Comparison in antioxidant action between α-chitosan and β-chitosan at a wide range of molecular weight and chitosan concentration.

abstract：:The molecular design and chemical synthesis of novel enediyne molecules related to the neocarzinostatin chromophore (1), and their chemical and DNA cleaving properties are described. The 10-membered enediyne triols 16-18 were effectively synthesized from xylitol (10) in a short step, and found to be quite stable when ...

journal_title：Bioorganic & medicinal chemistry

authors： Toshima K,Ohta K,Kano T,Nakamura T,Nakata M,Kinoshita M,Matsumura S

更新日期：1996-01-01 00:00:00

abstract：:A series of 3-N,N-di-n-propylamino-2-chromanones were synthesized as dopamine analogues. The lactone ring was introduced as a means to reduce their propensity to cross the blood-brain barrier and to avoid central side effects, rendering these compounds potentially useful for the treatment of glaucoma. Pharmacological ...

journal_title：Bioorganic & medicinal chemistry

authors： Benoit-Guyod M,Nicolle E,Namil A,Coulombeau C,Leclerc G

更新日期：1995-12-01 00:00:00

abstract：:We report an inhibitor of the homodimeric protein-protein interaction of the BCL6 oncoprotein, identified from a genetically encoded SICLOPPS library of 3.2 million cyclic hexapeptides in combination with a bacterial reverse two-hybrid system. This cyclic peptide is shown to bind the BTB domain of BCL6, disrupts its h...

journal_title：Bioorganic & medicinal chemistry

authors： Osher EL,Castillo F,Elumalai N,Waring MJ,Pairaudeau G,Tavassoli A

更新日期：2018-07-15 00:00:00

abstract：:Oleoyl Formononetin (OF) has good weight loss activity and hypolipidemic activity, could improve insulin sensitivity and suppress adipogenesis. To acquire better biological activities, three series of flavonoid fatty acid esters were designed and synthesized by optimizing the structure of OF. Their bioactivities were ...

journal_title：Bioorganic & medicinal chemistry

authors： Zhao W,Sun J,Xiang H,Zeng YY,Li XB,Xiao H,Chen DY,Ma RL

更新日期：2011-05-15 00:00:00

abstract：:In this study, a number of 2',4'-BNA- and 2',4'-BNA(NC)-modified siRNAs were designed and synthesized. Their thermal stability, nuclease resistance and gene silencing properties against cultured mammalian cells were evaluated and compared with those of natural siRNAs. The 2',4'-BNA- and 2',4'-BNA(NC)-modified siRNAs (...

journal_title：Bioorganic & medicinal chemistry

authors： Abdur Rahman SM,Sato H,Tsuda N,Haitani S,Narukawa K,Imanishi T,Obika S

更新日期：2010-05-15 00:00:00

abstract：:A series of cis-restricted 1,5-disubstituted 1,2,3-triazole analogues of combretastatin A-4 (1) have been prepared. The triazole 12f, 2-methoxy-5-(1-(3,4,5-trimethoxyphenyl)-1H-1,2,3-triazol-5-yl)aniline, displayed potent cytotoxic activity against several cancer cell lines with IC(50) values in the nanomolar range. T...

journal_title：Bioorganic & medicinal chemistry

authors： Odlo K,Hentzen J,dit Chabert JF,Ducki S,Gani OA,Sylte I,Skrede M,Flørenes VA,Hansen TV

更新日期：2008-05-01 00:00:00

abstract：:Efficient preparations of the titled compounds are described, their antimicrobial activity and mutagenic properties being evaluated. Some of the studied compounds are nonmutagenic and present a MIC as low as some of the usual standards in the field. ...

journal_title：Bioorganic & medicinal chemistry

authors： Arredondo Y,Moreno-Mañas M,Pleixats R,Palacín C,Raga MM,Castelló JM,Ortiz JA

更新日期：1997-10-01 00:00:00

abstract：:The dysfunction and mutual compensatory activation of RAF-MEK-ERK and PI3K-PDK1-AKT pathways have been demonstrated as the hallmarks in several primary and recurrent cancers. The strategy of concurrent blocking of these two pathways shows clinical merits on effective cancer therapy, such as combinatory treatments and ...

