- Novel imidazo[4,5-b]pyridine derived acrylonitriles: A combined experimental and computational study of their antioxidative potential
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We describe the synthesis of novel unsubstituted and N-substituted imidazo[4,5-b]pyridine derived acrylonitriles, which were prepared by classical and microwave assisted organic synthesis. Their antioxidative potential was studied using spectroscopic DPPH
- Bo?ek, Ida,Hranjec, Marijana,Novak Jovanovi?, Ivana,Star?evi?, Kristina,Vianello, Robert
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- Heterocyclic compound and organic light emitting device including the same
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Provided are a heterocyclic compound and an organic light-emitting device including the same. The heterocyclic compound may be represented by Formula 1: in the Formula 1, A1, X2, Y1, Y2, m1, m2, R10,R20, R30, b10, b20 and b30 are same as described in the description.
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Paragraph 0521; 0534-0537; 0628; 0633-0636
(2020/07/15)
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- Platinum compound with photoluminescence performance and preparation method thereof
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The invention belongs to the technical field of organic complex synthesis, and particularly relates to a platinum compound with photoluminescence performance and a preparation method thereof. The molecular formula of the platinum compound with the photolu
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Paragraph 0049; 0052; 0054; 0059; 0061; 0066; 0068
(2020/11/23)
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- Pt (II) photoluminescence compound based on pyridinoimidazole derivative and preparation method thereof
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The invention belongs to the technical field of synthesis of organic complexes, and particularly relates to a Pt (II) photoluminescence compound based on a pyridinoimidazole derivative and a preparation method thereof. The molecular formula of the Pt (II)
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Paragraph 0057; 0059; 0064; 0066; 0071; 0073
(2020/12/15)
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- Platinum luminescent compound based on pyridinoimidazole derivative and preparation method of platinum luminescent compound
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The invention belongs to the technical field of synthesis of organic complexes, and particularly relates to a platinum luminescent compound based on a pyridinoimidazole derivative and a preparation method of the platinum luminescent compound. The molecula
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Paragraph 0050; 0053; 0055; 0060; 0062; 0067; 0069
(2020/12/15)
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- Synthesis and biological evaluation of 1-benzyl-N-(2-(phenylamino)pyridin-3-yl)-1H-1,2,3-triazole-4-carboxamides as antimitotic agents
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A library of 1-benzyl-N-(2-(phenylamino)pyridin-3-yl)-1H-1,2,3-triazole-4-carboxamides (7a–al) have been designed, synthesized and screened for their anti-proliferative activity against some selected human cancer cell lines namely DU-145, A-549, MCF-7 and HeLa. Most of them have shown promising cytotoxicity against lung cancer cell line (A549), amongst them 7f was found to be the most potent anti-proliferative congener. Furthermore, 7f exhibited comparable tubulin polymerization inhibition (IC50 value 2.04 μM) to the standard E7010 (IC50 value 2.15 μM). Moreover, flow cytometric analysis revealed that this compound induced apoptosis via cell cycle arrest at G2/M phase in A549 cells. Induction of apoptosis was further observed by examining the mitochondrial membrane potential and was also confirmed by Hoechst staining as well as Annexin V-FITC assays. Furthermore, molecular docking studies indicated that compound 7f binds to the colchicine binding site of the β-tubulin. Thus, 7f exhibits anti-proliferative properties by inhibiting the tubulin polymerization through the binding at the colchicine active site and by induction of apoptosis.
- Prasad, Budaganaboyina,Lakshma Nayak,Srikanth,Baig, Mirza Feroz,Subba Reddy,Babu, Korrapati Suresh,Kamal, Ahmed
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p. 535 - 548
(2018/11/26)
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- Rational design and synthesis of 2-anilinopyridinyl-benzothiazole Schiff bases as antimitotic agents
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Based on our previous results and literature precedence, a series of 2-anilinopyridinyl-benzothiazole Schiff bases were rationally designed by performing molecular modeling experiments on some selected molecules. The binding energies of the docked molecules were better than the E7010, and the Schiff base with trimethoxy group on benzothiazole moiety, 4y was the best. This was followed by the synthesis of a series of the designed molecules by a convenient synthetic route and evaluation of their anticancer potential. Most of the compounds have shown significant growth inhibition against the tested cell lines and the compound 4y exhibited good antiproliferative activity with a GI50 value of 3.8?μM specifically against the cell line DU145. In agreement with the docking results, 4y exerted cytotoxicity by the disruption of the microtubule dynamics by inhibiting tubulin polymerization via effective binding into colchicine domain, comparable to E7010. Detailed binding modes of 4y with colchicine binding site of tubulin were studied by molecular docking. Furthermore, 4y induced apoptosis as evidenced by biological studies like mitochondrial membrane potential, caspase-3, and Annexin V-FITC assays.
