- Novel S-triazine accommodated 5-benzylidino-4-thiazolidinones: Synthesis and in vitro biological evaluations
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In order to explore various pharmacological effects associated with S-triazine accommodated 5-benzylidino-4-thiazolidinones, a series of compounds based on 5-benzylidene-2-[4-(4,6-bis-dimethylamino-[1,3,5]triazin-2-ylamino)-phenylimino]-thiazolidin-4-one
- Rana, Aniruddhasinh M.,Trivedi, Pooja,Desai, Kishor R.,Jauhari, Smita
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Read Online
- A novel series of potent cytotoxic agents targeting G2/M phase of the cell cycle and demonstrating cell killing by apoptosis in human breast cancer cells
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Breast cancer, a leading cause of mortality in women, warrants the development and biological evaluation of new anticancer agents. A novel series of thiopyridine triazine derivatives was synthesized and investigated in the human breast cancer cell line, MDA-MB-468. SM40, the most potent derivative, induced a G2/M arrest and apoptosis with a possible involvement of p53. The cytotoxicity of SM40 was also examined against the NCI 60 cell line panel and its potency was rationalized using molecular modeling. Results suggest that SM40 is a promising cytotoxic agent.
- Mandal, Soma,Berube, Gervais,Asselin, Eric,Mohammad, Iqbal,Richardson, Vernon J.,Gupta, Atul,Pramanik, Saroj K.,Williams, Arthur L.,Mandal, Sanat K.
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- HETEROCYCLIC COMPOUNDS AS MUTANT IDH INHIBITORS
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The present disclosure relates generally to compounds useful in treatment of conditions associated with mutant isocitrate dehydrogenase (mt-IDH), particularly mutant IDH1 enzymes. Specifically, the present invention discloses compound of formula (IA), which exhibits inhibitory activity against mutant IDH1 enzymes. Method of treating conditions associated with excessive activity of mutant IDH1 enzymes with such compound is disclosed. Uses thereof, pharmaceutical composition, and kits are also disclosed.
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Paragraph 0413-0414
(2020/07/16)
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- Glass engineering of aminotriazine-based materials with sub-ambient: T gand high kinetic stability
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A challenge in glass engineering is the design of molecular glasses combining a high glass kinetic stability (GS) of the amorphous phase with a low (sub-ambient) glass transition temperature (Tg). Triazine derivatives with arylamino substituents readily form glassy phases that can show outstanding resistance to crystallization. In the present study, a series of 12 analogous compounds incorporating phenylamino and cyclohexylamino groups was synthesized, and their thermal properties and intermolecular interactions were studied. All compounds possess an excellent glass-forming ability, a low Tg ranging from 32 °C to as low as -19 °C, and a high GS. While the cyclohexyl derivatives show higher Tg, the phenyl derivatives possess a higher GS with some compounds remaining completely amorphous for over three years despite their sub-ambient Tg. X-ray diffraction, infrared spectroscopy and DFT calculations reveal that the higher volume occupancy and rotational energy barrier of cyclohexyl groups are the main factors responsible for the compounds' higher Tg values but that they also contribute to their higher propensity to crystallize. In counterpart, the planarity of phenyl groups leads to poorer packing and enhances their GS while keeping their Tg well below ambient. The formation of hydrogen bonds or competing interactions provides an additional handle to tune the Tg of the compounds. Taken together, these studies provide guidelines for the design of molecular glasses with readily tunable thermal properties in view of their functionalization. This journal is
- Iankovitch, Anna,Jokar, Mahboubeh,Kara Ali, Zeinab,Lebel, Olivier,Maris, Thierry,Pellerin, Christian
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p. 4275 - 4288
(2020/07/10)
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- Synthesis of nitrogen and sulfur-containing synergistic flame retardant compound and preparation method of intercalated modified hydrotalcite thereof
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The invention relates to synthesis of a nitrogen and sulfur-containing synergistic flame retardant compound and a preparation method of intercalated modified hydrotalcite thereof. By means of the "structure memory effect" of hydrotalcite, the compound is introduced into the interlayer of hydrotalcite, thus significantly improving the dispersion performance of a hydrotalcite-based flame retardant and enhancing flame retardance to a polymer matrix. Based on the flame-retardant mechanism and high-efficiency flame-retardant properties peculiar to nitrogen-sulfur compounds, the compound is introduced to the interlayer of hydrotalcite by self-assembly reconstruction to prepare a novel organic-inorganic hybrid flame retardant, thus enhancing the hydrophilic properties of the hydrotalcite surface,and also further enhancing the flame-retardant properties. The prepared nitrogen and sulfur-containing synergistic flame retardant compound intercalated hydrotalcite composite flame retardant can significantly improve the flame-retardant effect after filling in the polymer matrix, and has good application value in improving the flame retardance of polyolefins. The preparation of the nitrogen-sulfur synergistic flame retardant compound is simple and practicable, the reaction conditions are easy to control, and the flame retardant efficiency is high.
