N-substituted aminohydroxypyridines as potential non-opioid analgesic agents.

abstract：:Most of present molecular descriptors just consider the molecular structure. In the present article we pretend extending the use of Markov chain models to define novel molecular descriptors, which consider in addition to molecular structure other parameters like target site or toxic effect. Specifically, this molecula...

journal_title：Bioorganic & medicinal chemistry

authors： González-Díaz H,Cruz-Monteagudo M,Molina R,Tenorio E,Uriarte E

更新日期：2005-02-15 00:00:00

abstract：:RNA cleavage by enediyne anticancer antibiotics was shown to occur with no apparent sequence selectivity, but RNA structure appears to be important in those substrates where cleavage was observed. Neocarzinostatin (NCS) cleaved a wider variety of RNA substrates than either esperamicin (ESP) or calicheamicin (CAL), and...

journal_title：Bioorganic & medicinal chemistry

authors： Battigello JM,Cui M,Roshong S,Carter BJ

更新日期：1995-06-01 00:00:00

abstract：:A novel class of (E)-3,4-dihydroxy styryl sulfonamides and their 3,4-diacetylated derivatives as caffeic acid phenethyl ester (CAPE) analogs was designed and prepared for improving stability and solubility of the lead compound. Their neuroprotective properties were assessed by several models. The results showed that t...

journal_title：Bioorganic & medicinal chemistry

authors： Ning X,Guo Y,Ma X,Zhu R,Tian C,Zhang Z,Wang X,Ma Z,Liu J

更新日期：2013-09-01 00:00:00

abstract：:Introduction of an alkylcarboxylic acid unit, which is a partial structure of endogenous peroxisome proliferator-activated receptor (PPAR) ligands, into a phenethylphenylphthalimide skeleton, which possesses liver X receptor (LXR) antagonistic activity, afforded novel PPAR ligands. The results of structure-activity re...

journal_title：Bioorganic & medicinal chemistry

authors： Motoshima K,Ishikawa M,Hashimoto Y,Sugita K

更新日期：2011-05-15 00:00:00

abstract：:Two novel series of all-trans-beta-retinoic acid derivatives were synthesized and found to possess anticancer activity. The first series, cephalosporin 3'-retinoic esters 6 and 7 were, respectively, obtained by the condensation of all-trans-beta-retinoic acid (2) with cephalosporins 4 and 5. The second series, 7-(reti...

journal_title：Bioorganic & medicinal chemistry

authors： Hakimelahi GH,Ly TW,Yu SF,Zakerinia M,Khalafi-Nezhad A,Soltani MN,Gorgani MN,Chadegani AR,Moosavi-Movahedi AA

更新日期：2001-08-01 00:00:00

abstract：:Versatile method for living cell labeling has been established. Cell surfaces are initially biotinylated by azaelectrocyclization, and then treated with the fluorescence-labeled avidin or the anti-biotin antibody. ...

journal_title：Bioorganic & medicinal chemistry

authors： Tanaka K,Yokoi S,Morimoto K,Iwata T,Nakamoto Y,Nakayama K,Koyama K,Fujiwara T,Fukase K

更新日期：2012-03-15 00:00:00

abstract：:Glucose flux through glucokinase (GK) controls insulin release from the pancreas in response to high levels of glucose. Flux through GK is also responsible for reducing hepatic glucose output. Since many individuals with type 2 diabetes appear to have an inadequacy or defect in one or both of these processes, identify...

journal_title：Bioorganic & medicinal chemistry

authors： Hinklin RJ,Baer BR,Boyd SA,Chicarelli MD,Condroski KR,DeWolf WE Jr,Fischer J,Frank M,Hingorani GP,Lee PA,Neitzel NA,Pratt SA,Singh A,Sullivan FX,Turner T,Voegtli WC,Wallace EM,Williams L,Aicher TD

更新日期：2020-01-01 00:00:00

abstract：:A novel series of acetamide-substituted derivatives and two prodrugs of doravirine were designed and synthesized as potent HIV-1 NNRTIs by employing the structure-based drug design strategy. In MT-4 cell-based assays using the MTT method, it was found that most of the new compounds exhibited moderate to excellent inhi...

