Novel symmetrical ureas as modulators of protein arginine methyl transferases.

abstract：:Several studies have demonstrated that N-substituted amino acid derivatives exhibit weak anticonvulsant activities in vivo. In the present study, a series of amides of aminoacids structurally related to aminoacetamide have been synthesised and investigated for anticonvulsant activity. Among the molecules investigated,...

journal_title：Bioorganic & medicinal chemistry

authors： Ghidini E,Delcanale M,De Fanti R,Rizzi A,Mazzuferi M,Rodi D,Simonato M,Lipreri M,Bassani F,Battipaglia L,Bergamaschi M,Villetti G

更新日期：2006-05-15 00:00:00

abstract：:The syntheses of new nitroimidazole compounds using silicon-[(18)F]fluorine chemistry for the potential detection of tumor hypoxia are described. [(18)F]silicon-based compounds were synthesized by coupling 2-nitroimidazole with silyldinaphtyl or silylphenyldi-tert-butyl groups and labeled by fluorolysis or isotopic ex...

journal_title：Bioorganic & medicinal chemistry

authors： Joyard Y,Azzouz R,Bischoff L,Papamicaël C,Labar D,Bol A,Bol V,Vera P,Grégoire V,Levacher V,Bohn P

更新日期：2013-07-01 00:00:00

abstract：:The investigation of new Mn(II)-based MRI/Molecular Imaging probes responsive to the enzyme tyrosinase for potential diagnostic applications is herein described. The expression of the enzyme tyrosinase, an oxidoreductase, is up-regulated in melanoma cancer cells. Three novel ligands (L(1), L(2) and L(3)) were designed...

journal_title：Bioorganic & medicinal chemistry

authors： Rolla GA,Tei L,Fekete M,Arena F,Gianolio E,Botta M

更新日期：2011-02-01 00:00:00

abstract：:Hedgehog (Hh) signaling plays an important role in cell signaling of embryonic development and adult tissue homeostasis. In vertebrates, the hh gene encodes three different unique proteins: sonic hedgehog (Shh), desert hedgehog (Dhh) and indian hedgehog (Ihh). Disruption of the Hh signaling pathway leads to severe dis...

journal_title：Bioorganic & medicinal chemistry

authors： Büttner A,Seifert K,Cottin T,Sarli V,Tzagkaroulaki L,Scholz S,Giannis A

更新日期：2009-07-15 00:00:00

abstract：:The following study describes the synthesis of new benzanilide derivatives and their pharmacological investigation on smooth muscle preparations of guinea pigs. All compounds were synthesized in good yields and showed a spasmolytic activity without significant effect on vascular smooth muscles and heart muscle prepara...

journal_title：Bioorganic & medicinal chemistry

authors： Brunhofer G,Handler N,Leisser K,Studenik CR,Erker T

更新日期：2008-06-01 00:00:00

abstract：:Various 4-(anilino)pyrrole-2-carboxamides were designed and synthesized as novel androgen receptor (AR) antagonists without steroidal or anilide structure, based on our strategy for developing full antagonists of nuclear receptors. Introduction of a bulky N-alkyl group, such as a cyclohexylmethyl or benzyl group, incr...

journal_title：Bioorganic & medicinal chemistry

authors： Wakabayashi K,Imai K,Miyachi H,Hashimoto Y,Tanatani A

更新日期：2008-07-15 00:00:00

abstract：:A concise and efficient synthesis of cyclopentitols as a scaffold for a two-dimensional compound library for drug discovery is described. Starting from d-mannose, the key steps are Wittig olefination and ring-closing metathesis (RCM) followed by a [3,3]-sigmatropic Overmann rearrangement to form an sp(3)-rich, natural...

journal_title：Bioorganic & medicinal chemistry

authors： Padwal JD,Filippov DV,Narhe BD,Aertssen S,Beuving RJ,Benningshof JC,van der Marel GA,Overkleeft HS,van der Stelt M

更新日期：2015-06-01 00:00:00

abstract：:A combination of fluorophore and nucleobase through a π-conjugated rigid linker integrates the base pairing and the fluorescence change into a single event. Such base discriminating fluorophore can change its fluorescence as a direct response to the base pairing event and therefore have advantages over tethered labels...

journal_title：Bioorganic & medicinal chemistry

authors： Nim-Anussornkul D,Vilaivan T

更新日期：2017-12-15 00:00:00

abstract：:Three-dimensional quantitative structure-activity relationship (3D-QSAR) studies for 3-aryloxazolidin-2-one antibacterials were performed using the genetic function approximation algorithm. This study was performed using 60 compounds, in which the QSAR models were developed using a training set of 50 compounds. The in...

journal_title：Bioorganic & medicinal chemistry

authors： Karki RG,Kulkarni VM

更新日期：2001-12-01 00:00:00

abstract：:Cyanocobalamin (vitamin B12) is an essential nutrient as well as a very useful carrier in drug delivery. Conjugates of vitamin B12 are investigated due to their wide range of therapeutic applications. We report the synthesis of six vitamin B12 conjugates, and the effect of conjugation on their solubilities and stabili...

