Biocatalytic combinatorial synthesis.

abstract：:We report the synthesis of several highly functionalized biotinylated philanthotoxin (PhTX) analogues (7, 8, 10, 13-16) designed on the basis of earlier structure-activity relationship studies. Despite the extensive modifications, the binding to nicotinic acetylcholine receptor (nAChR) is in the low micromolar range a...

journal_title：Bioorganic & medicinal chemistry

authors： Hashimoto M,Liu Y,Fang K,Li HY,Campiani G,Nakanishi K

更新日期：1999-06-01 00:00:00

abstract：:A new meso-2,4,6-trimethoxyphenyl porphyrin covalently linked to a 2',6'-dinitro-4'-trifluoromethylphenyl group by an amine bond 5 and its metal complex with Cd(II) 6 was prepared. The photodynamic activities of 5 and 6 were evaluated in vitro on Hep-2 cells. A considerable increase in the photocytotoxic effect was fo...

journal_title：Bioorganic & medicinal chemistry

authors： Milanesio ME,Morán FS,Yslas EI,Alvarez MG,Rivarola V,Durantini EN

更新日期：2001-08-01 00:00:00

abstract：:The fluorescent intercalator displacement assay using thiazole orange has been adapted to the study of RNA-binding helix-threading peptides (HTPs). This assay is highly sensitive with HTP-binding RNAs and provides binding affinity data in good agreement with quantitative ribonuclease footprinting without the need for ...

journal_title：Bioorganic & medicinal chemistry

authors： Krishnamurthy M,Schirle NT,Beal PA

更新日期：2008-10-01 00:00:00

abstract：:Protoporphyrinogen oxidase (Protox, EC 1.3.3.4) has attracted great interest during the last decades due to its unique biochemical characteristics and biomedical significance. As a continuation of our research work on the development of new PPO inhibitors, 23 new 1,3,4-thiadiazol-2(3H)-ones bearing benzothiazole subst...

journal_title：Bioorganic & medicinal chemistry

authors： Zuo Y,Yang SG,Jiang LL,Hao GF,Wang ZF,Wu QY,Xi Z,Yang GF

更新日期：2012-01-01 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：:We examined the properties of RNA analogues containing 2'-deoxy-2'-alpha-fluorouridine (1) or 2'-O-methyluridine (2) as inhibitors against human RNase L, that cleaves a single-stranded RNA in the presence of 2',5'-linked oligoadenylate (2-5A). The RNA analogue, FF, containing two molecules of 1 in place of uridine eff...

journal_title：Bioorganic & medicinal chemistry

authors： Ueno Y,Yamada Y,Nakanishi M,Kitade Y

更新日期：2003-11-17 00:00:00

abstract：:Bioassay-directed fractionation of the leaf and root extracts of the antiproliferative Madagascar plant Stuhlmannia moavi afforded 6-acetyl-5,8-dihydroxy-2-methoxy-7-methyl-1,4-naphthoquinone (stuhlmoavin, 1) as the most active compound, with an IC50 value of 8.1 μM against the A2780 human ovarian cancer cell line, as...

journal_title：Bioorganic & medicinal chemistry

authors： Liu Y,Harinantenaina L,Brodie PJ,Bowman JD,Cassera MB,Slebodnick C,Callmander MW,Randrianaivo R,Rakotobe E,Rasamison VE,Applequist W,Birkinshaw C,Lewis GP,Kingston DG

更新日期：2013-12-15 00:00:00

abstract：:In archaea the first general tetrapyrrole precursor 5-aminolevulinic acid (ALA) is formed via the tRNA-dependent five-carbon pathway from glutamate. We have cloned the hemA gene encoding the central enzyme of the pathway glutamyl-tRNA reductase from the methanogenic archaeon Methanobacterium thermoautotrophicum by com...

