In vitro antitumor activities of 2,6-di-[2-(heteroaryl)vinyl]pyridines and pyridiniums.

abstract：:Described herein are our limited structure-activity relationship (SAR) studies on a 5:7-fused heterocycle (1), containing the 4,6,8-triaminoimidazo[4,5-e][1,3]diazepine ring system, whose synthesis and potent broad-spectrum anticancer activity we reported a few years ago. Our SAR efforts in this study are mainly focus...

journal_title：Bioorganic & medicinal chemistry

authors： Xie M,Lapidus RG,Sadowska M,Edelman MJ,Hosmane RS

更新日期：2016-06-15 00:00:00

abstract：:2'-O-(2-Methoxyethyl)-5-(3-aminoprop-1-ynyl)-uridine phosphoramidite (MEPU) has been synthesized from d-ribose and 5-iodouracil and incorporated into triplex-forming oligonucleotides (TFOs) by automated solid-phase oligonucleotide synthesis. The TFOs gave very high triplex stability with their target duplexes as measu...

journal_title：Bioorganic & medicinal chemistry

authors： Lou C,Xiao Q,Brennan L,Light ME,Vergara-Irigaray N,Atkinson EM,Holden-Dye LM,Fox KR,Brown T

更新日期：2010-09-01 00:00:00

abstract：:Novel 4-amino-2-phenylpyrimidine derivatives were synthesized and evaluated as GPR119 agonists. Optimization of the substituents on the phenyl ring at the 2-position and the amino group at the 4-position led to the identification of 3,4-dihalogenated and 2,4,5-trihalogenated phenyl derivatives showing potent GPR119 ag...

journal_title：Bioorganic & medicinal chemistry

authors： Negoro K,Yonetoku Y,Misawa-Mukai H,Hamaguchi W,Maruyama T,Yoshida S,Takeuchi M,Ohta M

更新日期：2012-09-01 00:00:00

abstract：:The organoselenium antioxidant 1 was previously found to act as a catalytic antioxidant in a two-phase lipid peroxidation system. In aqueous environment, selenide 1 quenched ABTS-radicals more efficiently than Trolox and ascorbic acid. The selenide dose-dependently scavenged reactive oxygen and nitrogen species more e...

journal_title：Bioorganic & medicinal chemistry

authors： Johansson H,Svartström O,Phadnis P,Engman L,Ott MK

更新日期：2010-03-01 00:00:00

abstract：:Epolactaene, a neuritogenic compound in human neuroblastoma SH-SY5Y, induces apoptosis in a human leukemia B-cell line, BALL-1. The apoptosis-inducing activities of 34 epolactaene derivatives, including those of the newly synthesized alpha-alkyl-alpha,beta-epoxy-gamma-lactam derivative and cyclopropane derivatives, we...

journal_title：Bioorganic & medicinal chemistry

authors： Kuramochi K,Matsui R,Matsubara Y,Nakai J,Sunoki T,Arai S,Nagata S,Nagahara Y,Mizushina Y,Ikekita M,Kobayashi S

更新日期：2006-04-01 00:00:00

abstract：:The boronic acid group is widely used in chemosensor design due to its ability to reversibly bind diol-containing compounds. The thermodynamic properties of the boronic acid-diol binding process have been investigated extensively. However, there are few studies of the kinetic properties of such binding processes. In t...

journal_title：Bioorganic & medicinal chemistry

authors： Ni N,Laughlin S,Wang Y,Feng Y,Zheng Y,Wang B

更新日期：2012-05-01 00:00:00

abstract：:Polo-like kinase (Plk) 1 is a serine-threonine protein kinase that plays a role in cell division, and its overexpression is highly correlated with aggressiveness and prognosis of many cancers. We have designed, synthesized and evaluated a series of terphenyl compounds as inhibitors of the kinase activity of Plk1. Some...

