Novel pyrazolo[1,5-a]pyrimidines as c-Src kinase inhibitors that reduce IKr channel blockade.

abstract：:Seven new nitrogen heterocycle porphyrins, 5,10,15,20-tetra[4-(N-pyrrolidinyl)phenyl]porphine (TBPPH(2)), 5,10,15,20-tetra[4-(4'-ethylpiperazinyl)phenyl]porphine (TEPPH(2)), 5,10,15,20-tetra [4-(4'-butylpiperazinyl)phenyl]porphine (TUPPH(2)), 5,10,15,20-tetra[4-(4'-heptylpiperazinyl) phenyl]porphine (THPPH(2)), 5-[4-(...

journal_title：Bioorganic & medicinal chemistry

authors： Guo CC,Li HP,Zhang XB

更新日期：2003-04-17 00:00:00

abstract：:1,4,7-Trisubstituted isoquinolines were designed, synthesized and evaluated for their inhibition against Plasmodium falciparum cysteine protease falcipain-2. The 1-benzyloxyphenyl-dihydroisoquinoline and -isoquinoline derivatives were found to exhibit better activity against falcipain-2 than their corresponding 1-hydr...

journal_title：Bioorganic & medicinal chemistry

authors： Batra S,Sabnis YA,Rosenthal PJ,Avery MA

更新日期：2003-05-15 00:00:00

abstract：:The series of des-Cl (unsubstituted) and m-Cl phenyl analogues of PYR with various flexible 6-substituents were synthesized and studied for the binding affinities with highly resistant quadruple mutant (QM) DHFR. The derivatives carrying 4 atoms linker with a terminal carboxyl substituted on the aromatic ring exhibite...

journal_title：Bioorganic & medicinal chemistry

authors： Saepua S,Sadorn K,Vanichtanankul J,Anukunwithaya T,Rattanajak R,Vitsupakorn D,Kamchonwongpaisan S,Yuthavong Y,Thongpanchang C

更新日期：2019-12-15 00:00:00

abstract：:The boronic acid group is widely used in chemosensor design due to its ability to reversibly bind diol-containing compounds. The thermodynamic properties of the boronic acid-diol binding process have been investigated extensively. However, there are few studies of the kinetic properties of such binding processes. In t...

journal_title：Bioorganic & medicinal chemistry

authors： Ni N,Laughlin S,Wang Y,Feng Y,Zheng Y,Wang B

更新日期：2012-05-01 00:00:00

abstract：:A series of 8-hydroxyquinolin derivatives substituted with (benzo[d][1,2]selenazol-3(2H)-one) at the 2-position were synthesized and evaluated for treatment of Alzheimer's disease. In vitro assays demonstrated that most of the target compounds exhibit significant inhibition of Cu(II)-induced Aβ1-42 aggregation, rapid ...

journal_title：Bioorganic & medicinal chemistry

authors： Wang B,Wang Z,Chen H,Lu CJ,Li X

更新日期：2016-10-01 00:00:00

abstract：:Combinatorial biocatalysis, based on a principle of the combinatorial use of biosynthetic steps rather than the combinatorial use of reagents, offers a complementary approach to combinatorial chemistry, which, used individually or in connection with synthetic organic transformations, provides access to analogues not r...

journal_title：Bioorganic & medicinal chemistry

authors： Krstenansky JL,Khmelnitsky Y

更新日期：1999-10-01 00:00:00

abstract：:In order to find novel and environmental friendly insecticides targeting the ryanodine receptor, three series of novel phthalamides containing heptafluoroisopropyl group, low fluorine atoms group and non-fluorine group were designed and synthesized. 35 novel structures of three series were obtained. Insecticidal activ...

journal_title：Bioorganic & medicinal chemistry

authors： Chen Y,Li Y,Pan L,Liu J,Wan Y,Chen W,Xiong L,Yang N,Song H,Li Z

更新日期：2014-11-15 00:00:00

abstract：:Fourteen hybrids of farnesylthiosalicylic acid (FTS) with various diamines were synthesized and biologically evaluated. It was found that FTS-monoamide molecules (10a-g) displayed strong anti-proliferative activity against seven human cancer cell lines, superior to FTS and FTS-bisamide compounds (11a-g). The mono-amid...

journal_title：Bioorganic & medicinal chemistry

authors： Ling Y,Wang Z,Zhu H,Wang X,Zhang W,Wang X,Chen L,Huang Z,Zhang Y

更新日期：2014-01-01 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 cyclohexyl piperazine 1 (1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydro-naphthalen-1-yl)-propyl]-piperazine) has been shown to be a potent and selective sigma-2 receptor ligand. In the present study, we prepared [(11)C]1 by O-alkylation of the phenolic precursor 2 with [(11)C]CH(3)I. [(11)C]1 was obtained in a 29...