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Paragraph 0034-0035; 0037; 0041-0042; 0047-0048
(2019/10/01)
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- Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68)
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G protein-coupled receptor 68 (GPR68) is an understudied orphan G protein-coupled receptor (GPCR). It is expressed most abundantly in the brain, potentially playing important roles in learning and memory. Pharmacological studies with GPR68 have been hinde
- Yu, Xufen,Huang, Xi-Ping,Kenakin, Terry P.,Slocum, Samuel T.,Chen, Xin,Martini, Michael L.,Liu, Jing,Jin, Jian
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p. 7557 - 7574
(2019/09/09)
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- Synthesis method and application of naphthalimides derivatives containing cyanuric chloride
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The invention discloses synthesis and application of naphthalimides derivatives containing cyanuric chloride, and belongs to the field of biological organic synthesis. According to the invention, a cyanuric chloride derivative is introduced onto a naphthalimides parent, so that the drug tolerance can be effectively avoided, and an antitumour effect is improved. According to the naphthalimides derivatives containing cyanuric chloride, different cyclic amine groups are used for replacing Br at the tail end of anhydride naphthalene, and the structure-function relationship of pharmaceutical molecules is researched; cyanuric chloride is modified by different aliphatic amine, aromatic amine or alcohol, and the structure-function relationship of pharmaceutical molecules is researched; aminoethylpiperazine is taken as a bridge chain to connect the modified anhydride naphthalene with the naphthalimides derivatives through substitution reaction, and the novel naphthalimides derivatives containing cyanuric chloride is formed through synthesis and has the antitumour effect.
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Paragraph 0047; 0049; 0050; 0051; 0052
(2018/04/03)
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- S - triazine derivative using the polymerization of the curable composition, the curing and molding material using them (by machine translation)
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[Problem] s - triazine derivative using the same molding processability and excellent in storage stability of the polymerizable composition, such as a cured product having excellent heat resistance and productivity of the molding material. (1) Represented by the formula [a], s - triazine derivative polymer. (R1 And R2 Is independently, H, a straight chain alkyl group or branched C1 a-6 // non-substituted aryl group; R1 And R2 The ring may be bonded together to form a; R3 And R4 Is H or a straight-chain alkyl groups are independently C1 a-6/branched; and independently of the linear/branched C1 a-8 A B alkyl group, alkoxy group or halogen atom C1 a-6; n is an integer of 0 - 4 m and are independently; m and n are 2 or more A, each of the substituted benzene ring may condense with B)[Drawing] no (by machine translation)
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Paragraph 0074; 0085; 0086
(2018/12/12)
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- Docking, synthesis and antimalarial activity of novel 4-anilinoquinoline derivatives
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A series of 4-anilinoquinoline triazine derivatives were designed, synthesized and screened for in vivo antimalarial activity against a chloroquine-sensitive strain of Plasmodium berghei. The compounds were further subjected to in vitro antimalarial activity against chloroquine-resistant W2 strain of Plasmodium falciparum and β-haematin inhibition studies. All the compounds exhibited in vivo antimalarial activity better than that shown by the standard drug, chloroquine. Twelve out of fifteen compounds showed better inhibition than that of chloroquine against chloroquine-resistant W2 strain of Plasmodium falciparum. Ten compounds showed β-haematin inhibition, better than that of chloroquine, with IC50 values in the range of 18–25?μM. One compound, 3k, was found to be better than artemisinin against W2 strain of Plasmodium falciparum and also displayed the best β-haematin inhibitory activity, thereby becoming eligible to be explored as a potential lead for antimalarial chemotherapy.
