Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes.

abstract：:An unusual class of diterpenoid natural products, 'cycloterpenals' (with a central cyclohexadienal core), that arise in nature by condensation of retinoids and other isoprenes, have been isolated from a variety of organisms including marine sponges as well as from the human eye. A milk whey protein has also demonstrat...

journal_title：Bioorganic & medicinal chemistry

authors： Bench BJ,Tichy SE,Perez LM,Benson J,Watanabe CM

更新日期：2008-08-15 00:00:00

abstract：:Influenza is a continuing world-wide public health problem that causes significant morbidity and mortality during seasonal epidemics and sporadic pandemics. The purpose of the study was synthesis and investigation of antiviral activity of camphor-based symmetric diimines and diamines. A set of C2-symmetric nitrogen-co...

journal_title：Bioorganic & medicinal chemistry

authors： Sokolova AS,Yarovaya OC,Korchagina DV,Zarubaev VV,Tretiak TS,Anfimov PM,Kiselev OI,Salakhutdinov NF

更新日期：2014-04-01 00:00:00

abstract：:The synthesis and optimization of a class of trisubstituted quinazoline-2,4(1H,3H)-dione cPLA(2)alpha inhibitors are described. Utilizing pharmacophores that were found to be important in our indole series, we discovered inhibitors with reduced lipophilicity and improved aqueous solubility. These compounds are active ...

journal_title：Bioorganic & medicinal chemistry

authors： Kirincich SJ,Xiang J,Green N,Tam S,Yang HY,Shim J,Shen MW,Clark JD,McKew JC

更新日期：2009-07-01 00:00:00

abstract：:Several 11-substituted benzo[i]phenanthridine derivatives were synthesized, and their TOP1-targeting activity and cytotoxicity were assessed. Comparative data indicate that TOP1-targeting was often the primary molecular target associated with their cytotoxicity. Several 11-aminoalkyl derivatives, 11-aminocarboxy deriv...

journal_title：Bioorganic & medicinal chemistry

authors： Feng W,Satyanarayana M,Tsai YC,Liu AA,Liu LF,LaVoie EJ

更新日期：2008-09-15 00:00:00

abstract：:Leukemia stem cells (LSCs) account for the development of drug resistance and increased recurrence rate in acute myeloid leukemia (AML) patients. Targeted drug delivery to leukemia stem cells remains a major challenge in AML chemotherapy. Overexpressed interleukin-3 receptor alpha chain, CD123, on the surface of leuke...

journal_title：Bioorganic & medicinal chemistry

authors： Li B,Zhao W,Zhang X,Wang J,Luo X,Baker SD,Jordan CT,Dong Y

更新日期：2016-11-15 00:00:00

abstract：:New series of 3-phenylquinoxaline 1,4-di-N-oxide with selective activity against Mycobacterium tuberculosis have been prepared and evaluated. Thirty-four of the seventy tested compounds showed an MIC value less than 0.2 microg/mL, a value on the order of the MIC of rifampicin. Furthermore, 45% of the evaluated derivat...

journal_title：Bioorganic & medicinal chemistry

authors： Vicente E,Pérez-Silanes S,Lima LM,Ancizu S,Burguete A,Solano B,Villar R,Aldana I,Monge A

更新日期：2009-01-01 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：: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：:Callophycin A was originally isolated from the red algae Callophycus oppositifolius and shown to mediate anticancer and cytotoxic effects. In our collaborative effort to identify potential chemopreventive and anticancer agents with enhanced potency and selectivity, we employed a tetrahydro-β-carboline-based template i...

journal_title：Bioorganic & medicinal chemistry

authors： Shen L,Park EJ,Kondratyuk TP,Guendisch D,Marler L,Pezzuto JM,Wright AD,Sun D

更新日期：2011-11-01 00:00:00

abstract：:We have prepared three conformationally restricted analogs of DuP753 in which one of the phenyl rings in the biphenyl moiety is fused to the imidazole ring, and have investigated the conformation-biological activity relationship of these compounds. Conformational analysis on DuP753 and these compounds confirms that a ...

journal_title：Bioorganic & medicinal chemistry

authors： Yoo SE,Shin YA,Lee SH,Kim NJ

更新日期：1995-03-01 00:00:00

abstract：:A new series of 2-thioether-benzothiazoles has been synthesized and evaluated for JNK inhibition. The SAR studies led to the discovery of potent, allosteric JNK inhibitors with selectivity against p38. ...

journal_title：Bioorganic & medicinal chemistry

authors： De SK,Chen LH,Stebbins JL,Machleidt T,Riel-Mehan M,Dahl R,Chen V,Yuan H,Barile E,Emdadi A,Murphy R,Pellecchia M

