The influence of substitution at aromatic part of 1,2,3,4-tetrahydroisoquinoline on in vitro and in vivo 5-HT(1A)/5-HT(2A) receptor activities of its 1-adamantoyloaminoalkyl derivatives.

abstract：:The synthesis and binding affinities of 32 X3Gly4 dual-substitution analogues of the natural opioid heptapeptides deltorphin I and II are reported. A multiple regression QSAR analysis was performed using those results along with literature data for the X3Asp4 and Phe3X4 side chain analogues. Fitting to a three-term po...

journal_title：Bioorganic & medicinal chemistry

authors： Schullery SE,Mohammedshah T,Makhlouf H,Marks EL,Wilenkin BS,Escobar S,Mousigian C,Heyl DL

更新日期：1997-12-01 00:00:00

abstract：:Breast cancer is the second most common cancer worldwide after lung cancer with the vast majority of early stage breast cancers being hormone-dependent. One of the major therapeutic advances in the clinical treatment of breast cancer has been the introduction of selective estrogen receptor modulators (SERMs). We descr...

journal_title：Bioorganic & medicinal chemistry

authors： Kelly PM,Bright SA,Fayne D,Pollock JK,Zisterer DM,Williams DC,Meegan MJ

更新日期：2016-09-15 00:00:00

abstract：:Three fluoroalkylated derivatives (1-3) of the selective estrogen receptor modulator (SERM), raloxifene, have been synthesized. The key step in the synthesis is the C-C bond formation of benzo[b]thiophene and a substituted phenyl group (ring C) using a Stille reaction. The in vitro binding affinities of the substitute...

journal_title：Bioorganic & medicinal chemistry

authors： Lee KC,Moon BS,Lee JH,Chung KH,Katzenellenbogen JA,Chi DY

更新日期：2003-08-15 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：:We previously identified dibenzooxepine derivative 1 as a potent PPARγ ligand with a unique binding mode owing to its non-thiazolidinedione scaffold. However, while 1 showed remarkably potent MKN-45 gastric cancer cell aggregation activity, an indicator of cancer differentiation-inducing activity induced by PPARγ acti...

journal_title：Bioorganic & medicinal chemistry

authors： Yamamoto K,Tamura T,Nakamura R,Hosoe S,Matsubara M,Nagata K,Kodaira H,Uemori T,Takahashi Y,Suzuki M,Saito JI,Ueno K,Shuto S

更新日期：2019-11-15 00:00:00

abstract：:A series of anacardic acid analogues possessing different side chains viz. phenolic, branched, and alicyclic were synthesized and their antibacterial activity tested against methicillin-resistant Staphylococcus aureus (MRSA). The maximum activity against this bacterium occurred with the branched side-chain analogue, 6...

journal_title：Bioorganic & medicinal chemistry

authors： Green IR,Tocoli FE,Lee SH,Nihei K,Kubo I

更新日期：2007-09-15 00:00:00

abstract：:A series of (2E,2'E)-1,1'-(3-hydroxy-5-methylbiphenyl-2,6-diyl)-bis(3-pheylprop-2-ene-1-ones (5-33) were prepared by the reaction of 1,3-diacetyl biphenyls (1-4) with different aldehydes in presence of catalytic amount of solid KOH in ethanol in excellent yields. The compounds were evaluated for anticancer activity ag...

journal_title：Bioorganic & medicinal chemistry

authors： Sharma A,Chakravarti B,Gupt MP,Siddiqui JA,Konwar R,Tripathi RP

更新日期：2010-07-01 00:00:00

abstract：:The dopamine D4 receptor has been shown to play key roles in certain CNS pathologies including addiction to cigarette smoking. Thus, selective D4 ligands may be useful in treating some of these conditions. Previous studies in our laboratory have indicated that the piperazine analog of haloperidol exhibits selective an...

journal_title：Bioorganic & medicinal chemistry

authors： Sampson D,Zhu XY,Eyunni SV,Etukala JR,Ofori E,Bricker B,Lamango NS,Setola V,Roth BL,Ablordeppey SY

