Salicylanilide diethyl phosphates: synthesis, antimicrobial activity and cytotoxicity.

abstract：:Adenylyl cyclases (ACs) are promising pharmacological targets for treating heart failure, cancer, and psychosis. Ribose-substituted nucleotides have been reported as a potent family of AC inhibitors. In silico analysis of the docked conformers of such nucleotides in AC permits assembly of a consistent, intuitive QSAR ...

journal_title：Bioorganic & medicinal chemistry

authors： Wang JL,Guo JX,Zhang QY,Wu JJ,Seifert R,Lushington GH

更新日期：2007-04-15 00:00:00

abstract：:This review discusses all pyridine alkaloids with CNS activity, their therapeutic potential, and the interesting array of sources whence they originate. ...

journal_title：Bioorganic & medicinal chemistry

authors： Lin SX,Curtis MA,Sperry J

更新日期：2020-12-15 00:00:00

abstract：:Protein-protein interfaces are prominent in many therapeutically important targets. Using small organic molecules to disrupt protein-protein interactions is a current challenge in chemical biology. An important example of protein-protein interactions is provided by the Myc protein, which is frequently deregulated in h...

journal_title：Bioorganic & medicinal chemistry

authors： Xu Y,Shi J,Yamamoto N,Moss JA,Vogt PK,Janda KD

更新日期：2006-04-15 00:00:00

abstract：:We examined effects of alpha-, beta-galactosylceramides (CalCers) and alpha-, beta-glucosylceramides (GlcCers) on the syngeneic mixed leukocyte reaction (MLR) using spleen cells (responder cells) and dendritic cells (DC, stimulator cells). The DC pretreated with these alpha-monoglycosylceramides markedly stimulated th...

journal_title：Bioorganic & medicinal chemistry

authors： Iijima H,Kimura K,Sakai T,Uchimura A,Shimizu T,Ueno H,Natori T,Koezuka Y

更新日期：1998-10-01 00:00:00

abstract：:A series of novel benzofuran-dihydropyridine hybrids were designed by molecular hybridization approach and evaluated for bone anabolic activities. Among the screened library, ethyl 4-(7-(sec-butyl)-2-(4-methylbenzoyl)benzofuran-5-yl)-2-methyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate (compound 21) significant...

journal_title：Bioorganic & medicinal chemistry

authors： Modukuri RK,Choudhary D,Gupta S,Rao KB,Adhikary S,Sharma T,Siddiqi MI,Trivedi R,Sashidhara KV

更新日期：2017-12-15 00:00:00

abstract：:Glucuronide derivatives of CBI-bearing CC-1065 analogues have been synthesized, and their cytotoxicities tested against U937 leukemia cells. The new compounds show potent antitumor activity in vitro. Compounds 1 and 2, and their corresponding glucuronides 3 and 4 have IC(50) values of 0.6, 0.1, 1.4 and 0.6 nM, respect...

journal_title：Bioorganic & medicinal chemistry

authors： Wang Y,Yuan H,Wright SC,Wang H,Larrick JW

更新日期：2003-04-03 00:00:00

abstract：:We have used fluorescence anisotropy to measure in situ the thermodynamics of binding of alanine-rich mutants of the GCN4 basic region/leucine zipper (bZIP) to short DNA duplexes, in which thymines were replaced with uracils, in order to quantify the contributions of the C5 methyl group on thymines with alanine methyl...

journal_title：Bioorganic & medicinal chemistry

authors： Kise KJ Jr,Shin JA

更新日期：2001-09-01 00:00:00

abstract：:Based on our recent findings that piperine is a potent Staphylococcus aureus NorA efflux pump inhibitor (EPI), 38 piperine analogs were synthesized and bioevaluated for their EPI activity. Twenty-five of them were found active with potentiating activity equivalent or more than known EPIs like reserpine, carsonic acid ...

journal_title：Bioorganic & medicinal chemistry

authors： Sangwan PL,Koul JL,Koul S,Reddy MV,Thota N,Khan IA,Kumar A,Kalia NP,Qazi GN

更新日期：2008-11-15 00:00:00

abstract：:Valinol is part of numerous pharmaceuticals and has various other important applications. Optically pure valinol (ee >99%) was prepared employing different ω-transaminases from the corresponding prochiral hydroxy ketone. By the choice of the enzyme the (R)- as well as the (S)-enantiomer were accessible. Reductive amin...

journal_title：Bioorganic & medicinal chemistry

authors： Fuchs CS,Simon RC,Riethorst W,Zepeck F,Kroutil W

更新日期：2014-10-15 00:00:00

abstract：:This paper reports the synthesis of new derivatives (formed by two indole systems separated by a central moiety) analogous of potent antitumor agents previously described. The activity of the bis-indoles bearing a pyridine core confirms the good result described in the previous paper and compound 4c was chosen for the...