- Shaik, Thokhir B.,Hussaini, S.M. Ali,Nayak, V. Lakshma,Sucharitha, M. Lakshmi,Malik, M. Shaheer,Kamal, Ahmed
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supporting information
p. 2549 - 2558
(2017/05/09)
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- Synthesis of 2-anilinopyridine dimers as microtubule targeting and apoptosis inducing agents
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A series of 2-anilinopyridine dimers have been synthesized and evaluated for their anticancer potential. Most of the compounds have showed significant growth inhibition of the cell lines tested and compound 4d was most effective amongst the series display
- Kamal, Ahmed,Ali Hussaini,Lakshma Nayak,Shaheer Malik,Lakshmi Sucharitha,Shaik, Thokhir Basha,Ashraf, Md.,Bagul, Chandrakant
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p. 6755 - 6767
(2015/02/02)
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- Imidazopyridine derivatives as PI3K inhibitors
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New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks)
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Page/Page column 32-33
(2012/11/13)
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- IMIDAZOPYRIDINE DERIVATIVES AS PI3K INHIBITORS
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New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
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Page/Page column 80
(2012/11/13)
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- HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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Page/Page column 118
(2012/08/27)
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- PYRIDYL CARBENE PHOSPHORESCENT EMITTERS
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Organometallic compounds comprising an imidazole carbene ligand having a N-containing ring fused to the imidazole ring are provided. In particular, the N-containing ring fused to the imidazole ring may contain one nitrogen atom or more than one nitrogen a
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- PYRIDYL CARBENE PHOSPHORESCENT EMITTERS
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Organometallic compounds comprising an imidazole carbene ligand having a N- containing ring fused to the imidazole ring are provided. In particular, the N-containing ring fused to the imidazole ring may contain one nitrogen atom or more than one nitrogen
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Page/Page column 66
(2012/09/22)
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- Synthesis and cytotoxicity studies of novel 2-hydrazonylpyrido[2,3-b] pyrazin-3(4H)-ones
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In an attempt to develop potent antitumor agents, a series of novel 2-hydrazonylpyrido[2,3-b]pyrazin-3(4H)-one derivatives were designed and synthesized. All the prepared compounds were screened for their cytotoxic activities against A549, MDA-MB-231 and HT-29 cell lines in vitro. Pharmacological data indicated that five of the target compounds showed cytotoxicity against A549 cell line below a concentration of 1 μM. Compound 15g was the most potent one with IC50 values of 0.19, 2.11 and 2.15 μM against A549, MDA-MB-231 and HT29 cell lines, respectively. A series of 2-hydrazonylpyrido[2,3-b]pyrazin-3(4H)-one derivatives was designed and synthesized. Preliminary structure-activity relationships suggested that compounds with 4-methoxyphenyl or 4-(trifluoromethoxy)phenyl groups on the N-4 position were generally more potent than those with an unsubstituted phenyl group. Copyright
- Zhang, Guogang,Liu, Yajing,Wang, Shuobing,Zhou, Chuan,Huang, Qingchang,Gong, Ping
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experimental part
p. 49 - 56
(2012/03/11)
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- Synthesis and in vitro cytotoxic evaluation of 2-hydrazinylpyrido[2,3-b] pyrazin-3(4H)-one derivatives
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A series of novel 2-hydrazinylpyrido[2,3-b]pyrazin-3(4H)-one derivatives were synthesized and evaluated for their cytotoxic activities against A549, MDA-MB-231 and HT-29 cell lines in vitro. Pharmacological data indicated that compounds 5b, 5c, 10a and 10
- Zhang, Guo Gang,Liu, Ya Jing,Ma, Xiao Guang,Dong, Hao,Li, Ju,Gong, Ping
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scheme or table
p. 1223 - 1225
(2012/01/12)
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- ARYL SULFAMIDE DERIVATIVES AND METHODS OF THEIR USE
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The present invention is directed to aryl sulfamide derivatives of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
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Page/Page column 111
(2008/12/06)
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- Polymer-assisted parallel solution phase synthesis of substituted benzimidazoles
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A small library of benzimidazoles was prepared using polymer-bound reagents and scavengers. Polymer-assisted reaction of diphenyl diamines with carboxylic acids yielded o-amido-diphenylamines in the presence of Polystyrene-Carbodiimide (PS-Carbodiimide) u
- Yun, Young K.,Porco Jr., John A.,Labadie, Jeff
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p. 739 - 742
(2007/10/03)
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- Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor
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1-Phenylbenzimidazoles are shown to be a new class of ATP-site inhibitors of the platelet-derived growth factor receptor (PDGFR). Structure- activity relationships (SARs) are narrow, with closely related heterocycles being inactive. A systematic study of
- Palmer, Brian D.