journal_title：Bioorganic & medicinal chemistry

authors： Wang X,Wei L,Kotra LP

更新日期：2007-02-15 00:00:00

abstract：:The problem of predicting torsadogenic cardiotoxicity of drugs is afforded in this work. QSAR studies on a series of molecules, acting as hERG K+ channel blockers, were carried out for this purpose by using the CODESSA program. Molecules belonging to the analyzed dataset are characterized by different therapeutic targ...

journal_title：Bioorganic & medicinal chemistry

authors： Coi A,Massarelli I,Murgia L,Saraceno M,Calderone V,Bianucci AM

更新日期：2006-05-01 00:00:00

abstract：:We designed, synthesized and evaluated 13 novel tricyclic indeno[2,1-d]pyrimidines as RTK inhibitors. These analogues were synthesized via a Dieckmann condensation of 1,2-phenylenediacetonitrile followed by cyclocondensation with guanidine carbonate to afford the 2-amino-3,9-dihydro-indeno[2,1-d]pyrimidin-4-one. Sulfo...

journal_title：Bioorganic & medicinal chemistry

authors： Gangjee A,Zhao Y,Ihnat MA,Thorpe JE,Bailey-Downs LC,Kisliuk RL

更新日期：2012-07-15 00:00:00

abstract：:The synthesis of the ethylenediamine-connected cyclodextrin dimer is reported, together with the syntheses of several reference cyclodextrinylamines. Each compound displayed enhanced transacylation or transphosphorylation of activated substrates, with the primary amine-bearing monocyclodextrin compound showing the gre...

journal_title：Bioorganic & medicinal chemistry

authors： Beeson JC,Czarnik AW

更新日期：1994-04-01 00:00:00

abstract：:A series of 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines were prepared and evaluated as potential allosteric modulators at the A(1) adenosine receptor. The structure-activity relationships of the 3- and 6-positions of a series of 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines were explored. Despite finding that ...

journal_title：Bioorganic & medicinal chemistry

authors： Aurelio L,Valant C,Figler H,Flynn BL,Linden J,Sexton PM,Christopoulos A,Scammells PJ

更新日期：2009-10-15 00:00:00

abstract：:A molecular modeling study meant to detect pharmacophore-like patterns in the active site of trypanothione reductase (TR) offered hints about the opportunity of synthesizing and testing diphenylsulfide derivatives with prolonged or branched polyamino side chains as putative TR inhibitors. The inhibition results within...

journal_title：Bioorganic & medicinal chemistry

authors： Baillet S,Buisine E,Horvath D,Maes L,Bonnet B,Sergheraert C

更新日期：1996-06-01 00:00:00

abstract：:The effect of 7,8-diacetoxy-4-methylcoumarin (DAMC) has been studied on hepatic NADPH cytochrome C reductase-- an enzyme participating in the microsomal electron transport. The preincubation of liver microsomes with DAMC resulted in a time-dependent activation of NADPH cytochrome C reductase. The catalytic activity of...

journal_title：Bioorganic & medicinal chemistry

authors： Raj HG,Parmar VS,Jain SC,Goel S,Singh A,Tyagi YK,Jha HN,Olsen CE,Wengel J

更新日期：1999-02-01 00:00:00

abstract：:A small library of spirooxindole-pyrrolidine hybrids have been synthesized for the first time in an ionic liquid, [bmim]Br in good to excellent yields employing a new class of non-stabilized azomethine ylides derived from isatin and tyrosine, a combination that has been rarely employed for the in situ generation of az...

journal_title：Bioorganic & medicinal chemistry

authors： Kumar RS,Almansour AI,Arumugam N,Mohammad F,Kotresha D,Menéndez JC

更新日期：2019-06-15 00:00:00

abstract：:The cytotoxicity showed by 1b, an interesting representant of the title compounds, for HT-29 human colon cancer cells (CI(50) value of 1.95 x 10(-7)M) has been related to the induced cell death at the G2 phase and not to DNA damage. This compound promotes the degradation of components of the G2/M checkpoint machinery,...

journal_title：Bioorganic & medicinal chemistry

authors： Ortín I,González JF,Cuesta Ede L,Manguan-García C,Perona R,Avendaño C

更新日期：2009-12-01 00:00:00

abstract：:A series of new isoxazolyl, triazolyl and phenyl based 3-thiophen-2-yl-quinoline derivatives were synthesized adopting click chemistry approach. In addition, the synthesis of new useful synthon, (2-chloroquinolin-3-yl) (thiophen-2-yl) methanol, is reported. The obtained compounds were characterized by spectral data an...

journal_title：Bioorganic & medicinal chemistry

authors： Othman DIA,Selim KB,El-Sayed MA,Tantawy AS,Amen Y,Shimizu K,Okauchi T,Kitamura M

更新日期：2019-10-01 00:00:00

abstract：:This report describes the synthesis and evaluation of glycosylated polyacrylate nanoparticles that have covalently-bound antibiotics within their framework. The requisite glycosylated drug monomers were prepared from one of three known antibiotics, an N-sec-butylthio beta-lactam, ciprofloxacin, and a penicillin, by ac...