更新日期：2014-06-15 00:00:00

abstract：:To develop nonprostanoid prostacyclin receptor agonists with a high degree of metabolic resistance and an extended duration of action, a novel series of diphenylpyrazine derivatives was synthesized and evaluated for their inhibition of ADP-induced human platelet aggregation. Structure-activity relationship studies on ...

journal_title：Bioorganic & medicinal chemistry

authors： Asaki T,Hamamoto T,Sugiyama Y,Kuwano K,Kuwabara K

更新日期：2007-11-01 00:00:00

abstract：:The kainoids are a class of excitatory and excitotoxic pyrrolidine dicarboxylates that act at ionotropic glutamate receptors. The kainoids bind kainate receptors with high affinity and, while binding affinity is lower at AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptors, they are active in func...

journal_title：Bioorganic & medicinal chemistry

authors： Carcache LM,Rodriguez J,Rein KS

更新日期：2003-02-20 00:00:00

abstract：:Therapeutic development of a targeted agent involves a series of decisions over additional activities that may be ignored, eliminated or pursued. This paper details the concurrent application of two methods that provide a spectrum of information about the biological activity of a compound: biochemical profiling on a l...

journal_title：Bioorganic & medicinal chemistry

authors： Ross-Macdonald P,de Silva H,Patel V,Truong A,He A,Neuhaus I,Tilford C,Ji R,Siemers N,Greer A,Carboni J,Gottardis M,Menard K,Lee F,Dodier M,Frennesson D,Sampognaro A,Saulnier M,Trainor G,Vyas D,Zimmermann K,Wittm

更新日期：2012-03-15 00:00:00

abstract：:A series of novel tetrahydropyrazolopyridone derivatives containing 1,3,4-triazole, triazolylmethyl, and partially saturated heterocyclic moieties as P2 binding element was designed, synthesized, and evaluated in vitro for anticoagulant activity in human and rabbit plasma. All compounds showed moderate to significant ...

journal_title：Bioorganic & medicinal chemistry

authors： Sun X,Hong Z,Liu M,Guo S,Yang D,Wang Y,Lan T,Gao L,Qi H,Gong P,Liu Y

更新日期：2017-05-15 00:00:00

abstract：:Amyotrophic lateral sclerosis (ALS) is an orphan neurodegenerative disease currently without a cure. Mutations in copper/zinc superoxide dismutase 1 (SOD1) have been implicated in the pathophysiology of this disease. Using a high-throughput screening assay expressing mutant G93A SOD1, two bioactive chemical hit compou...

journal_title：Bioorganic & medicinal chemistry

authors： Chen T,Benmohamed R,Arvanites AC,Ralay Ranaivo H,Morimoto RI,Ferrante RJ,Watterson DM,Kirsch DR,Silverman RB

更新日期：2011-01-01 00:00:00

abstract：:The Wnt signaling pathway plays a key role in organ and tissue homeostasis, and when dysregulated, can become a major underlying mechanism of disease, particularly cancer. We reported previously that the anthelmintic drug Niclosamide inhibits Wnt/β-catenin signaling and suppresses colon cancer cell growth in vitro and...

journal_title：Bioorganic & medicinal chemistry

authors： Mook RA Jr,Ren XR,Wang J,Piao H,Barak LS,Kim Lyerly H,Chen W

更新日期：2017-03-15 00:00:00

abstract：:Theoretical and structural studies followed by the directed synthesis and in vitro biological tests lead us to novel noncovalent thrombin pseudopeptide inhibitors. We have incorporated an azapeptide scaffold into the central part of the classical tripeptide D-Phe-Pro-Arg inhibitor structure thus eliminating one stereo...

journal_title：Bioorganic & medicinal chemistry

authors： Zega A,Mlinsek G,Sepic P,Golic Grdadolnik S,Solmajer T,Tschopp TB,Steiner B,Kikelj D,Urleb U