- Vijayaraghavan, Shilpa,Mahajan, Supriya
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p. 1693 - 1697
(2017/04/04)
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- MK2 INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 0304
(2016/04/09)
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- Synthesis of new 5-aza-isosteres of guanine containing aryl and hetaryl substituents on the 1,2,4-triazole ring
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The oxidative cyclization of 4-amino-substituted 6-arylidene(hetarylmethylidene)hydrazinyl-1,3,5-triazin-2-ones with lead(IV) tetraacetate proceeds via a Dimroth-type rearrangement to give 5-amino-substituted 2-aryl(hetaryl)-1,2,4-triazolo[1,5-a]-1,3,5-tr
- Zavodskaya, Anna V.,Bakharev, Vladimir V.,Parfenov, Victor E.,Gidaspov, Alexander A.,Slepukhin, Pavel A.,Isenov, Maksim L.,Eltsov, Oleg S.
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p. 1103 - 1106
(2015/02/19)
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- Targeting the erythrocytic and liver stages of malaria parasites with s-triazine-based hybrids
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A diversity-oriented library of s-triazine-based hybrids was screened for activity against the chloroquine-resistant Plasmodium falciparum W2 strain. The most striking result was sub-micromolar activity against cultured erythrocytic-stage parasites of hybrid molecules containing one or two 8-aminoquinoline moieties. These compounds were not clearly toxic to human cells. The most effective blood-schizontocidal s-triazine derivatives were then screened for activity against the liver stage of malaria parasites. The s-triazine hybrid containing two 8-aminoquinoline moieties and one chlorine atom emerged as the most potent against P. berghei liver-stage infection, active in the low nanomolar region, combined with good metabolic stability in rat liver microsomes. These results indicate that s-triazine-8-aminoquinoline-based hybrids are excellent starting points for lead optimization as dual-stage antimalarials.
- Rodrigues, Catarina A. B.,Frade, Raquel F. M.,Albuquerque, Inês S.,Perry, Maria J.,Gut, Jiri,Machado, Marta,Rosenthal, Philip J.,Prudêncio, Miguel,Afonso, Carlos A. M.,Moreira, Rui
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p. 883 - 890
(2015/05/05)
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- Synthesis of 4-amino-6-chloro-1,3,5-triazin-2(1H)-ones
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Conditions for selective substitution for one chlorine atom in 2-(R,R-amino)-4,6-dichloro-1,3,5-triazines with a hydroxide ion were elaborated. Spectral and calculation methods showed that the products formed are in the lactam form, i.e., have the structure of 4-chloro-6-(R,R- amino)-1,3,5-triazin-2(1H)-ones.