journal_title：Bioorganic & medicinal chemistry

authors： Kassiou M,Dannals RF,Liu X,Wong DF,Ravert HT,Scheffel UA

更新日期：2005-06-01 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：:Four kaempferol glycosides were isolated from the leaves of Cinnamomum osmophloeum Kaneh, a Taiwan endemic tree. These compounds namely, kaempferitrin (1), kaempferol 3-O-beta-D-glucopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-7-O-alpha-L-rhamnopyranoside (2), kaempferol 3-O-beta-D-apiofuranosyl-(1-->2)-alpha-L-arabinof...

journal_title：Bioorganic & medicinal chemistry

authors： Fang SH,Rao YK,Tzeng YM

更新日期：2005-04-01 00:00:00

abstract：:A novel class of N-substituted tetrahydropyridine derivatives was found to have multiple kinetic mechanisms of monoamine oxidase A inhibition. Eleven structurally similar tetrahydropyridine derivatives were synthesized and evaluated as inhibitors of MAO-A and MAO-B. The most potent MAO-A inhibitor in the series, 2,4-d...

journal_title：Bioorganic & medicinal chemistry

authors： Wichitnithad W,O'Callaghan JP,Miller DB,Train BC,Callery PS

更新日期：2011-12-15 00:00:00

abstract：:Genomic studies revealed the absence of glutaminyl-tRNA synthetase and/or asparaginyl-tRNA synthetase in many bacteria and all known archaea. In these microorganisms, glutaminyl-tRNA(Gln) (Gln-tRNA(Gln)) and/or asparaginyl-tRNA(Asn) (Asn-tRNA(Asn)) are synthesized via an indirect pathway involving side chain amidation...

journal_title：Bioorganic & medicinal chemistry

authors： Balg C,De Mieri M,Huot JL,Blais SP,Lapointe J,Chênevert R

更新日期：2010-11-15 00:00:00

abstract：:Petrosaspongiolides M-R (PM-PR, 1-5) are marine sesterterpenes structurally characterised by a gamma-hydroxybutenolide moiety. They have shown an in vitro and in vivo potent anti-inflammatory activity, mediated by specific inhibition of secretory phospholipase A(2) (sPLA(2) enzymes). The molecular mechanism underlying...

journal_title：Bioorganic & medicinal chemistry

authors： Monti MC,Casapullo A,Riccio R,Gomez-Paloma L

更新日期：2004-03-15 00:00:00

abstract：:The carcinogenic activity has been investigated by using a topological substructural molecular design approach (TOPS-MODE). A discriminant model was developed to predict the carcinogenic and noncarcinogenic activity on a data set of 189 compounds. The percentage of correct classification was 76.32%. The predictive pow...

journal_title：Bioorganic & medicinal chemistry

authors： Helguera AM,Cabrera Pérez MA,González MP,Ruiz RM,González Díaz H

更新日期：2005-04-01 00:00:00

abstract：:The high-pressure Diels-Alder reaction of N-carbomethyoxypyrroles and phenyl vinyl sulfone affords versatile intermediates for the palladium-catalyzed preparation of new epibatidine analogues. Structure-activity relationships of new epibatidine analogues are presented. High affinities of Ki = 0.81 and 2.6 nM for the [...

journal_title：Bioorganic & medicinal chemistry

authors： Seerden JP,Tulp MT,Scheeren HW,Kruse CG

更新日期：1998-11-01 00:00:00

abstract：:A molecular modeling study using Comparative Molecular Field Analysis (CoMFA) was undertaken to develop a predictive model for combretastatin binding to the colchicine binding site of tubulin. Furthermore, we examined the potential contribution of lipophilicity (log P) and molecular dipole moment and were unable to co...

journal_title：Bioorganic & medicinal chemistry

authors： Brown ML,Rieger JM,Macdonald TL

更新日期：2000-06-01 00:00:00

abstract：:The activated vitamin D3 derivative 26,27-F6-1alpha,25(OH)2D3 (2a), its three A-ring diastereomers (2b, 2c, 2d), and 5,6-trans isomer (2e) were prepared. Two analogues (2b, 2c) of these isomers were synthesized by a palladium catalyzed coupling reaction using vinyl bromide 5 and enynes (6a, 6b), which were derived fro...

journal_title：Bioorganic & medicinal chemistry

authors： Ikeda M,Takahashi K,Dan A,Koyama K,Kubota K,Tanaka T,Hayashi M

更新日期：2000-08-01 00:00:00

abstract：:The photoeffect of new proflavine derivatives with DNA-binding and antitumour activities, 3,6-bis((1-alkyl-5-oxo-imidazolidin-2-yliden)imino)acridine hydrochlorides (AcrDIMs), was studied to evaluate them as potential photosensitizers for photodynamic antitumor therapy. EPR measurements showed that superoxide radical ...

journal_title：Bioorganic & medicinal chemistry

authors： Cižeková L,Grolmusová A,Ipóthová Z,Barbieriková Z,Brezová V,Hunáková L,Imrich J,Janovec L,Dovinová I,Paulíková H