更新日期：2001-10-01 00:00:00

abstract：:To establish the role of the ferrocenyl moiety in the antiplasmodial activity of ferroquine, compounds in which this moiety is replaced by the corresponding ruthenium-based moieties were synthesized and evaluated. In both the sensitive (D10) and resistant (K1) strains of Plasmodium falciparum, ruthenoquine analogues s...

journal_title：Bioorganic & medicinal chemistry

authors： Blackie MA,Beagley P,Croft SL,Kendrick H,Moss JR,Chibale K

更新日期：2007-10-15 00:00:00

abstract：:Neurotoxic organophosphorus compounds (OPs), which are used as pesticides and chemical warfare agents lead to more than 700,000 intoxications worldwide every year. The main target of OPs is the inhibition of acetylcholinesterase (AChE), an enzyme necessary for the control of the neurotransmitter acetylcholine (ACh). T...

journal_title：Bioorganic & medicinal chemistry

authors： da Cunha Xavier Soares SF,Vieira AA,Delfino RT,Figueroa-Villar JD

更新日期：2013-09-15 00:00:00

abstract：:A satisfactory model is developed using CODESSA PRO for the correlation and prediction of milk to plasma concentration ratios (M/P ratio) for diverse pharmaceuticals. A set of experimentally derived M/P ratio values were collected from the literature for 115 widely used pharmaceuticals. The experimental logarithmic M/...

journal_title：Bioorganic & medicinal chemistry

authors： Katritzky AR,Dobchev DA,Hür E,Fara DC,Karelson M

更新日期：2005-03-01 00:00:00

abstract：:Synthesis and base-pairing studies of two 2'-deoxyribonucleosides, containing a common heterocyclic base, 7(4)-amino-5(6)H-imidazo[4,5-d]pyridazin-4(7)one (1 and 2), have been reported. The synthesis was accomplished by base-promoted deoxyribosylation of ethyl 5(4)-cyanoimidazole-4(5)-carboxylate (6), followed by ring...

journal_title：Bioorganic & medicinal chemistry

authors： Ujjinamatada RK,Paulman RL,Ptak RG,Hosmane RS

更新日期：2006-09-15 00:00:00

abstract：:The nitronate and nitrovinyl methods to synthesize indole glucosinolates (GLs) have been investigated. The results were applied to generally the most prevalent natural indole glucosinolates to synthesize 4-methoxyglucobrassicin (MGB) and neo-glucobrassicin (NGB) in moderate overall yield for the first time. The anti-i...

journal_title：Bioorganic & medicinal chemistry

authors： Vo QV,Trenerry C,Rochfort S,Wadeson J,Leyton C,Hughes AB

更新日期：2014-01-15 00:00:00

abstract：:DNA and DNA-related enzymes are one of the most effective and common used intracellular anticancer targets in clinic and laboratory studies, however, most of DNA-targeting drugs suffered from toxic side effects. Development of new molecules with good antitumor activity and low side effects is important. Based on compu...

journal_title：Bioorganic & medicinal chemistry

authors： Li D,Yuan Z,Chen S,Zhang C,Song L,Gao C,Chen Y,Tan C,Jiang Y

更新日期：2017-07-01 00:00:00

abstract：:γ-Aminobutyric acid (GABA) receptors are important targets of parasiticides/insecticides. Several 4-substituted analogs of the partial GABAA receptor agonist 5-(4-piperidyl)-3-isothiazolol (Thio-4-PIOL) were synthesized and examined for their antagonism of insect GABA receptors expressed in Drosophila S2 cells or Xeno...

journal_title：Bioorganic & medicinal chemistry

authors： Liu G,Furuta K,Nakajima H,Ozoe F,Ozoe Y

更新日期：2014-09-01 00:00:00

abstract：:Peptidomimetic compounds possessing a caprolactam ring constraint were prepared and evaluated as interleukin-1beta converting enzyme (ICE) inhibitors. The caprolactam ring was used to constrain the P3 region of our inhibitors. This strategy proved to be effective for the synthesis of ICE inhibitors, maintaining key hy...

