A new strategy for the synthesis of crucigasterin A, and cytotoxic activity of this compound and its related analogues.

abstract：:We have focused on the C5-modification of 2'-deoxyuridine with substituted heterocycles for bioactivity, such as antiviral or anticancer activity. Herein, we report a novel class of nucleoside analogues with perfluoroalkyltriazole moiety as an anticancer drug candidate. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park SM,Yang H,Park SK,Kim HM,Kim BH

更新日期：2010-10-01 00:00:00

abstract：:The synthesis and structure-activity relationships (SAR) of novel, potent imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors are described. The X-ray crystal structure of imidazo[1,2-a]pyrazine Aurora inhibitor 1j is disclosed. Compound 10i was identified as lead compound with a promising overall profile. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Belanger DB,Curran PJ,Hruza A,Voigt J,Meng Z,Mandal AK,Siddiqui MA,Basso AD,Gray K

更新日期：2010-09-01 00:00:00

abstract：:A new series of benzene and isoquinoline sulfonamide derivatives were synthesized by nucleophilic displacement reaction on benzene and isoquinoline sulfonyl chlorides by substituted amines (primary and secondary). The title compounds were evaluated for antimalarial activity against Plasmodium falciparum in vitro and s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kumar Parai M,Panda G,Srivastava K,Kumar Puri S

更新日期：2008-01-15 00:00:00

abstract：:To overcome the chemical and metabolic instability of the secondary fatty acyl residues in the AGP class of lipid A mimetics, the secondary ether lipid analogs of the potent TLR4 agonist CRX-527 (2) and TLR4 antagonist CRX-526 (3) were synthesized and evaluated along with their ester counterparts for agonist/antagonis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bazin HG,Murray TJ,Bowen WS,Mozaffarian A,Fling SP,Bess LS,Livesay MT,Arnold JS,Johnson CL,Ryter KT,Cluff CW,Evans JT,Johnson DA

更新日期：2008-10-15 00:00:00

abstract：:1,2,4-Oxadiazoles have been prepared in parallel using 1,1'-carbonyldiimidazole (CDI) as a reagent for both formation and cyclodehydration of O-acyl benzamidoximes. The use of CDI facilitates parallel purification of the oxadiazole products by simple liquid-liquid extraction and filtration. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Deegan TL,Nitz TJ,Cebzanov D,Pufko DE,Porco JA Jr

更新日期：1999-01-18 00:00:00

abstract：:Ligand-protein binding is a complex process that involves the formation of number of non-covalent interactions, e.g. H-bonds and hydrophobic interactions, between the ligand and the protein host. Upon binding, ligand functional groups can act synergistically (positive cooperativity) to improve the overall ligand bindi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Said AM,Hangauer DG

更新日期：2016-08-15 00:00:00

abstract：:A series of tacrine-pyrazolo[3,4-b]pyridine hybrids were synthesised and evaluated as dual cholinesterase (ChE) and phosphodiesterase 4D (PDE4D) inhibitors for the treatment of Alzheimer's disease (AD). Compound 10j, which is tacrine linked with pyrazolo[3,4-b]pyridine moiety by a six-carbon spacer, was the most poten...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pan T,Xie S,Zhou Y,Hu J,Luo H,Li X,Huang L

更新日期：2019-08-15 00:00:00

abstract：:We have designed and synthesized twenty-six N-arylindazole-3-carboxamide (3a-p) and N-benzoylindazole (6a-j) derivatives to discover with excellent inhibition activities of α-MSH-stimulated melanogenesis. In the bio evaluation studies of these compounds, we discovered eighteen compounds, out of twenty-six exhibited mo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Arepalli SK,Lee C,Jung JK,Kim Y,Lee K,Lee H