journal_title：Bioorganic & medicinal chemistry

authors： Hungerer C,Weiss DS,Thauer RK,Jahn D

更新日期：1996-07-01 00:00:00

abstract：:Six novel N(4)-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines and their N(2)-trimethylacetyl substituted analogs were synthesized as receptor tyrosine kinase (RTK) inhibitors. A microwave-mediated Sonogashira reaction was used as a key step for the synthesis of these compounds. Biol...

journal_title：Bioorganic & medicinal chemistry

authors： Gangjee A,Namjoshi OA,Yu J,Ihnat MA,Thorpe JE,Bailey-Downs LC

更新日期：2013-03-01 00:00:00

abstract：:The piperazine ring of the potent nootropic drug DM235 has been decorated with H-bond donor and acceptor groups (CH2OH, CH2OMe, CH2OCOMe, COOEt); the aim was to insert new functional groups, suitable for further chemical manipulation. The influence of these modifications on nootropic activity was assessed by means of ...

journal_title：Bioorganic & medicinal chemistry

authors： Martino MV,Guandalini L,Di Cesare Mannelli L,Menicatti M,Bartolucci G,Dei S,Manetti D,Teodori E,Ghelardini C,Romanelli MN

更新日期：2017-03-15 00:00:00

abstract：:5-Bromouracil ((Br)U) was incorporated into three types of synthetic RNA and the products of the photoirradiated (Br)U-containing RNAs were investigated using HPLC and MS analysis. The photoirradiation of r(GCA(Br)UGC)(2) and r(CGAA(Br)UUGC)/r(GCAAUUCG) in A-form RNA produced the corresponding 2'-keto adenosine ((keto...

journal_title：Bioorganic & medicinal chemistry

authors： Morinaga H,Kizaki S,Takenaka T,Kanesato S,Sannohe Y,Tashiro R,Sugiyama H

更新日期：2013-01-15 00:00:00

abstract：:Three haloderivatives of noscapine 2-4 were synthesized chemoselectively and their in vitro cytotoxicity was assessed by MTT assay on U-87 human glioblastoma cell lines. At 50 microM concentration after 72 h, 9-chloronoscapine 2, 9-bromonoscapine 3 (EM011), and 9-iodonoscapine 4 killed 87.8%, 51.2%, and 56.8% cells, r...

journal_title：Bioorganic & medicinal chemistry

authors： Verma AK,Bansal S,Singh J,Tiwari RK,Kasi Sankar V,Tandon V,Chandra R

更新日期：2006-10-01 00:00:00

abstract：:Further structure-activity relationship (SAR) studies with the 1,2,3,4-tetrahydroisoquinoline (THIQ) class of 5-HT(1A) ligands led to the synthesis of new 1-adamantoyloaminoalkyl derivatives. The impact of substituent variations in the aromatic part of THIQ moiety on 5-HT(1A) and 5-HT(2A) receptor affinities, as well ...

journal_title：Bioorganic & medicinal chemistry

authors： Bojarski AJ,Mokrosz MJ,Minol SC,Kozioł A,Wesołowska A,Tatarczyńska E,Kłodzińska A,Chojnacka-Wójcik E

更新日期：2002-01-01 00:00:00

abstract：:Vitamin E succinate selenium-conjugated molecules were synthesized and their apoptogenic properties were evaluated. 4-Methyl-2-phenylselenyl succinate (4) was prepared by the reaction of sodium benzeneselenolate with 2-bromosuccinic anhydrite in methanol solution. The methyl ester was converted to the acid (5) by hydr...

journal_title：Bioorganic & medicinal chemistry

authors： Vraka PS,Drouza C,Rikkou MP,Odysseos AD,Keramidas AD

更新日期：2006-04-15 00:00:00

abstract：:In this work, four series of tertiary amine-containing derivatives of 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents were prepared, and their in vitro antimycobacterial effects were evaluated. We found that the studied compounds showed lipophilicity-dependent antimycobacterial activity. The N-benzylp...