journal_title：Bioorganic & medicinal chemistry

authors： Yu Z,Chen Z,Su Q,Ye S,Yuan H,Kuai M,Lv M,Tu Z,Yang X,Liu R,Hu G,Li Q

更新日期：2019-03-15 00:00:00

abstract：:Four palladium(II) and platinum(II) saccharinate (sac) complexes with 2-(hydroxymethyl)pyridine (2-hmpy) and 2-(2-hydroxyethyl)pyridine (2-hepy), namely trans-[Pd(2-hmpy)2(sac)2]·H2O (1), trans-[Pt(2-hmpy)2(sac)2]·3H2O (2), trans-[Pd(2-hepy)2(sac)2] (3) and trans-[Pt(2-hepy)2(sac)2] (4), have been synthesized and char...

journal_title：Bioorganic & medicinal chemistry

authors： Ari F,Aztopal N,Icsel C,Yilmaz VT,Guney E,Buyukgungor O,Ulukaya E

更新日期：2013-11-01 00:00:00

abstract：:A series of 3,6-disubstituted β-carbolines was synthesized and evaluated for their in vitro affinities at α(x)β(3)γ(2) GABA(A)/benzodiazepine receptor subtypes by radioligand binding assays in search of α(1) subtype selective ligands to treat alcohol abuse. Analogues of β-carboline-3-carboxylate-t-butyl ester (βCCt, 1...

journal_title：Bioorganic & medicinal chemistry

authors： Yin W,Majumder S,Clayton T,Petrou S,VanLinn ML,Namjoshi OA,Ma C,Cromer BA,Roth BL,Platt DM,Cook JM

更新日期：2010-11-01 00:00:00

abstract：:We report the kinetic properties and sulfonamide inhibition profile of an α-carbonic anhydrase (CA, EC 4.2.1.1), named CruCA4, identified in the red coral Corallium rubrum. This isoform is involved in the biomineralization process leading to the formation of a calcium carbonate skeleton. Experiments performed on the r...

journal_title：Bioorganic & medicinal chemistry

authors： Del Prete S,Vullo D,Zoccola D,Tambutté S,Capasso C,Supuran CT

更新日期：2017-07-01 00:00:00

abstract：:With the goal of developing multitargeted receptor tyrosine kinase inhibitors that display potent inhibition against PDGFRβ and VEGFR-2 we designed and synthesized eleven N(4)-(3-bromophenyl)-7-(substitutedbenzyl) pyrrolo[2,3-d]pyrimidines 9a-19a. These compounds were obtained from the key intermediate N(4)-(3-bromoph...

journal_title：Bioorganic & medicinal chemistry

authors： Gangjee A,Zaware N,Raghavan S,Yang J,Thorpe JE,Ihnat MA

更新日期：2012-04-01 00:00:00

abstract：:Previous studies on the indoloquinoline alkaloid, cryptolepine (2), revealed that it has antii-nfective properties among other activities. Using Structure-activity relationship (SAR) techniques, several ring-opened analogs of cryptolepine (3-phenylaminopyridinium and 3-phenylaminoquinolinium derivatives) were designed...

journal_title：Bioorganic & medicinal chemistry

authors： Mazu TK,Etukala JR,Zhu XY,Jacob MR,Khan SI,Walker LA,Ablordeppey SY

更新日期：2011-01-01 00:00:00

abstract：:A series of novel pyrimidinylthioacetanilides were designed, synthesized, and evaluated for their biological activity as potent HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Most of the tested compounds were proved to be effective in inhibiting HIV-1 (IIIB) replication with EC50 ranging from 0.15 μM ...

journal_title：Bioorganic & medicinal chemistry

authors： Li X,Lu X,Chen W,Liu H,Zhan P,Pannecouque C,Balzarini J,De Clercq E,Liu X

更新日期：2014-10-01 00:00:00

abstract：:Since nimesulide, a nonsteroidal anti-inflammatory drug, is known to be a selective inhibitor of cyclooxygenase-2 and shows activity against cancer cells, there has been much interest in developing related molecules with enhanced anticancer properties. Taking in consideration structural features of nimesulide analogue...

journal_title：Bioorganic & medicinal chemistry

authors： Catarro M,Serrano J,Cavalheiro E,Ramos S,Santos AO,Silvestre S,Almeida P