journal_title：Bioorganic & medicinal chemistry

authors： Abeylath SC,Turos E,Dickey S,Lim DV

更新日期：2008-03-01 00:00:00

abstract：:To develop technetium and rhenium-labeled imaging agents for estrogen receptor (ER) positive breast tumors, we have prepared tridentate metal tricarbonyl chelates substituted at the 7alpha- and 17alpha-positions of estradiol. Some of the Re(CO)(3) conjugates have high binding for the ER in vitro. The in vivo biodistri...

journal_title：Bioorganic & medicinal chemistry

authors： Luyt LG,Bigott HM,Welch MJ,Katzenellenbogen JA

更新日期：2003-11-17 00:00:00

abstract：:A series of the 9-acetoxy enediyne compounds, 6a-k which were simplified from natural dynemicin A, and designed to be equipped with various aryl carbamate moieties, was synthesized and evaluated for DNA-cleaving ability, in vitro cytotoxicity, and in vivo antitumor activity. As a result of this study of the structure-...

journal_title：Bioorganic & medicinal chemistry

authors： Unno R,Michishita H,Inagaki H,Suzuki Y,Baba Y,Jomori T,Nishikawa T,Isobe M

更新日期：1997-05-01 00:00:00

abstract：:P-glycoprotein (P-gp) is known to mediate multidrug resistance (MDR) by acting as an efflux pump to actively transport chemotherapeutic agents out of carcinoma cells. Inhibition of P-gp function may represent one of the strategies to reverse MDR. We have previously reported that marchantin C (MC), a macrocyclic bisbib...

journal_title：Bioorganic & medicinal chemistry

authors： Xi GM,Sun B,Jiang HH,Kong F,Yuan HQ,Lou HX

更新日期：2010-09-15 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：:1α,25-Dihydroxyvitamin D3 exerts its actions by binding to vitamin D receptor (VDR). We are continuing the study related to the alteration of pocket structure of VDR by 22-alkyl substituent of ligands and the relationships between the alteration and agonistic/antagonistic activity. Previously we reported that compound...

journal_title：Bioorganic & medicinal chemistry

authors： Anami Y,Sakamaki Y,Itoh T,Inaba Y,Nakabayashi M,Ikura T,Ito N,Yamamoto K

更新日期：2015-11-15 00:00:00

abstract：:Research in recent years has demonstrated that the Trypanosoma cruzi cysteine protease cruzain (TCC) is a valid chemotherapeutic target, since inhibitors of this protease affect the pathology appropriately. By exploring the N-acylhydrazones (NAH) as privileged structures usually present in antiparasitic agents, we inv...

journal_title：Bioorganic & medicinal chemistry

authors： dos Santos Filho JM,Leite AC,de Oliveira BG,Moreira DR,Lima MS,Soares MB,Leite LF

更新日期：2009-09-15 00:00:00

abstract：:The malarial parasite Plasmodium falciparum encodes for an alpha-carbonic anhydrase (CA) enzyme possessing catalytic properties distinct of that of the human host, which was only recently purified. A series of aromatic sulfonamides, most of which were Schiff's bases derived from sulfanilamide/homosulfanilamide/4-amino...

journal_title：Bioorganic & medicinal chemistry

authors： Krungkrai J,Scozzafava A,Reungprapavut S,Krungkrai SR,Rattanajak R,Kamchonwongpaisan S,Supuran CT

更新日期：2005-01-17 00:00:00

abstract：:Both histone deacetylase (HDAC) and fibroblast growth factor receptor (FGFR) are important targets for cancer therapy. Although combining dual HDAC pharmacophore with tyrosine kinase inhibitors (TKIs) had achieved a successful progress, dual HDAC/FGFR1 inhibitors haven't been reported yet. Herein, we designed a series...

journal_title：Bioorganic & medicinal chemistry

authors： Liu J,Qian C,Zhu Y,Cai J,He Y,Li J,Wang T,Zhu H,Li Z,Li W,Hu L

更新日期：2018-02-01 00:00:00

abstract：:Due to the global threat of antibiotic resistance mediated by New Delhi metallo-beta-lactamase-1 (NDM-1) and the lack of structurally diverse inhibitors reported for this enzyme, we developed screening and counter-screening assays for manual and automated formats. The manual assay is a trans-well absorbance-based endp...

journal_title：Bioorganic & medicinal chemistry

authors： Thomas PW,Spicer T,Cammarata M,Brodbelt JS,Hodder P,Fast W

更新日期：2013-06-01 00:00:00

abstract：:Small molecules that act on multiple biological targets have been proposed to combat the drug resistance commonly observed for cancer chemotherapy. By combining the structural features of known inhibitors of inosine monophosphate dehydrogense (IMPDH) and histone deacetylase (HDAC), dual inhibitors of IMPDH and HDAC ba...

journal_title：Bioorganic & medicinal chemistry

authors： Chen L,Petrelli R,Gao G,Wilson DJ,McLean GT,Jayaram HN,Sham YY,Pankiewicz KW

更新日期：2010-08-15 00:00:00