journal_title：Bioorganic & medicinal chemistry

authors： Andreani A,Burnelli S,Granaiola M,Leoni A,Locatelli A,Morigi R,Rambaldi M,Varoli L,Landi L,Prata C,Dalla Sega FV,Caliceti C,Shoemaker RH

更新日期：2010-05-01 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：:A series of 1,2,3-triazolylsalicylamide derivatives has been developed from the antiproliferative agent 7 and was evaluated for their Aurora kinase inhibitory activity. The novel 1,2,3-triazolylsalicylamide scaffold could be readily assembled by Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition, allowing rapid ac...

journal_title：Bioorganic & medicinal chemistry

authors： Song D,Park Y,Yoon J,Aman W,Hah JM,Ryu JS

更新日期：2014-09-01 00:00:00

abstract：:The clinical success of covalent kinase inhibitors in the treatment of EGFR-dependent non-small cell lung cancer (NSCLC) has rejuvenated the appreciation of reactive small molecules. Acquired drug resistance against first-line EGFR inhibitors remains the major bottleneck in NSCLC and is currently addressed by the appl...

journal_title：Bioorganic & medicinal chemistry

authors： Basu D,Richters A,Rauh D

更新日期：2015-06-15 00:00:00

abstract：:Bacterial DNA and synthetic oligodeoxynucleotides containing unmethylated CpG-motifs in a particular sequence context activate vertebrate immune cells. We examined the significance of negatively charged internucleoside linkages in the flanking sequences 5' and 3' to the CpG-motif on immunostimulatory activity. Cell pr...

journal_title：Bioorganic & medicinal chemistry

authors： Yu D,Kandimalla ER,Zhao Q,Cong Y,Agrawal S

更新日期：2001-11-01 00:00:00

abstract：:A novel series of pyridyl nitrofuranyl isoxazolines were synthesized and evaluated for their antibacterial activity against multiple drug resistant (MDR) Staphylococcus strains. Compounds with piperazine linker between the pyridyl group and isoxazoline ring showed better activity when compared to compounds without the...

journal_title：Bioorganic & medicinal chemistry

authors： Picconi P,Prabaharan P,Auer JL,Sandiford S,Cascio F,Chowdhury M,Hind C,Wand ME,Sutton JM,Rahman KM

更新日期：2017-08-01 00:00:00

abstract：:Three soft drug analogs and a metabolite of methatropine based on phenylsuccinic structural moiety were synthesized and tested for activity. In an in vivo assay, the soft drugs were found to be two orders of magnitude less potent than methatropine while the carboxylate metabolite was found to be one order of magnitude...

journal_title：Bioorganic & medicinal chemistry

authors： Hammer RH,Gunes E,Kumar GN,Wu WM,Srinivasan V,Bodor NS

更新日期：1993-09-01 00:00:00

abstract：:The design and evaluation of a novel decahydroisoquinolin scaffold as an inhibitor for severe acute respiratory syndrome (SARS) chymotrypsin-like protease (3CL(pro)) are described. Focusing on hydrophobic interactions at the S2 site, the decahydroisoquinolin scaffold was designed by connecting the P2 site cyclohexyl g...

journal_title：Bioorganic & medicinal chemistry

authors： Shimamoto Y,Hattori Y,Kobayashi K,Teruya K,Sanjoh A,Nakagawa A,Yamashita E,Akaji K

更新日期：2015-02-15 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：:Various estrogen analogs were synthesized and tested for binding to human ERα using a fluorescence polarization displacement assay. Binding affinity and orientation were also predicted using docking calculations. Docking was able to accurately predict relative binding affinity and orientation for estradiol, but only i...

journal_title：Bioorganic & medicinal chemistry

authors： McCullough C,Neumann TS,Gone JR,He Z,Herrild C,Wondergem Nee Lukesh J,Pandey RK,Donaldson WA,Sem DS

更新日期：2014-01-01 00:00:00

abstract：:To investigate the effect of elongating base-pair (bp) recognition sequences, we synthesized N-methylpyrrole-N-methylimidazole (PI) polyamide conjugates with eight-bp recognition (3-5). The DNA alkylating activities of conjugates 3-5 were evaluated by high-resolution denaturing polyacrylamide gel electrophoresis with ...