更新日期：2017-08-15 00:00:00

abstract：:Forty six new 1,4-epoxy-2-exo-aryl- and cis-2-aryl-4-hydroxytetrahydro-1-benzazepine derivatives were synthesized and fully characterized. All compounds were tested in vitro against both Trypanosoma cruzi and Leishmania chagasi parasites and also for cytotoxicity using Vero and THP-1 mammalian cell lines. Many of the ...

journal_title：Bioorganic & medicinal chemistry

authors： Gómez-Ayala S,Castrillón JA,Palma A,Leal SM,Escobar P,Bahsas A

更新日期：2010-07-01 00:00:00

abstract：:Three carboranyltetraphenylporphyrins containing 40 or 80 boron atoms were synthesized and evaluated for their biodistribution and toxicity in EMT-6 tumor-bearing mice. Copper (II) meso-5,10,15,20-tetrakis[3-methoxy-4-(o-carboranylmethoxy)phenyl]porphyrin, 6, and copper (II) meso-5,10,15,20-tetrakis[3-hydroxy-4-(o-car...

journal_title：Bioorganic & medicinal chemistry

authors： Wu H,Micca PL,Makar MS,Miura M

更新日期：2006-08-01 00:00:00

abstract：:Selections from dynamic combinatorial libraries (DCL) benefit from the dynamic nature of the library that can change constitution upon addition of a selection pressure, such as ligands binding to a protein. This technology has been predominantly used with small molecules interacting with each other through reversible ...

journal_title：Bioorganic & medicinal chemistry

authors： Farrera-Soler L,Daguer JP,Raunft P,Barluenga S,Imberty A,Winssinger N

更新日期：2020-05-15 00:00:00

abstract：:1,3,5,6-tetrahydroxyxanthone was synthesized. The relationship between protective effect of xanthone on endothelial cells and endogenous nitric oxide synthase inhibitors was investigated. Endothelial cells were treated with ox-LDL (100 microg/mL) for 48 h. Adhesion of monocytes to endothelial cells and release of lact...

journal_title：Bioorganic & medicinal chemistry

authors： Jiang DJ,Hu GY,Jiang JL,Xiang HL,Deng HW,Li YJ

更新日期：2003-11-17 00:00:00

abstract：:To develop agents for radionuclide imaging Aβ plaques in vivo, we prepared three fluorine-substituted analogs of arylbenzothiazole class; compound 2 has a high affinity for Aβ (K(i)=5.5nM) and the specific binding to Aβ in fluorescent staining. In preparation for the synthesis of these arylbenzothiazole analogs in rad...

journal_title：Bioorganic & medicinal chemistry

authors： Lee BC,Kim JS,Kim BS,Son JY,Hong SK,Park HS,Moon BS,Jung JH,Jeong JM,Kim SE

更新日期：2011-05-01 00:00:00

abstract：:Over the last several years we have synthesized and studied the in vitro and in vivo nAChR pharmacological properties of epibatidine (4) analogs. In this study we report the synthesis, nAChR in vitro and in vivo pharmacological properties of 3'-(substituted pyridinyl)-deschloroepibatidine analogs (5a-e and 6a-e). All ...

journal_title：Bioorganic & medicinal chemistry

authors： Ondachi PW,Ye Z,Castro AH,Luetje CW,Damaj MI,Mascarella SW,Navarro HA,Carroll FI

更新日期：2015-09-01 00:00:00

abstract：:The irreversible inhibition of histidine ammonia lyase by L-cysteine and dioxygen has been reexamined. After denaturation and consecutive digestion of the inhibited enzyme by trypsin and endoproteinase Glu-C, the generated chromophoric system (lambda max = 340 nm) remained intact and was isolated in an octapeptide con...

journal_title：Bioorganic & medicinal chemistry

authors： Weber K,Rétey J

更新日期：1996-07-01 00:00:00

abstract：:As part of a continuing effort aimed at the development of selective, efficacious, and centrally active m1 muscarinic agonists for the treatment of Alzheimer's disease, a series of amide and hydrazide amidine derivatives (2a-e and 3b-d) was synthesized and examined for muscarinic agonist activity. Preliminary biochemi...