journal_title：Bioorganic & medicinal chemistry

authors： Mita Y,Noguchi-Yachide T,Ishikawa M,Hashimoto Y

更新日期：2013-02-01 00:00:00

abstract：:Gangjee et al. recently reported a novel series of 2-amino-4-methyl-5-phenylethyl substituted-7-benzyl-pyrrolo[2,3-d]pyrimidines, some of which exhibited two digit nanomolar antitumor and antimitotic activity and were not subject to P-glycoprotein (Pgp) or multidrug resistance protein 1 (MRP1) mediated tumor resistanc...

journal_title：Bioorganic & medicinal chemistry

authors： Gangjee A,Namjoshi OA,Keller SN,Smith CD

更新日期：2011-07-15 00:00:00

abstract：:A novel series of '4-1' pentacyclic naphthalimides, where the chromophore consists of a naphthalimide moiety, fused to an imidazole ring containing an unfused aryl or heteroaryl ring, were synthesized and evaluated for in vitro antitumor activity. In general, the new derivatives showed an improved cytotoxic activity o...

journal_title：Bioorganic & medicinal chemistry

authors： Li F,Cui J,Guo L,Qian X,Ren W,Wang K,Liu F

更新日期：2007-08-01 00:00:00

abstract：:Non-viral gene therapy is based on the development of efficient and safe gene carrier systems able to transfer DNA into cells. Polyethylenimine (PEI), the most promising non-viral vector, with its high cationic-charge-density potential is able (1) to compact DNA in complexes (polyplexes) smaller than those formed by l...

journal_title：Bioorganic & medicinal chemistry

authors： Masotti A,Moretti F,Mancini F,Russo G,Di Lauro N,Checchia P,Marianecci C,Carafa M,Santucci E,Ortaggi G

更新日期：2007-02-01 00:00:00

abstract：:A type of novel α,β-unsaturated cyclohexanone analogous, which designed based on the curcumin core structure, have been discovered as potential EGFR inhibitors. These compounds exhibit potent antiproliferative activity in two human tumor cell lines (Hep G2 and B16-F10). Among them, compounds I(3) and I(12) displayed t...

journal_title：Bioorganic & medicinal chemistry

authors： Xu YY,Cao Y,Ma H,Li HQ,Ao GZ

更新日期：2013-01-15 00:00:00

abstract：:(R)- and (S)-Hippuryl-alpha-methylphenylalanine [(R)- and (S)-Hipp-alpha-MePhe] and (S)-hippuryl-alpha-methylphenyllactic acid [(S)-Hipp-alpha-MeOPhe] were synthesized and evaluated as substrates for carboxypeptidase A (CPA) in an effort to shed further light on the catalytic mechanism of the enzyme. The rate of CPA-c...

journal_title：Bioorganic & medicinal chemistry

authors： Lee M,Kim DH

更新日期：2000-04-01 00:00:00

abstract：:MO theoretical calculations were used with the aim to investigate the electronic properties of a number of sulphonylureas 1-8 which are employed as antifeedants. Quantum chemical descriptors [electron density, molecular electrostatic potential (MEP), the topology of frontier orbitals and reactivity index] were determi...

journal_title：Bioorganic & medicinal chemistry

authors： Galeazzi R,Marucchini C,Orena M,Zadra C

更新日期：2002-04-01 00:00:00

abstract：:Malaria and HIV are among the most important global health problems of our time and together are responsible for approximately 3 million deaths annually. These two diseases overlap in many regions of the world including sub-Saharan Africa, Southeast Asia and South America, leading to a higher risk of co-infection. In ...

journal_title：Bioorganic & medicinal chemistry

authors： Aminake MN,Mahajan A,Kumar V,Hans R,Wiesner L,Taylor D,de Kock C,Grobler A,Smith PJ,Kirschner M,Rethwilm A,Pradel G,Chibale K

更新日期：2012-09-01 00:00:00

abstract：:We describe the development of a computational model for the prediction of the inhibition of K(+) flow through the hERG ion channel. Using a collection of 1075 discovery compounds with hERG inhibition measured in our standard patch-clamp electrophysiology assay, molecular features important for drug-induced inhibition...