更新日期：2019-09-15 00:00:00

abstract：:We report a dimerization strategy to enhance the antibacterial potency of an otherwise weak cationic amphiphilic polyproline helical (CAPH) peptide. Overall, the dimeric CAPHs were more active against Escherichia coli and Staphylococcus aureus than the monomeric counterpart, reaching up to a 60-fold increase in potenc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hernandez-Gordillo V,Geisler I,Chmielewski J

更新日期：2014-01-15 00:00:00

abstract：:Carbonic anhydrase inhibitors AZA, EZA, and 4-acetamidobenzsulfonamide were found to inhibit human AQP4-M23 mediated water transport by 80%, 68%, and 23%, respectively, at 20 microM in an in vitro functional assay. AZA was found to have an IC50 against AQP4 of 0.9 microM. Phloretin was inactive under the same conditio...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huber VJ,Tsujita M,Yamazaki M,Sakimura K,Nakada T

更新日期：2007-03-01 00:00:00

abstract：:We designed and synthesized of 1,3,5-trioxazatriquinanes with o- or p-hydroxyphenyl rings as analogs of the κ opioid receptor agonist SYK-146 with m-hydroxyphenyl groups. Although almost all tested compounds did not bind to the opioid receptors, only 17b (SYK-524) with two o-hydroxyphenyl rings showed moderate or pote...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hirayama S,Wada N,Kuroda N,Iwai T,Yamaotsu N,Hirono S,Fujii H,Nagase H

更新日期：2014-10-15 00:00:00

abstract：:Inactivation of the NF-κB signaling pathway by inhibition of IKKβ is a well-known approach to treat inflammatory diseases such as rheumatoid arthritis and cancer. Thienopyrimidine-based analogues were designed through modification of the known IKKβ inhibitor, SPC-839, and then biologically evaluated. The resulting ana...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park CH,Lee C,Yang JS,Joe BY,Chun K,Kim H,Kim HY,Kang JS,Lee JI,Kim MH,Han G

更新日期：2014-06-15 00:00:00

abstract：:It is well known that resveratrol (RSV) displayed cancer-preventing and anticancer properties but its clinical application is limited because of a low bioavailability and a rapid clearance from the circulation. Aim of this work was to synthesize pharmacologically active resveratrol analogs with an enhanced structural ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sala M,Chimento A,Saturnino C,Gomez-Monterrey IM,Musella S,Bertamino A,Milite C,Sinicropi MS,Caruso A,Sirianni R,Tortorella P,Novellino E,Campiglia P,Pezzi V

更新日期：2013-09-01 00:00:00

abstract：:A 26-member library of novel N-hydroxyquinolinone derivatives was synthesized by a one-pot Buchwald-type palladium catalyzed amidation and condensation sequence. The design of these rare scaffolds was inspired from N-hydroxypyridones and 2-quinolinones classes of compounds which have been shown to have rich biological...

journal_title：Bioorganic & medicinal chemistry letters

authors： Teng Y,Suwanarusk R,Ngai MH,Srinivasan R,Ong AS,Ho B,Rénia L,Chai CL

更新日期：2015-02-01 00:00:00

abstract：:A series of 4-aryl-3-aminoquinoline-2-one derivatives was synthesized and evaluated as activators of the cloned maxi-K channel mSlo (hSlo) expressed in Xenopus laevis oocytes using electrophysiological methods. A brain penetrable activator of maxi-K channels was identified and shown to be significantly active in the M...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hewawasam P,Fan W,Knipe J,Moon SL,Boissard CG,Gribkoff VK,Starrett JE

更新日期：2002-07-08 00:00:00

abstract：:Over 195 4-alkyl and 4,4-dialkyl 1,2-bis(4-chlorophenyl)pyrazolidine-3,5-dione derivatives were synthesized, utilizing microwave accelerated synthesis, for evaluation as new inhibitors of bacterial cell wall biosynthesis. Many of them demonstrated good activity against MurB in vitro and low MIC values against gram-pos...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kutterer KM,Davis JM,Singh G,Yang Y,Hu W,Severin A,Rasmussen BA,Krishnamurthy G,Failli A,Katz AH