journal_title：Bioorganic & medicinal chemistry

authors： Roh J,Karabanovich G,Vlčková H,Carazo A,Němeček J,Sychra P,Valášková L,Pavliš O,Stolaříková J,Klimešová V,Vávrová K,Pávek P,Hrabálek A

更新日期：2017-10-15 00:00:00

abstract：:5-HT(7) receptor antagonists generated antidepressant-like effects in animal model and the involvement of the 5-HT(7) receptor in other pathophysiological mechanisms such as thermoregulation, learning and memory, and sleep has been highlighted by various studies. As one of our efforts to discover a new type of 5-HT(7)...

journal_title：Bioorganic & medicinal chemistry

authors： Na YH,Hong SH,Lee JH,Park WK,Baek DJ,Koh HY,Cho YS,Choo H,Pae AN

更新日期：2008-03-01 00:00:00

abstract：:Twenty-four asymmetric divalent head group cholesterol-based cationic lipids were designed and synthesized by parallel solid phase chemistry. These asymmetric head groups composed of amino functionality together with trimethylamino, di(2-hydroxyethyl)amino or guanidinyl groups. Spacers between cationic heads and linke...

journal_title：Bioorganic & medicinal chemistry

authors： Radchatawedchakoon W,Watanapokasin R,Krajarng A,Yingyongnarongkul BE

更新日期：2010-01-01 00:00:00

abstract：:P2X4 receptor has become an interesting molecular target for treatment and PET imaging of neuroinflammation and associated brain diseases such as Alzheimer's disease. This study reports the first design, synthesis, radiolabeling and biological evaluation of new candidate PET P2X4 receptor radioligands using 5-BDBD, a ...

journal_title：Bioorganic & medicinal chemistry

authors： Wang M,Gao M,Meyer JA,Peters JS,Zarrinmayeh H,Territo PR,Hutchins GD,Zheng QH

更新日期：2017-07-15 00:00:00

abstract：:The N-demethylation of 3-deoxymorphine (1) was investigated using methyl chloroformate and hydrazine. 3-Deoxynormorphine (2) was obtained in 70% yield, and 3-deoxydihydronormorphine (3) was also obtained as a side product. The mu, delta, and kappa receptor binding affinity of a series of N-substituted 3-deoxynormorphi...

journal_title：Bioorganic & medicinal chemistry

authors： Csutoras C,Zhang A,Bidlack JM,Neumeyer JL

更新日期：2004-05-15 00:00:00

abstract：:Twenty-seven natural product-like polyprenylated phenols and quinones were synthesized and their neuroprotective activity was tested using human monoamine oxidase B (MAO-B) and SH-SY5Y cells. Eight compounds inhibited MAO-B (IC50 values < 25 μM) and the inhibition mode and molecular docking of two (8c and 16c) were in...

journal_title：Bioorganic & medicinal chemistry

authors： Kamauchi H,Oda T,Horiuchi K,Takao K,Sugita Y

更新日期：2020-01-01 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 synthesis and optimization of a class of trisubstituted quinazoline-2,4(1H,3H)-dione cPLA(2)alpha inhibitors are described. Utilizing pharmacophores that were found to be important in our indole series, we discovered inhibitors with reduced lipophilicity and improved aqueous solubility. These compounds are active ...

journal_title：Bioorganic & medicinal chemistry

authors： Kirincich SJ,Xiang J,Green N,Tam S,Yang HY,Shim J,Shen MW,Clark JD,McKew JC

更新日期：2009-07-01 00:00:00

abstract：:The use of methanethiosulfonates as thiol-specific modifying reagents in the strategy of combined site-directed mutagenesis and chemical modification allows virtually unlimited opportunities for creating new protein surface environments. As a consequence of our interest in electrostatic manipulation as a means of tail...