journal_title：Bioorganic & medicinal chemistry

authors： Johnson SR,Yue H,Conder ML,Shi H,Doweyko AM,Lloyd J,Levesque P

更新日期：2007-09-15 00:00:00

abstract：:Adenosine A1 receptors are attracting great interest as drug targets for their role in cognitive deficits. Antagonism of the adenosine A1 receptor may offer therapeutic benefits in complex neurological diseases, such as Alzheimer's and Parkinson's disease. The aim of this study was to discover potential selective aden...

journal_title：Bioorganic & medicinal chemistry

authors： Van der Walt MM,Terre'Blanche G

更新日期：2015-10-15 00:00:00

abstract：:A series of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides bearing the halogens iodine and bromine were synthesised and their binding affinity for the peripheral benzodiazepine binding sites (PBBS) in rat kidney mitochondrial membranes was evaluated using [(3)H]PK11195. Central benzodiazepine receptor (CBR) affinities we...

journal_title：Bioorganic & medicinal chemistry

authors： Homes TP,Mattner F,Keller PA,Katsifis A

更新日期：2006-06-01 00:00:00

abstract：:A novel series of homo- and heterodimeric ligands containing κ/μ agonist and μ agonist/antagonist pharmacophores joined by a 10-carbon ester linker chain were synthesized and evaluated for their in vitro binding affinity at κ, μ, and δ opioid receptors, and their functional activities were determined at κ and μ recept...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang B,Zhang T,Sromek AW,Scrimale T,Bidlack JM,Neumeyer JL

更新日期：2011-05-01 00:00:00

abstract：:6-N-(Benzothiazol-2-yl)deoxyadenosine (A(BT)) was synthesized and incorporated into DNAs. Although, the multipoint benzothiazole (BT) modification of oligodeoxynucleotides reduced the stability of duplexes with their complementary strands, it induced the strong exciton coupling between BT moieties. The circular dichro...

journal_title：Bioorganic & medicinal chemistry

authors： Masaki Y,Ohkubo A,Seio K,Sekine M

更新日期：2010-01-15 00:00:00

abstract：:Soluble epoxide hydrolase (sEH) is a potential target for the treatment of inflammation and hypertension. X-ray crystallographic fragment screening was used to identify fragment hits and their binding modes. Eight fragment hits were identified via soaking of sEH crystals with fragment cocktails, and the co-crystal str...

journal_title：Bioorganic & medicinal chemistry

authors： Amano Y,Tanabe E,Yamaguchi T

更新日期：2015-05-15 00:00:00

abstract：:The effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles have been studied to design new potent antibacterials against Gram-positive multidrug-resistant pathogens. The adopted strategy involved a molecular modelling approach, the synthesis and biological evaluation of new designed compo...

journal_title：Bioorganic & medicinal chemistry

authors： Fortuna CG,Berardozzi R,Bonaccorso C,Caltabiano G,Di Bari L,Goracci L,Guarcello A,Pace A,Palumbo Piccionello A,Pescitelli G,Pierro P,Lonati E,Bulbarelli A,Cocuzza CE,Musumarra G,Musumeci R

更新日期：2014-12-15 00:00:00

abstract：:Two of the histone deacetylases, TbDAC1 and TbDAC3, have been reported to be essential genes in trypanosomes. Therefore, we tested the activity of a panel of human histone deacetylase inhibitors (HDACi) for their ability to block proliferation of Trypanosoma brucei brucei. Among the HDACi's, the hydroxamic acid deriva...

journal_title：Bioorganic & medicinal chemistry

authors： Carrillo AK,Guiguemde WA,Guy RK

更新日期：2015-08-15 00:00:00

abstract：:Hydroxylated 6H-benzo[c]chromen-6-one derivatives (i.e., urolithins) are the main bioavailable metabolites, and biomarkers of ellagitannins present in various nutrition. Although these dietaries, the sources of urolithins, are employed in folk medicine as cognitive enhancer in the treatment of Alzheimer's Disease, uro...