journal_title：Bioorganic & medicinal chemistry

authors： Wang Y,O'Neil SV,Wos JA,Oppong KA,Laufersweiler MC,Soper DL,Ellis CD,Baize MW,Fancher AN,Lu W,Suchanek MK,Wang RL,Schwecke WP,Cruze CA,Buchalova M,Belkin M,De B,Demuth TP Jr

更新日期：2007-02-01 00:00:00

abstract：:We have developed a method for the chemoselective introduction of spacer modified biotin labels into unprotected multi-functional amines. A range of novel biotin spacer conjugates attached to a polymer-bound sulfonamide anchor was prepared using established amide bond forming procedures. After chemical transformation ...

journal_title：Bioorganic & medicinal chemistry

authors： Herforth C,Heidler P,Franke S,Link A

更新日期：2004-06-01 00:00:00

abstract：:A new class of compounds--acridone derivatives--was tested using the direct fluorometric helicase activity assay to determine the inhibitory properties of the derivatives towards the NS3 helicase of Hepatitis C virus (HCV). The compounds were also tested as putative transcription inhibitors of in vitro transcription b...

journal_title：Bioorganic & medicinal chemistry

authors： Stankiewicz-Drogon A,Palchykovska LG,Kostina VG,Alexeeva IV,Shved AD,Boguszewska-Chachulska AM

更新日期：2008-10-01 00:00:00

abstract：:Cyclopentane derivatives, designated as BCX-1812, BCX-1827, BCX-1898, and BCX-1923, were tested in parallel with oseltamivir carboxylate and zanamivir for the in vivo activity in mice infected with A/Turkey/Mas/76 X A/Beijing/32/92 (H6N2) influenza virus. The compounds were tested orally and intranasally at different ...

journal_title：Bioorganic & medicinal chemistry

authors： Chand P,Bantia S,Kotian PL,El-Kattan Y,Lin TH,Babu YS

更新日期：2005-06-02 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：:Synthetic modification of cyclosporin A at P3-P4 positions led to the discovery of NIM258, a next generation cyclophilin inhibitor with excellent anti-hepatitis C virus potency, with decreased transporter inhibition, and pharmacokinetics suitable for coadministration with other drugs. Herein is disclosed the evolution...

journal_title：Bioorganic & medicinal chemistry

authors： Fu J,Becker C,Cao L,Capparelli M,Denay R,Fujimoto R,Gai Y,Gao Z,Guenat C,Karur S,Kim H,Li W,Li X,Li W,Lochmann T,Lu A,Lu P,Luneau A,Meier N,Mergo W,Ng S,Parker D,Peng Y,Riss B,Rivkin A,Roggo S,Schroede

更新日期：2018-02-15 00:00:00

abstract：:In our previous work, a series of 2-amino-3,4-dihydroquinazoline derivativesusing an electron acceptor group was reported to be potent T-type calcium channel blockers and exhibit strong cytotoxic effects against various cancerous cell lines. To investigate the role of the guanidine moiety in the 2-amino-3,4-dihydroqui...

journal_title：Bioorganic & medicinal chemistry

authors： Nam Y,Ryu KD,Jang C,Moon YH,Kim M,Ko D,Chung KS,Gandini MA,Lee KT,Zamponi GW,Lee JY

更新日期：2020-06-01 00:00:00

abstract：:Removal of each of the acyl groups of thapsigargin at O-3, O-8 and O-10 significant reduces the affinity of the inhibitors to the SERCA1a pump. Replacement of the acyl groups at O-3 and O-10 with flexible residues could be performed with only a minor decrease of the affinity, whereas introduction of voluminous stiff r...

journal_title：Bioorganic & medicinal chemistry

authors： Skytte DM,Møller JV,Liu H,Nielsen HØ,Svenningsen LE,Jensen CM,Olsen CE,Christensen SB

更新日期：2010-08-01 00:00:00