journal_title：Bioorganic & medicinal chemistry

authors： Wang Z,Yu Z,Kang D,Zhang J,Tian Y,Daelemans D,De Clercq E,Pannecouque C,Zhan P,Liu X

更新日期：2019-02-01 00:00:00

abstract：:Epolactaene, a neuritogenic compound in human neuroblastoma SH-SY5Y, induces apoptosis in a human leukemia B-cell line, BALL-1. The apoptosis-inducing activities of 34 epolactaene derivatives, including those of the newly synthesized alpha-alkyl-alpha,beta-epoxy-gamma-lactam derivative and cyclopropane derivatives, we...

journal_title：Bioorganic & medicinal chemistry

authors： Kuramochi K,Matsui R,Matsubara Y,Nakai J,Sunoki T,Arai S,Nagata S,Nagahara Y,Mizushina Y,Ikekita M,Kobayashi S

更新日期：2006-04-01 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：:Hetero-Diels-Alder reactions of 1,3-bis(silyloxy)-1,3-butadienes with arylsulfonylcyanides afforded a variety of 4-hydroxy-2-(arylsulfonyl)pyridines. Several derivatives show antimicrobial activity against Gram-positive bacteria. ...

journal_title：Bioorganic & medicinal chemistry

authors： Hussain I,Yawer MA,Lalk M,Lindequist U,Villinger A,Fischer C,Langer P

更新日期：2008-12-01 00:00:00

abstract：:The conformational profiles of a selected group of a new series of small linear and cyclic penta- and hexapeptides, inspired on the C-terminal segment of second-generation bradykinin (BK) antagonists, were independently computed in order to assess the chemical and geometrical requirements necessary for BK antagonism. ...

journal_title：Bioorganic & medicinal chemistry

authors： Filizola M,Llorens O,Cartení-Farina M,Perez JJ

更新日期：1998-09-01 00:00:00

abstract：:A series of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles 14a-e, 15a-e, 17a-c, and 18a-d have been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The 6-quinolinyl pyrazole analogue 14b inhibited ALK5 phosphorylation ...

journal_title：Bioorganic & medicinal chemistry

authors： Jin CH,Krishnaiah M,Sreenu D,Rao KS,Subrahmanyam VB,Park CY,Son JY,Sheen YY,Kim DK

更新日期：2011-04-15 00:00:00

abstract：:In vitro studies, using combined spectrophotometry and oximetry together with hplc/ms examination of the products of tyrosinase action demonstrate that hydroquinone is not a primary substrate for the enzyme but is vicariously oxidised by a redox exchange mechanism in the presence of either catechol, L-3,4-dihydroxyphe...

journal_title：Bioorganic & medicinal chemistry

authors： Stratford MR,Ramsden CA,Riley PA

更新日期：2012-07-15 00:00:00

abstract：:The need for novel therapeutic options to fight herpesvirus infections still persists. Herein we report the design, synthesis and antiviral evaluation of a new family of non-nucleoside antivirals, derived from 1-[ω-(4-bromophenoxy)alkyl]uracil derivatives--previously reported inhibitors of human cytomegalovirus (HCMV)...

journal_title：Bioorganic & medicinal chemistry

authors： Babkov DA,Khandazhinskaya AL,Chizhov AO,Andrei G,Snoeck R,Seley-Radtke KL,Novikov MS

更新日期：2015-11-01 00:00:00

abstract：:A library of 1,4-benzodiazepines has been synthesised and evaluated for activity against Trypanosoma brucei, a causative parasite of Human African Trypanosomiasis (HAT). The most potent of these derivatives has an MIC value of 0.97 μM. Herein we report the design, synthesis and biological evaluation of the abovementio...

journal_title：Bioorganic & medicinal chemistry

authors： Clark RL,Clements CJ,Barrett MP,Mackay SP,Rathnam RP,Owusu-Dapaah G,Spencer J,Huggan JK

更新日期：2012-10-15 00:00:00

abstract：:Thirty three derivatives of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues were synthesized by molecular modification of a reported antimycobacterial molecule (GSK163574A). Compounds were evaluated in vitro against actively replicative and nutrient starved non-replicative Mycobacter...