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p. 5457 - 5465
(2007/10/03)
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- Heterocyclic compounds having anti-diabetic activity and their use
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Compounds of formula (I): STR1 [wherein: X represents an unsubstituted or substituted indolyl, indolinyl, azaindolyl, azaindolinyl, imidazopyridyl or imidazopyrimidinyl group; Y represents an oxygen or sulfur atom; Z represents a 2,4-dioxothiazolidin-5-ylidenylmethyl, 2,4-dioxothiazolidin-5-ylmethyl, 2,4-dioxooxazolidin-5-ylmethyl, 3,5-dioxooxadiazolidin-2-ylmethyl or N-hydroxyureidomethyl group; R represents a hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, a hydroxy group, a nitro group, an aralkyl group or a unsubstituted or substituted amino group; and m is an integer of from 1 to 5] have hypoglycemic and anti-diabetic activities.
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- Sulfonamide derivatives
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Sulfonamide derivatives of the general formula (I): STR1 wherein preferably R1 represents a lower alkoxy group, R2, R3, R4, R5, R6 and R7 are as defined in the specification, A and B may be the same or different from each other and each represents =N-- or =CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and may be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R2 and R3 which are each a hydrogen atom, A and B which are each =CH-- and E which is a phenyl group which may be substituted with 1 to 3 substituents G which may be the same or different from one another is excluded, or pharmacologically acceptance salts of them.
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- The ortho effect in pyridines. Part XI(1). Substituent effects on basicity of 2- and 4-substituted 3-aminopyridines
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The substituent effects on the pKa values corresponding to the first protonation site of thirty 2- and 4-substituted 3-aminopyridines have been studied.It was found that the relative localized and delocalized effects are apparently sensitive to the variation of substituent position in the pyridine ring.An interaction of the 2-substituent with the protonation centre has mainly inductive character, whereas, the pKa values of 4-substituted 3-aminopyridines are highly affected by through-resonance.The steric effect was found to be insignificant.Keywords: substituent effects / 2- and 4-substituted 3-aminopyridines / basicity
- Rasala, D.
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- New Synthesis of 11-Acyl-5,11-dihydro-6H-pyridobenzodiazepin-6-ones and Related Studies
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New synthesis of 11-acyl-5,11-dihydro-6H-pyridobenzodiazepin-6-ones (42-44) is reported.The crucial steps (Scheme VI) represented N-oxidation of 1 (1A) to 35 (35A), facilitated ring-closure of 36 into 37, its subsequent N-α-chloroacetylation to 38, aminolysis to 39-41 (involving N-O anchimeric assistance as depicted in 38A) and deoxygenation to 42-44 (Scheme VII).The central intermediate 37 is also obtained on oxygenation of 2, a new synthesis of which was reported in the previous paper of this series .Other attempts of cyclisation "from the top" or "from the bottom" (Scheme I) are described.Thus, interaction of 1 with acetamide afforded 3 and 4 instead of the expected 2A.Compound 5 cyclised into 3-pyridoquinazolone 6 while its 2-(4'-methylpiperazin-1'-yl) analogue 9 was observed to be unstable for the attempted ring-opening and reclosure to 42. "From the bottom" cyclisations of 10A-10C, via intermediary amines 11A-11C failed and pyridoquinazolinone 13 was isolated (Scheme V).The attempted oxidative cyclisation of the compounds 15 and 18 into 2 and 42, respectively, 13 afforded imidazolopyridine derivative (18-19), while 15 remained unchanged. 3-Acylamino-2-arylaminopyridines (21-24), cyclised into the imidazolopyridines 29-30.Model compounds 45-50 were prepared to study selective aminolysis of the chlorine atoms in 2-chloro-3-(2'-chlorobenzoyl)aminopyridine 1, and its N-oxide 35.
- Kovac, T.,Oklobdzija, M.,Comisso, G.,Decorte, E.,Fajdiga, T.,et al.
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p. 1339 - 1349
(2007/10/02)
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