- Bakharev,Gidaspov,Parfenov,Ulyankina,Zavodskaya,Selezneva,Suponitskii,Sheremetev
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- Synthesis and biological evaluation of some thiazolidinones as antimicrobial agents
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A novel series of thiazolidinone derivatives namely 4-(4-dimethylamino-6- {4-[5-(4-ethylpiperazin-1-ylmethyl)-4-oxo-2-phenylthiazolidin-3-yl]-phenylamino} -[1,3,5]triazin-2-yloxy)-1-methyl-1H-quinolin-2-one have been synthesized from the key intermediate
- Patel, Divyesh,Kumari, Premlata,Patel, Navin
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experimental part
p. 354 - 362
(2012/03/22)
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- Synthesis of 3-{4-[4-dimethylamino-6-(4-methyl-2-oxo-2Hchromen-7-yloxy)-[1, 3,5]triazin-2-ylamino]-phenyl}-2-phenyl-5- (4-pyridin-2-yl-piperazin-1-ylmethyl) -thiazolidin-4-one and their biological evaluation
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A novel series of thiazolidinone derivatives namely 3-{4-[4-dimethylamino- 6-(4-methyl-2-oxo-2Hchromen- 7-yloxy)-[1,3,5]triazin-2-ylamino]-phenyl}-2- phenyl-5-(4-pyridin-2-yl-piperazin-1-ylmethyl)-thiazolidin- 4-one have been synthesized from the intermed
- Patel, Divyesh,Kumari, Premlata,Patel, Navin
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p. 2926 - 2944
(2012/11/07)
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- Synthesis and photovoltaic performances of donor-p-acceptor dyes utilizing 1,3,5-triazine as p spacers
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A series of new-type of donor-p-acceptor dyes (TCT-1-6) utilizing 1,3,5-triazine as p spacers were synthesized. These dyes were characterized by 1H NMR, ESI-MS, EA, and X-ray crystallography. Their photovoltaic performances were also investigat
- Liu, Jian,Wang, Kai,Xu, Feng,Tang, Zekun,Zheng, Wei,Zhang, Jiyuan,Li, Chenghui,Yu, Tao,You, Xiaozeng
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supporting information; experimental part
p. 6492 - 6496
(2011/12/16)
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- Structure-activity relationships of novel antibacterial translation inhibitors: 3,5-Diamino-piperidinyl triazines
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Structure-activity relationships of the 3,5-diamino-piperidinyl triazine series, a novel class of bacterial translation inhibitors, are described. Optimization was focused on the triazine C-4 position in which aromatic substituents that contained electron-withdrawing groups led to potent inhibitors. The initial lack of antibacterial activity was correlated with poor cellular penetration. Whole cell antibacterial activity was achieved by linking additional aromatic moieties at the triazine C-4 position.
- Zhou, Yuefen,Sun, Zhongxiang,Froelich, Jamie M.,Hermann, Thomas,Wall, Daniel
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p. 5451 - 5456
(2007/10/03)
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- AZOLE METHYLIDENE CYANIDE DERIVATIVES AND THEIR USE AS PROTEIN KINASE MODULATORS
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The present invention is related to azole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such azole derivatives. Said azole derivatives are modulators of the protein kinase signalling pathways, particularly the one involving c-Jun N-terminal kinase and/or Glycogen Kinase Synthase 3. The present invention is furthermore related to novel azole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstituted or substituted C1 -C6 alkyl; A is 2-pyridyl, 3-pyridyl, 4-pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or triazinyl group.
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- Synthesis and aromatase-inhibitory activity of imidazolyl-1,3,5-triazine derivatives
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Triamino-substituted 1,3,5-triazine derivatives were synthesized and tested for inhibitory activities against the aromatase of human placental microsomes and the cytochrome P450 side chain cleavage of cholesterol (P450(SCC)) of pig adrenal mitochondria. The compounds having imidazolyl and tertiary amino groups as substituents in the 1,3,5-triazine ring showed significant aromatase-inhibitory activity. Among them, compounds 17, 23, 26, 27 and 28 were more active than the reference compound, CGS 16949A. The inhibitory activities of these compounds against P450(SCC) were much weaker than their aromatase-inhibitory activities. These compounds may be regarded as selective aromatase inhibitors.
- Matsuno, Toshiyuki,Kato, Masanobu,Tsuchida, Yoshio,Takahashi, Masayuki,Yaguchi, Sin-Ichi,Terada, Sumio
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p. 291 - 296
(2007/10/03)
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- Triazinediones
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Herbicidal and fungicidal triazinediones of the formula: STR1 wherein R1 is an aliphatic radical, R2 is a carboxylic acyl radical, R3 is a hydrogen atom or an aliphatic radical, and X is a hydrogen atom or an aliphatic radical.
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