更新日期：2005-05-16 00:00:00

abstract：:Novel, low brain penetrant, orally bioavailable CB1 receptor agonists were designed starting from a mature lead series of potent brain penetrant CB1 receptor agonists. Increasing the calculated polar surface area was found to be a good strategy for reducing brain penetration whilst retaining drug-like properties. This...

journal_title：Bioorganic & medicinal chemistry letters

authors： Adam JM,Clark JK,Davies K,Everett K,Fields R,Francis S,Jeremiah F,Kiyoi T,Maidment M,Morrison A,Ratcliffe P,Prosser A,Schulz J,Wishart G,Baker J,Boyce S,Campbell R,Cottney JE,Deehan M,Martin I

更新日期：2012-04-15 00:00:00

abstract：:Modification of the biphenyl portion of MMP inhibitor 2a gave analogue 2i which is greater than 1000-fold selective against MMP-2 versus MMP-1. The stereospecific synthesis of both enantiomers of 2i was achieved beginning with (S)- or (R)-benzyl glycidyl ether. The (S)-enantiomer, 11 (ABT-770), is orally bioavailable ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Curtin ML,Florjancic AS,Heyman HR,Michaelides MR,Garland RB,Holms JH,Steinman DH,Dellaria JF,Gong J,Wada CK,Guo Y,Elmore IB,Tapang P,Albert DH,Magoc TJ,Marcotte PA,Bouska JJ,Goodfellow CL,Bauch JL,Marsh KC,Morgan

更新日期：2001-06-18 00:00:00

abstract：:We report the discovery of a novel, chiral azetidine urea inhibitor of Fatty Acid Amide Hydrolase (FAAH,) and describe the surprising species selectivity of VER-156084 versus rat and human FAAH and also hCB1. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hart T,Macias AT,Benwell K,Brooks T,D'Alessandro J,Dokurno P,Francis G,Gibbons B,Haymes T,Kennett G,Lightowler S,Mansell H,Matassova N,Misra A,Padfield A,Parsons R,Pratt R,Robertson A,Walls S,Wong M,Roughley S

更新日期：2009-08-01 00:00:00

abstract：:A new series of triazole-imidazo[2,1-b][1,3,4]thiadiazole hybrids (6a-s, 7a) were designed by a molecular hybridisation approach and the target molecules were synthesized via one pot click chemistry protocol. All the intermediates and final molecules were characterised using spectral methods and one of the target comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ramprasad J,Nayak N,Dalimba U,Yogeeswari P,Sriram D

更新日期：2015-10-01 00:00:00

abstract：:A novel series of diphenyl lactam containing calcium channel blockers is described. Extensive SAR studies resulted in compounds with low molar activity and good plasma exposure after oral dosing. Compounds 2, 6 and 7 demonstrated significant efficacy in the capsaicin model of secondary hyperalgesia following oral admi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Doherty GA,Bhatia P,Vortherms TA,Marsh KC,Wetter JM,Mack H,Scott VE,Jarvis MF,Stewart AO

更新日期：2012-02-15 00:00:00

abstract：:Novel 1,7- and 2,7-naphthyridine derivatives, designed by the introduction of nitrogen atom into the phenyl ring of previously reported 4-aryl-1-isoquinolinone derivatives, were disclosed as a new structural class of potent and specific PDE5 inhibitors. Among them, 2,7-naphthyridine 4c showed potent PDE5 inhibition (I...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ukita T,Nakamura Y,Kubo A,Yamamoto Y,Moritani Y,Saruta K,Higashijima T,Kotera J,Fujishige K,Takagi M,Kikkawa K,Omori K

更新日期：2003-07-21 00:00:00

abstract：:A number of novel 1-(3-arylprop-2-ynyl) substituted 1,2-dihydroquinoline derivatives related to nimesulide and their 2-oxo analogues have been designed as potential inhibitors of PDE4. All these compounds were synthesized by using Sonogashira coupling as a key step. In vitro PDE4B inhibitory properties and molecular m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pal S,Durgadas S,Nallapati SB,Mukkanti K,Kapavarapu R,Meda CL,Parsa KV,Pal M