journal_title：Bioorganic & medicinal chemistry

authors： Samala G,Brindha Devi P,Saxena S,Gunda S,Yogeeswari P,Sriram D

更新日期：2016-11-01 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：:Platinum compounds are the first-line therapy for many types of cancer. However, drug resistance has frequently been reported for and is a major limitation of platinum-based chemotherapy in the clinic. In the current study, we examined the anti-tumor activity of phomoxanthone A (PXA), a tetrahydroxanthone dimer isolat...

journal_title：Bioorganic & medicinal chemistry

authors： Wang C,Engelke L,Bickel D,Hamacher A,Frank M,Proksch P,Gohlke H,Kassack MU

更新日期：2019-10-01 00:00:00

abstract：:A novel series of naphthalimide-cyclam conjugates were designed and synthesized. Among them, compounds 4c, 4d, 8c and 8d which bearing long lipophilic alkyl chains, displayed comparable or more potent cytotoxic activities against human tumor cell lines than amonafide. Furthermore, the four compounds were proved to pos...

journal_title：Bioorganic & medicinal chemistry

authors： Tan S,Sun D,Lyu J,Sun X,Wu F,Li Q,Yang Y,Liu J,Wang X,Chen Z,Li H,Qian X,Xu Y

更新日期：2015-09-01 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：:In earlier investigations we have described the synthesis and biological evaluation of a panel of novel glycosylated heteroaromatics (1-12). It was found that these compounds can bind to DNA in vitro and are cytotoxic against several cancer cell lines at low micromolar concentration. We report here structure-activity ...

journal_title：Bioorganic & medicinal chemistry

authors： Shi W,Lowary TL

更新日期：2011-03-01 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

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：:Thiol- or acid-promoted additions of silyl radicals to camptothecin are reported. At 105 degrees C, mixtures of 7-silyl (favored) and 12-silyl camptothecins are formed alongside substantial amounts of recovered camptothecin. At 160 degrees C, 12-silyl isomers are formed preferentially, but the total mass balance is su...

journal_title：Bioorganic & medicinal chemistry

authors： Du W,Kaskar B,Blumbergs P,Subramanian PK,Curran DP

更新日期：2003-02-06 00:00:00

abstract：:One of the grand challenges in chemical biology is identifying a small-molecule modulator for each individual function of all human proteins. Instead of targeting one protein at a time, an efficient approach to address this challenge is to target entire protein families by taking advantage of the relatively high level...

journal_title：Bioorganic & medicinal chemistry

authors： Areias FM,Brea J,Gregori-Puigjané E,Zaki ME,Carvalho MA,Domínguez E,Gutiérrez-de-Terán H,Proença MF,Loza MI,Mestres J

更新日期：2010-05-01 00:00:00

abstract：:To detect γ-Glutamyl Transpeptidase (GGT) activity in vitro and in vivo, a bioluminescence probe with high sensitivity and specificity was well designed and synthesized. This probe can be recognized by GGT and release strong bioluminescence with its further reaction with luciferase. The performance of this probe was d...

journal_title：Bioorganic & medicinal chemistry

authors： Lin Y,Gao Y,Ma Z,Jiang T,Zhou X,Li Z,Qin X,Huang Y,Du L,Li M

更新日期：2018-01-01 00:00:00

abstract：:Focusing on alpha-pyridoin (1, 1,2-di(2-pyridyl)-1,2-ethenediol) as the lead compound of the novel antioxidative enediol, we synthesized 5,5'- or 6,6'-bis-substituted derivatives of 1 from disubstituted pyridines. The antioxidant activity of 1 and its synthetic derivatives 2-7 was evaluated by DPPH (1,1-diphenyl-2-pic...

journal_title：Bioorganic & medicinal chemistry

authors： Hatanaka M,Takahashi K,Nakamura S,Mashino T

更新日期：2005-12-15 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：:Polyamines and polyamine toxins are biologically important molecules, having modulatory effects on nucleotides and proteins. The wasp toxin, philanthotoxin-433 (PhTX-433), is a non-selective and uncompetitive antagonist of ionotropic receptors, such as ionotropic glutamate receptors and nicotinic acetylcholine recepto...

journal_title：Bioorganic & medicinal chemistry

authors： Andersen TF,Vogensen SB,Jensen LS,Knapp KM,Strømgaard K

更新日期：2005-09-01 00:00:00