equation Presented) A remarkably efficient double crossed aldol condensation of piperidin-4-one with various aromatic aldehydes is described at room temperature in the presence of diethylamine and lithium perchlorate under solvent-free condition
- Abaee, M. Saeed,Mojtahedi, Mohammad M.,Sharifi, Roholah,Zahedi, M. Mehdi
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p. 1497 - 1499
(2008/09/18)
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- ANTINEOPLASTIC COMPOUNDS
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The present invention relates to 4-piperidone derivatives represented by the following formula (I) and the acid addition salts thereof. The method of preparation and antineoplastic activity of the said compounds are disclosed. A number of the compounds po
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Page/Page column 13-14
(2008/06/13)
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- 2-Amino-8-arylideno-3,4,5,6,7,8-hexahydro-4-arlypyrido[4,3-d]pyrimidines
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Compounds of the formula STR1 and the pharmaceutically acceptable acid-addition salts thereof wherein R1 and R2 are hydrogen or alkyl of 1 to 4 carbons; R is hydrogen, alkyl of 1 to 4 carbons, alkanoyl of 2 to 5 carbons, or STR2 WHER
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- 2-(2,2,2,-Trifluoroethyl)-3,3a,4,5,6,7-hexahydro-2H-pyrazolo[4,3-c]pyridines
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Antiinflammatory activity is demonstrated by compounds having the formula STR1 wherein R1 is hydrogen, chloro, fluoro, alkyl, alkoxy or trifluoromethyl and R2 is hydrogen, alkyl, arylalkyl, hydroxyalkyl, or carboximidamide, or pharma
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- 5-Substituted-pyrazolo(4,3-c)pyridines
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Compounds of the formula SPC1 Their N-oxides and acid addition salts thereof are provided which have been found to possess anti-inflammatory activity. In addition, methods for preparing such compounds, pharmaceutical compositions containing such compounds
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