journal_title：Bioorganic & medicinal chemistry

authors： Takagaki T,Bando T,Kitano M,Hashiya K,Kashiwazaki G,Sugiyama H

更新日期：2011-10-01 00:00:00

abstract：:A series of anilides and phenyl esters of piperidine-3-carboxylic acid (nipecotic acid) were synthesized and tested for the ability to inhibit aggregation of human platelet rich-plasma triggered by adenosine 5'-diphosphate (ADP) and adrenaline. As a rule, amides were about two times more active than the corresponding ...

journal_title：Bioorganic & medicinal chemistry

authors： de Candia M,Summo L,Carrieri A,Altomare C,Nardecchia A,Cellamare S,Carotti A

更新日期：2003-04-03 00:00:00

abstract：:Two novel C(27)N(3)-type Lycopodium alkaloids, cryptadines A (1) and B (2) consisting of two octahydroquinoline rings (C(11)N) and a piperidine ring (C(5)N), have been isolated from the club moss Lycopodium cryptomerinum, and their structures and relative stereochemistry were elucidated on the basis of spectroscopic d...

journal_title：Bioorganic & medicinal chemistry

authors： Koyama K,Hirasawa Y,Kobayashi J,Morita H

更新日期：2007-12-15 00:00:00

abstract：:The 3-D QSAR analysis with new imidazo- and pyrrolo-quinolinedione derivatives was conducted by Comparative Molecular Field Analysis (CoMFA) and Comparative Molecular Similarity Indices Analysis (CoMSIA). When crossvalidation value (q(2)) is 0.844 at four components, the Pearson correlation coefficient (r(2)) of the C...

journal_title：Bioorganic & medicinal chemistry

authors： Suh ME,Kang MJ,Park SY

更新日期：2001-11-01 00:00:00

abstract：:A series of ring-constrained phenylpropyloxyethylamines, partial opioid structure analogs and derivatives of a previously studied sigma (σ) receptor ligand, was synthesized and evaluated at σ and opioid receptors for receptor selectivity. The results of this study identified several compounds with nanomolar affinity a...

journal_title：Bioorganic & medicinal chemistry

authors： Stavitskaya L,Seminerio MJ,Healy JR,Noorbakhsh B,Matsumoto RR,Coop A

更新日期：2013-09-01 00:00:00

abstract：:Three novel peptidomimetic phosphinate inhibitors have been synthesized and evaluated as inhibitors of matrix metalloproteinases MMP-2 and MMP-8. Their IC50 values are in the micromolar range, and one of them showed to be the most effective inhibitor of MMP-2. The differences in binding affinities for MMP-2 and MMP-8 ...

journal_title：Bioorganic & medicinal chemistry

authors： Bianchini G,Aschi M,Cavicchio G,Crucianelli M,Preziuso S,Gallina C,Nastari A,Gavuzzo E,Mazza F

更新日期：2005-08-01 00:00:00

abstract：:The four stereoisomeric 1,5-dideoxy-1,5-iminopentitols with D-arabino-(D-lyxo-) (3), ribo- (9), L-lyxo (L-arabino-) (13) and xylo-(18) configurations were synthesized. The corresponding aldonolactones (1, 7 and 11) or aldonic acid ester (15b) having a leaving group at C-5 gave by reaction with aqueous ammonia, the 5-a...

journal_title：Bioorganic & medicinal chemistry

authors： Godskesen M,Lundt I,Madsen R,Winchester B

更新日期：1996-11-01 00:00:00

abstract：:During the course of a collaborative screening program, a set of 1-phenyl-4-pyridyl-butadienes was found to exhibit in vitro activity against Eimeria tenella in a cell-based assay. Activity was dependent on the chain length and degree of unsaturation of the linker between the two aryl groups as well as substitution of...

journal_title：Bioorganic & medicinal chemistry

authors： Gage JL,Kirst HA,O'Neil D,David BA,Smith CK 2nd,Naylor SA

更新日期：2003-09-01 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：:(+)-4-Demethoxy-1,4-dimethyldaunomycinone 1 was synthesized using a convergent approach. Here, the key tetracyclic compound 10 was assembled by way of a Diels-Alder reaction using the sugar-based diene 8 and the quinizarin-related dienophile 7. ...

journal_title：Bioorganic & medicinal chemistry

authors： Kotha S,Stoodley RJ

更新日期：2002-03-01 00:00:00

abstract：:Semiempirical quantum mechanical and molecular mechanics calculations were carried out to identify and characterize the steric and electronic properties that modulate ligand recognition and activation of the cerebellar GABAA/benzodiazepine (BDZ) receptor. For this hypothesis development, thirteen compounds belonging t...

journal_title：Bioorganic & medicinal chemistry

authors： Schove LT,Perez JJ,Loew GH

更新日期：1994-10-01 00:00:00