更新日期：2009-04-01 00:00:00

abstract：:The synthesis and in vitro antibacterial activity of 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido] cephalosporins bearing various 2-alkyl-3-aminopyrazolium groups at the 3-position are described. Antibacterial activity against MRSA was affected by the nature of the substituent at the 2-position on the 3...

journal_title：Bioorganic & medicinal chemistry

authors： Ohki H,Kawabata K,Inamoto Y,Okuda S,Kamimura T,Sakane K

更新日期：1997-08-01 00:00:00

abstract：:For the purpose of rational modification of the TRH molecule, we were pursuing an approach that consists of two steps: (1) 'obligatory' replacement of histidine with glutamine in TRH and (2) the application of conformational constraints for putative bioactive conformation I stabilized by an intramolecular hydrogen bon...

journal_title：Bioorganic & medicinal chemistry

authors： Mazurov AA,Andronati SA,Korotenko TI,Sokolenko NI,Dyadenko AI,Shapiro YE,Gorbatyuk VYa,Voronina TA

更新日期：1997-11-01 00:00:00

abstract：:A novel peptidyl chemosensor (PySO2-His-Gly-Gly-Lys(PySO2)-NH2, 1) was synthesized by incorporation of two pyrene (Py) fluorophores into the tetrapeptide using sulfonamide group. Compound 1 exhibited selective fluorescence response towards Hg(II) over the other metal ions in aqueous buffered solutions. Furthermore, 1 ...

journal_title：Bioorganic & medicinal chemistry

authors： Thirupathi P,Lee KH

更新日期：2013-12-15 00:00:00

abstract：:The action of the coumarin-type drugs and related compounds is reviewed to their VKOR antagonistic effects. In our study, twenty 3-pyridinyl, pyrimidinyl and pyrazolyl-4-hydroxycoumarin derivatives were synthesized. A comparative in vivo (CT, PT determination) and in vitro (measurement of PIVKA-II levels) anticoagulan...

journal_title：Bioorganic & medicinal chemistry

authors： Abdelhafez OM,Amin KM,Batran RZ,Maher TJ,Nada SA,Sethumadhavan S

更新日期：2010-05-15 00:00:00

abstract：:The activity-structure relationships (ASR) of phenolic compounds as hydroxyl-radical scavengers have mostly been studied and discussed with regard to their iron-chelating and hydrogen-donation properties in Fenton-type system, but extensive elucidation of multiple mechanisms underlying the hydroxyl radical scavenging ...

journal_title：Bioorganic & medicinal chemistry

authors： Cheng Z,Ren J,Li Y,Chang W,Chen Z

更新日期：2002-12-01 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：:In our ongoing program aimed at deeply investigating the endocannabinoid system (ES), a set of new alkyl-resorcinol derivatives was prepared focusing on the nature and the importance of the carboxamide functionality. Binding studies on CB1 and CB2 receptors, monoacylglycerol lipase (MAGL) and fatty acid amide hydrolas...

journal_title：Bioorganic & medicinal chemistry

authors： Brizzi A,Aiello F,Marini P,Cascio MG,Corelli F,Brizzi V,De Petrocellis L,Ligresti A,Luongo L,Lamponi S,Maione S,Pertwee RG,Di Marzo V

更新日期：2014-09-01 00:00:00

abstract：:The molecular design and chemical synthesis of novel enediyne molecules related to the neocarzinostatin chromophore (1), and their chemical and DNA cleaving properties are described. The 10-membered enediyne triols 16-18 were effectively synthesized from xylitol (10) in a short step, and found to be quite stable when ...

journal_title：Bioorganic & medicinal chemistry

authors： Toshima K,Ohta K,Kano T,Nakamura T,Nakata M,Kinoshita M,Matsumura S

更新日期：1996-01-01 00:00:00

abstract：:Pin1 (Protein interacting with NIMA1) is a cis-trans isomerase and promotes the amide bond rotation of phosphoSer/Thr-Pro motifs in its substrates. Inhibition of Pin1 might be a novel strategy for developing anticancer agents. Herein, a series of pyrimidine derivatives were synthesized and their Pin1 inhibitory activi...

journal_title：Bioorganic & medicinal chemistry

authors： Cui G,Jin J,Chen H,Cao R,Chen X,Xu B

更新日期：2018-05-01 00:00:00

abstract：:Several N-substituted quindolines were made to further evaluate the role of N-alkylation on the activity of indoloquinolines as antifungal agents. While N-5 substitution is required for these activities, N-10 alkylation alone leads to inactive products but is tolerated in the presence of N-5 alkyl groups. It was also ...