更新日期：2014-09-01 00:00:00

abstract：:Eurycomanone (1) and 13β,21-epoxyeurycomanone (2) were isolated from Eurycoma longifolia for studies of lipolytic activity. Compound 1 enhanced lipolysis in adipocytes with an EC50 of 14.6μM, while its epoxy derivate, compound 2, had a stronger activity with an EC50 of 8.6μM. Based on molecular mechanistic study using...

journal_title：Bioorganic & medicinal chemistry

authors： Lahrita L,Hirosawa R,Kato E,Kawabata J

更新日期：2017-09-01 00:00:00

abstract：:We report the synthesis and the functional studies of multiple crown alpha-helical peptides designed to form artificial ion channels. The approach combines the versatility of solid phase peptide synthesis, the conformational predictability of peptidic molecules, and the solution synthesis of crown ethers with engineer...

journal_title：Bioorganic & medicinal chemistry

authors： Biron E,Otis F,Meillon JC,Robitaille M,Lamothe J,Van Hove P,Cormier ME,Voyer N

更新日期：2004-03-15 00:00:00

abstract：:Erypoegin K, an isoflavone isolated from the stem bark of Erythrina poeppigiana, has potent apoptosis-inducing effect on human leukemia HL-60 cells. Erypoegin K has a chiral carbon at the C-2'' position of its furan ring and naturally occurs as a racemic mixture of (S)- and (R)-isomers. In the present study, we semi-s...

journal_title：Bioorganic & medicinal chemistry

authors： Hikita K,Saigusa S,Takeuchi Y,Matsuyama H,Nagai R,Kato K,Murata T,Tanaka H,Wagh YS,Asao N,Kaneda N

更新日期：2020-06-01 00:00:00

abstract：:2-Styrylchromones (2-SC) are a chemical family of oxygen heterocyclic compounds, vinylogues of flavones (2-phenylchromones), whose occurrence in nature has been reported. Recently, several 2-SC derivatives were demonstrated to have antioxidant properties, namely, xanthine oxidase inhibition, hepatoprotection against p...

journal_title：Bioorganic & medicinal chemistry

authors： Gomes A,Fernandes E,Garcia MB,Silva AM,Pinto DC,Santos CM,Cavaleiro JA,Lima JL

更新日期：2008-09-01 00:00:00

abstract：:Glyoxalase I (GLO I) is the rate-limiting enzyme for detoxification of methylglyoxal (MG), a side product of glycolysis, which is able to induce apoptosis. Since GLO I is known to be highly expressed in the most tumor cells and little in normal cells, specific inhibitors of this enzyme have been expected as effective ...

journal_title：Bioorganic & medicinal chemistry

authors： Takasawa R,Takahashi S,Saeki K,Sunaga S,Yoshimori A,Tanuma S

更新日期：2008-04-01 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：:In continuing our efforts to identify small molecules able to inhibit c-Met kinase, three series of novel 6,7-disubstituted-4-phenoxyquinoline derivatives (23a-w, 26a-d and 30a-d) bearing (thio)semicarbazone scaffold were designed, synthesized and evaluated for their cytotoxicity. The biological data revealed that mos...

journal_title：Bioorganic & medicinal chemistry

authors： Zhai X,Bao G,Wang L,Cheng M,Zhao M,Zhao S,Zhou H,Gong P

更新日期：2016-03-15 00:00:00

abstract：:Bovine plasma amine oxidase (BPAO) was previously shown to be irreversibly inhibited by propargylamine and 2-chloroallylamine. 1,4-Diamine versions of these two compounds are here shown to be highly potent inactivators, with IC50 values near 20 microM. Mono-N-alkylation or N,N-dialkylation greatly lowered the inactiva...

journal_title：Bioorganic & medicinal chemistry

authors： Jeon HB,Lee Y,Qiao C,Huang H,Sayre LM

更新日期：2003-10-15 00:00:00

abstract：:The solution-phase parallel synthesis involving reactions of Baylis-Hillman products of 3-substituted-5-isoxazolecarbaldehydes with nucleophiles and their in vivo antithrombotic evaluations are described along with the results of in vitro platelet aggregation inhibition assay of a few compounds. Results of the detaile...

journal_title：Bioorganic & medicinal chemistry

authors： Batra S,Roy AK,Patra A,Bhaduri AP,Surin WR,Raghavan SA,Sharma P,Kapoor K,Dikshit M

更新日期：2004-05-01 00:00:00

abstract：:Protozoan parasites are unable to synthesize purines de novo and must rely on purine salvage pathways for their requirements. Nucleoside hydrolases, which are not found in mammals, function as key enzymes in purine salvage in protozoa. Inhibition of these enzymes may disrupt purine supply and specific inhibitors are p...

journal_title：Bioorganic & medicinal chemistry

authors： Furneaux RH,Schramm VL,Tyler PC

更新日期：1999-11-01 00:00:00