journal_title：Bioorganic & medicinal chemistry

authors： Ojo B,Dunbar PG,Durant GJ,Nagy PI,Huzl JJ 3rd,Periyasamy S,Ngur DO,el-Assadi AA,Hoss WP,Messer WS Jr

更新日期：1996-10-01 00:00:00

abstract：:A series of novel 2,4-disubstituted quinazoline derivatives were prepared and their inhibitory activities on hPin1 were evaluated. Of all the synthesized compounds, eight compounds displayed inhibitory activities with IC(50) value at the level of 10(-6)mol/L. Preliminary structure-activity relationships were analyzed ...

journal_title：Bioorganic & medicinal chemistry

authors： Zhu L,Jin J,Liu C,Zhang C,Sun Y,Guo Y,Fu D,Chen X,Xu B

更新日期：2011-05-01 00:00:00

abstract：:Systematic replacement in the 3- or 4-position of the pyrrolidine ring at P1' proline was carried out. Compound 26, which has a Cl atom in the 4(S)-position was the most active among inhibitors substituted with other halogen atoms or other substituents. Furthermore, the replacement of the Z group in compound 26 with f...

journal_title：Bioorganic & medicinal chemistry

authors： Komai T,Higashida S,Sakurai M,Nitta T,Kasuya A,Miyamaoto S,Yagi R,Ozawa Y,Handa H,Mohri H,Yasuoka A,Oka S,Nishigaki T,Kimura S,Shimada K,Yabe Y

更新日期：1996-08-01 00:00:00

abstract：:Polyamides consisting of N-methylpyrrole (Py), N-methylimidazole (Im), and N-methyl-3-hydroxypyrrole (Hp) are synthetic ligands that recognize predetermined DNA sequences with affinities and specificities comparable to many DNA-binding proteins. As derivatives of the natural products distamycin and netropsin, Py/Im/Hp...

journal_title：Bioorganic & medicinal chemistry

authors： Bremer RE,Szewczyk JW,Baird EE,Dervan PB

更新日期：2000-08-01 00:00:00

abstract：:The calcium-sensing receptor antagonist (CaSR) has been recognized as a promising target of anabolic agents for treating osteoporosis. In the course of developing a new drug candidate for osteoporosis, we found tetrahydropyrazolopyrimidine derivative 1 to be an orally active CaSR antagonist that stimulated transient P...

journal_title：Bioorganic & medicinal chemistry

authors： Yoshida M,Mori A,Morimoto S,Kotani E,Oka M,Notoya K,Makino H,Ono M,Shirasaki M,Tada N,Fujita H,Ban J,Ikeda Y,Kawamoto T,Goto M,Kimura H,Baba A,Yasuma T

更新日期：2011-03-15 00:00:00

abstract：:Novel quinazolin- and benzothiazol-6-yloxyacetamides show excellent in vivo activity against the three economically most important Oomycete pathogens Phytophthora infestans, Plasmopara viticola and Pythium ultimum. They are polar analogs of known quinolin-6-yloxyacetamides, which are not active against the soil-borne ...

journal_title：Bioorganic & medicinal chemistry

authors： Beaudegnies R,Quaranta L,Murphy Kessabi F,Lamberth C,Knauf-Beiter G,Fraser T

更新日期：2016-02-01 00:00:00

abstract：:Synthetic 6-chromanol derivatives were prepared with several chlorine substitutions, which conferred both electron-withdrawing inductive effects and electron-donating resonance effects. A trichlorinated compound (2), a dichlorinated compound (3), and three monochlorinated compounds (4, 5, and 6) were synthesized; comp...

journal_title：Bioorganic & medicinal chemistry

authors： Inami K,Iizuka Y,Furukawa M,Nakanishi I,Ohkubo K,Fukuhara K,Fukuzumi S,Mochizuki M

更新日期：2012-07-01 00:00:00

abstract：:WAP-8294A2 is a cyclic peptide antibiotic with novel structure and excellent activity against Gram-positive pathogens. Herein, we report the total synthesis of complex macrocyclic peptide WAP-8294A2 (W1), ent-analogue W2, deoxy analogue W3 and de-methyl analogue W4 using a solid-phase synthetic route followed by a fin...

journal_title：Bioorganic & medicinal chemistry

authors： Chen D,Tian L,Po KHL,Chen S,Li X

更新日期：2020-09-15 00:00:00