更新日期：2011-11-01 00:00:00

abstract：:Several non-amidino S1 derivatives of the 1,2-diaminobenzene-based scaffold (4) were synthesized and evaluated for their ability to bind to the active site and inhibit the human protease factor Xa. A subset of these compounds were also evaluated for their anticoagulant effects in human plasma as measured by prothrombi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Franciskovich JB,Masters JJ,Tinsley JM,Craft TJ,Froelich LL,Gifford-Moore DS,Klimkowski VJ,Smallwood JK,Smith GF,Smith T,Towner RR,Weir LC,Wiley MR

更新日期：2005-11-01 00:00:00

abstract：:The synthesis and biological evaluation of novel human A-FABP inhibitors based on the 6-(trifluoromethyl)pyrimidine-4(1H)-one scaffold is described. Two series of compounds, bearing either an amino or carbon substituent in the 2-position of the pyrimidine ring were investigated. Modification of substituents and chain ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ringom R,Axen E,Uppenberg J,Lundbäck T,Rondahl L,Barf T

更新日期：2004-09-06 00:00:00

abstract：:High throughput screening for β-lactamase inhibitors afforded biphenyl hits such as 1. Hit confirmation and X-ray soaking experiments with Pseudomonas Aeruginosa AmpC enzyme led to the identification of an aryl boronic acid-serine complex 4, which was formed from phenyl boronic acid 8 (an impurity in compound 1) and e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang SW,Pan J,Root Y,Scapin G,Xiao L,Su J

更新日期：2020-01-15 00:00:00

abstract：:Triphosphate of a new fluorescent labeled thymidine analogue was incorporated as a substrate for PCR using KOD Dash DNA polymerase forming the corresponding fluorescent labeled DNA which is useful for a DNA probe. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Obayashi T,Masud MM,Ozaki AN,Ozaki H,Kuwahara M,Sawai H

更新日期：2002-04-22 00:00:00

abstract：:The discovery, synthesis, and SAR of chromanes as ER alpha subtype selective ligands are described. X-ray studies revealed that the origin of the ER alpha-selectivity resulted from a C-4 trans methyl substitution to the cis-2,3-diphenyl-chromane platform. Selected compounds from this class demonstrated very potent in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tan Q,Blizzard TA,Morgan JD 2nd,Birzin ET,Chan W,Yang YT,Pai LY,Hayes EC,DaSilva CA,Warrier S,Yudkovitz J,Wilkinson HA,Sharma N,Fitzgerald PM,Li S,Colwell L,Fisher JE,Adamski S,Reszka AA,Kimmel D,DiNinno F,Rohre

更新日期：2005-03-15 00:00:00

abstract：:Structure-based design, synthesis, and biological evaluation of a series of peptidomimetic beta-secretase inhibitors incorporating hydroxyethylamine isosteres are described. We have identified inhibitor 24 which has shown exceedingly potent activity in memapsin 2 enzyme inhibitory (K(i) 1.8 nM) and cellular (IC(50)=1 ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ghosh AK,Kumaragurubaran N,Hong L,Kulkarni S,Xu X,Miller HB,Reddy DS,Weerasena V,Turner R,Chang W,Koelsch G,Tang J

更新日期：2008-02-01 00:00:00

abstract：:We report herein a one-pot four-enzyme approach for the synthesis of the rare sugars d-psicose, d-sorbose, l-tagatose, and l-fructose with aldolase FucA from a thermophilic source (Thermus thermophilus HB8). Importantly, the cheap starting material DL-GP (DL-glycerol 3-phosphate), was used to significantly reduce the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li Z,Cai L,Qi Q,Styslinger TJ,Zhao G,Wang PG

更新日期：2011-09-01 00:00:00