journal_title：Bioorganic & medicinal chemistry

authors： Mardenborough LG,Zhu XY,Fan P,Jacob MR,Khan SI,Walker LA,Ablordeppey SY

更新日期：2005-06-02 00:00:00

abstract：:Two series of combretastatin A4 derivatives (acrylamide=carboxamide and carbamate) were synthesized in order to improve the water solubility and stabilize the cis-configuration of the double bond. Their cytotoxic effects were evaluated against MCF-7, KB-3-1 and IGROV human cancer cell lines, as well as their inhibitor...

journal_title：Bioorganic & medicinal chemistry

authors： Borrel C,Thoret S,Cachet X,Guénard D,Tillequin F,Koch M,Michel S

更新日期：2005-06-01 00:00:00

abstract：:A new series of 4-aminochloroquinoline based sulfonamides were synthesized and evaluated for antiamoebic and antimalarial activities. Out of the eleven compounds evaluated (F1-F11), two of them (F3 and F10) showed good activity against Entamoeba histolytica (IC50 <5 μM). Three of the compounds (F5, F7 and F8) also dis...

journal_title：Bioorganic & medicinal chemistry

authors： Salahuddin A,Inam A,van Zyl RL,Heslop DC,Chen CT,Avecilla F,Agarwal SM,Azam A

更新日期：2013-06-01 00:00:00

abstract：:A natural product inspired synthesis of 6,6,5-tricyclic compounds via a silver(I)-catalyzed formal 1,3-dipolar cycloaddition of coumarins with α-iminoesters was developed. The reaction proceeds in a stepwise reaction course under formation of the trans-substituted diastereomer with respect to the 1,3-dipole and shows ...

journal_title：Bioorganic & medicinal chemistry

authors： Potowski M,Golz C,Strohmann C,Antonchick AP,Waldmann H

更新日期：2015-06-15 00:00:00

abstract：:Synthetic derivatives of cyclic adenosine monophosphate, such as halogenated or other more hydrophobic analogs, are widely used compounds, to investigate diverse signal transduction pathways of eukaryotic cells. This inspired us to develop cyclic nucleotides, which exhibit chemical structures composed of brominated 7-...

journal_title：Bioorganic & medicinal chemistry

authors： Lelle M,Otte M,Thon S,Bertinetti D,Herberg FW,Benndorf K

更新日期：2019-04-15 00:00:00

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：:A facile, one-pot enzymatic glycan remodeling of antibody rituximab to produce homogeneous high-mannose and hybrid type antibody glycoforms is described. This method was based on the unique substrate specificity of the endoglycosidase S (Endo-S) from Streptococcus pyogenes. While Endo-S efficiently hydrolyzes the bi-a...

journal_title：Bioorganic & medicinal chemistry

authors： Tong X,Li T,Orwenyo J,Toonstra C,Wang LX

更新日期：2018-04-01 00:00:00

abstract：:A group of novel tricyclic Delta(2)-isoxazolines (4b, 5b, 7a-b, and 8a-b) and 3-oxo-isoxazolidines (6a-b and 9a-b), structurally related to cytisine or norferruginine, was prepared through 1,3-dipolar cycloadditions involving suitable olefins and bromonitrile oxide. The target compounds were assayed at alpha4beta2 and...

journal_title：Bioorganic & medicinal chemistry

authors： Dallanoce C,Frigerio F,Martelli G,Grazioso G,Matera C,Pomè DY,Pucci L,Clementi F,Gotti C,De Amici M

更新日期：2010-06-15 00:00:00

abstract：:4-Aminoantipyrine (4-amino-1,5-dimethyl-2-phenylpyrazole-3-one) and its analogues have been found to be compounds of interest for their anti-inflammatory, analgesic, antiviral, antipyretic, antirheumatic and antimicrobial activities. In the present study, Schiff base analogues of 4-aminoantipyrine were synthesized by ...

journal_title：Bioorganic & medicinal chemistry

authors： Alam MS,Choi JH,Lee DU

更新日期：2012-07-01 00:00:00

abstract：:To develop agents for radionuclide imaging Aβ plaques in vivo, we prepared three fluorine-substituted analogs of arylbenzothiazole class; compound 2 has a high affinity for Aβ (K(i)=5.5nM) and the specific binding to Aβ in fluorescent staining. In preparation for the synthesis of these arylbenzothiazole analogs in rad...

journal_title：Bioorganic & medicinal chemistry

authors： Lee BC,Kim JS,Kim BS,Son JY,Hong SK,Park HS,Moon BS,Jung JH,Jeong JM,Kim SE

更新日期：2011-05-01 00:00:00