journal_title：Bioorganic & medicinal chemistry

authors： Gulcan HO,Unlu S,Esiringu I,Ercetin T,Sahin Y,Oz D,Sahin MF

更新日期：2014-10-01 00:00:00

abstract：:Molecules designed for cell-specific imaging were studied, taking advantage of an enzyme-inhibitor interaction. 1-Deoxynojirimycin (DNJ) can be actively captured by cells which express the surface membrane protein α-glucosidase. New probes composed of DNJ for recognition linked to a fluorophore signal portion were pre...

journal_title：Bioorganic & medicinal chemistry

authors： Hatano A,Kanno Y,Kondo Y,Sunaga Y,Umezawa H,Fukui K

更新日期：2019-03-01 00:00:00

abstract：:A library of 25-membered chalcones was prepared by parallel synthesis. Substituted acetophenones and benzaldehydes were condensed using the Claisen-Schmidt base-catalyzed aldol condensation. Several chalcones showed in vitro antiparasitic activity against Giardia lamblia. The highest activity observed for the IC(50) v...

journal_title：Bioorganic & medicinal chemistry

authors： Montes-Avila J,Díaz-Camacho SP,Sicairos-Félix J,Delgado-Vargas F,Rivero IA

更新日期：2009-09-15 00:00:00

abstract：:Three series of new N-substituted 1,2,3,4-tetrahydroisoquinolines with 2-, 3-, and 4-membered alkyl chains (a, b, and c, respectively) were synthesized, and the effect of some structural modifications on their 5-HT1A receptor affinities and functional properties was discussed. It was found that the volume of the termi...

journal_title：Bioorganic & medicinal chemistry

authors： Mokrosz MJ,Bojarski AJ,Duszyńska B,Tatarczyńska E,Kłodzińska A,Dereń-Wesołek A,Charakchieva-Minol S,Chojnacka-Wójcik E

更新日期：1999-02-01 00:00:00

abstract：:N-acetyl-β-d-hexosaminidase (Hex) is potential target for pesticide design. Here, a series of thiazolylhydrazone derivatives were designed, synthesized and evaluated as competitive inhibitors of OfHex1, a Hex from the agricultural pest Ostrinia furnacalis. The derivative 3k, with a (benzyloxy)methyl group at the N3 at...

journal_title：Bioorganic & medicinal chemistry

authors： Yang H,Liu T,Qi H,Huang Z,Hao Z,Ying J,Yang Q,Qian X

更新日期：2018-11-01 00:00:00

abstract：:Inhibition of the endonuclease activity of influenza RNA-dependent RNA polymerase is recognized as an attractive target for the development of new agents for the treatment of influenza infection. Our earlier study employing small molecule fragment screening using a high-resolution crystal form of pandemic 2009 H1N1 in...

journal_title：Bioorganic & medicinal chemistry

authors： Parhi AK,Xiang A,Bauman JD,Patel D,Vijayan RS,Das K,Arnold E,Lavoie EJ

更新日期：2013-11-01 00:00:00

abstract：:A series of quinoline derivatives featuring the novelty of introducing intra-molecular hydrogen bonding scaffold (iMHBS) were designed, synthesized and biologically evaluated for their mTOR inhibitory activity, as well as anti-proliferative efficacies against HCT-116, PC-3 and MCF-7 cell lines. As a result, six compou...

journal_title：Bioorganic & medicinal chemistry

authors： Ma X,Lv X,Qiu N,Yang B,He Q,Hu Y

更新日期：2015-12-15 00:00:00

abstract：:The synthesis and the biological activity of compounds 5-40 as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), as well as modulators of voltage-dependent Ca(2+) channels and nicotinic receptors, are described. These molecules are tacrine analogues, which have been prepared from polyfunctio...

journal_title：Bioorganic & medicinal chemistry

authors： Marco JL,de los Ríos C,García AG,Villarroya M,Carreiras MC,Martins C,Eleutério A,Morreale A,Orozco M,Luque FJ

更新日期：2004-05-01 00:00:00