journal_title：Bioorganic & medicinal chemistry

authors： Davis BG,Khumtaveeporn K,Bott RR,Jones JB

更新日期：1999-11-01 00:00:00

abstract：:We disclose herein our efforts aimed at discovery of selective PARP-1 and PARP-2 inhibitors. We have recently discovered several novel classes of quinazolinones, quinazolidinones, and quinoxalines as potent PARP-1 inhibitors, which may represent attractive therapeutic candidates. In PARP enzyme assays using recombinan...

journal_title：Bioorganic & medicinal chemistry

authors： Ishida J,Yamamoto H,Kido Y,Kamijo K,Murano K,Miyake H,Ohkubo M,Kinoshita T,Warizaya M,Iwashita A,Mihara K,Matsuoka N,Hattori K

更新日期：2006-03-01 00:00:00

abstract：:The discovery of the first class of potent glucose-6-phosphatase catalytic site inhibitors, substituted 4,5,6,7-tetrahydrothieno[3,2-c]- and -[2,3-c]pyridines, is described. Optimisation of this series involved solution phase combinatorial synthesis and very potent compounds were prepared with IC50 values down to 140 ...

journal_title：Bioorganic & medicinal chemistry

authors： Madsen P,Lundbeck JM,Jakobsen P,Varming AR,Westergaard N

更新日期：2000-09-01 00:00:00

abstract：:A series of indole analogs that are synthesized using the scaffold of a potent radiosensitizer, YTR107, were tested for their ability to alter the solubility of phosphorylated nucleophosmin 1 (pNPM1). NPM1 is critical for DNA double strand break (DSB) repair. In response to formation of DNA DSBs, phosphorylated T199 N...

journal_title：Bioorganic & medicinal chemistry

authors： Penthala NR,Crooks PA,Freeman ML,Sekhar KR

更新日期：2015-07-01 00:00:00

abstract：:There is still a need for additional scaffolds to further explore tissue selectivity and improving efficacy of selective estrogen receptor modulators (SERMs). A series of hydroxyl substituted diphenylnaphthyl alkene ligands for the two estrogen receptors are described that arose from an initial de novo designed diphen...

journal_title：Bioorganic & medicinal chemistry

authors： Schmidt JM,Tremblay GB,Plastina MA,Ma F,Bhal neé Basra S,Feher M,Dunn-Dufault R,Redden PR

更新日期：2005-03-01 00:00:00

abstract：:We synthesized homologated truncated 4'-thioadenosine analogues 3 in which a methylene (CH(2)) group was inserted in place of the glycosidic bond of a potent and selective A(3) adenosine receptor antagonist 2. The analogues were designed to induce maximum binding interaction in the binding site of the A(3) adenosine r...

journal_title：Bioorganic & medicinal chemistry

authors： Lee HW,Kim HO,Choi WJ,Choi S,Lee JH,Park SG,Yoo L,Jacobson KA,Jeong LS

更新日期：2010-10-01 00:00:00

abstract：:(-)-Cubebin showed a melanogenesis stimulation activity in a concentration-dependent manner in murine B16 melanoma cells without any significant effects on cell proliferation. Tyrosinase activity was increased at 24-72 h after addition of cubebin to B16 cells, and then intracellular melanin amount was increased at 48-...

journal_title：Bioorganic & medicinal chemistry

authors： Hirata N,Naruto S,Ohguchi K,Akao Y,Nozawa Y,Iinuma M,Matsuda H

更新日期：2007-07-15 00:00:00

abstract：:Bexarotene (1), a retinoid X receptor (RXR) agonist approved for the treatment of cutaneous T cell lymphoma (CTCL), was reported to migrate into baboon brain based on findings obtained by positron emission tomography (PET) with a 11C-labeled tracer. However, co-administration of non-radioactive 1 had no effect on the ...

journal_title：Bioorganic & medicinal chemistry

authors： Takamura Y,Shibahara O,Watanabe M,Fujihara M,Yamada S,Akehi M,Sasaki T,Hirano H,Kakuta H

更新日期：2019-07-15 00:00:00