Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides.

abstract：:A series of 2-phenoxy-indan-1-one derivatives have been designed, synthesized, and tested as acetylcholinesterase inhibitors. The most potent compound exhibited high AChE inhibitory activity (IC50 = 50 nM), and the molecular docking study indicated that it was nicely accommodated by AChE. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sheng R,Lin X,Li J,Jiang Y,Shang Z,Hu Y

更新日期：2005-09-01 00:00:00

abstract：:Benz[b]oxepines 4a-g and 12-oxobenzo[c]phenanthridines 5a-d were designed and synthesized as constrained forms of 3-arylisoquinolines through an intramolecular radical cyclization reaction. Radical cyclization of O-vinyl compounds preferentially led to the 7-endo-trig cyclization pathway to the benz[b]oxepines and 12-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee SH,Van HT,Yang SH,Lee KT,Kwon Y,Cho WJ

更新日期：2009-05-01 00:00:00

abstract：:Mandelate racemase has been studied as a paradigm for enzyme-catalyzed abstraction of a proton from carbon acids with relatively high pKa values. 1,1-Diphenyl-1-hydroxymethylphosphonate is a substrate-intermediate-product analogue and is a modest competitive inhibitor of the enzyme (Ki=1.41+/-0.09 mM), suggesting that...

journal_title：Bioorganic & medicinal chemistry letters

authors： Burley RK,Bearne SL

更新日期：2005-10-01 00:00:00

abstract：:Two series of nitrogenous heterocycle compounds--1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles have been synthesized and evaluated for their ALK5 inhibitory activity and cytotoxicity in TGFbeta-Smad2 assay and MTT assay, respectively. The ALK4/5/7 inhibitory activity of some compound was also eval...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li X,Wang L,Long L,Xiao J,Hu Y,Li S

更新日期：2009-08-15 00:00:00

abstract：:A structure-activity relationship of the 3- and 6-positions of the pyrazolo[1,5-a]pyrimidine scaffold of the known BMP inhibitors dorsomorphin, 1, LDN-193189, 2, and DMH1, 3, led to the identification of a potent and selective compound for ALK2 versus ALK3. The potency contributions of several 3-position substituents ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Engers DW,Frist AY,Lindsley CW,Hong CC,Hopkins CR

更新日期：2013-06-01 00:00:00

abstract：:EGF receptor-binding peptides could be found by a peptide screening method using fifteen fluorescent amino acids as fluorescent tags. Of 225 peptides, we found an 8-mer peptide containing a dipeptide unit, Y-F, which was the strongest binding peptide to the EGF receptor. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kitamatsu M,Yamamoto T,Futami M,Sisido M

更新日期：2010-10-15 00:00:00

abstract：:Several efficient synthetic routes for 2-, 4-, and 6-aryl-1,2,4-triazine-3,5-diones were developed. Derivatives were synthesized and studied as gonadotropin-releasing hormone antagonists in an effort to understand structure-activity relationships of the monocyclic compounds. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pontillo J,Guo Z,Wu D,Struthers RS,Chen C

更新日期：2005-10-01 00:00:00

abstract：:A dumbbell-shaped circular oligonucleotide containing topoisomerase I-binding sites and two mismatched base pairs in its sequence has been designed and synthesized. Our further studies demonstrate that this particularly designed oligonucleotide displays an IC(50) value of 9 nM in its inhibition on the activity of huma...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li X,Tao Ng MT,Wang Y,Liu X,Li T

更新日期：2007-09-01 00:00:00

abstract：:A series of 7-acyloxymethylcamptothecin and 20-O-acyl-7-acyloxymethylcamptothecin derivatives were regioselectively prepared on different solvents. 7-Acyloxymethylcamptothecins possess more efficacy than 20-O-acyl-7-acyloxymethylcamptothecins against six human cancer cell lines in vitro. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pan XD,Han R,Sun PY

更新日期：2003-11-03 00:00:00

abstract：:Enedione derivatives of thieno[2,3-d]oxazinones are nanomolar inhibitors of CMV protease which act through a novel dual acylation of the catalytic serine and alkylation of the protease cysteine 161 via a Michael addition to the enedione moiety of the inhibitor. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pinto IL,Jarvest RL,Clarke B,Dabrowski CE,Fenwick A,Gorczyca MM,Jennings LJ,Lavery P,Sternberg EJ,Tew DG,West A

更新日期：1999-02-08 00:00:00

abstract：:The efficient synthesis of 7-substituted pyrido[2',3':4,5]furo[3,2-d]pyrimidin-4-amines and their N-aryl analogues is described. 3,5-Dibromopyridine was converted into 3-amino-6-bromofuro[3,2-b]pyridine-2-carbonitrile intermediate which was formylated with DMFDMA. Functionalization at position 7 of the tricyclic scaff...

journal_title：Bioorganic & medicinal chemistry letters

authors： Deau E,Loidreau Y,Marchand P,Nourrisson MR,Loaëc N,Meijer L,Levacher V,Besson T

更新日期：2013-12-15 00:00:00

abstract：:Bioactivity-guided fractionation of the CHCl3 extract from hooks of Uncaria rhynchophylla led to the isolation of two triterpene esters, namely uncarinic acids A (1) and B (2). Their structures were established by spectroscopic and chemical methods. These compounds inhibited phospholipase Cgamma1 with IC50 values of 3...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee JS,Yang MY,Yeo H,Kim J,Lee HS,Ahn JS

更新日期：1999-05-17 00:00:00

abstract：:A novel series of benzo-[1,2,4]-triazolo-[1,4]-oxazepine GPR142 agonists are described. The series was designed to address the suboptimal PK (pharmacokinetic) and off-target profile of a class of N-aryl-benzo-[1,4]-oxazepine-4-carboxamides, represented by 1, that were identified from a high-throughput screen of the Me...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wilson JE,Kurukulasuriya R,Sinz C,Lombardo M,Bender K,Parker D,Sherer EC,Costa M,Dingley K,Li X,Mitelman S,Tong S,Bugianesi R,Ehrhardt A,Priest B,Ratliff K,Ujjainwalla F,Nargund R,Hagmann WK,Edmondson S

更新日期：2016-06-15 00:00:00

abstract：:The 5,5-bicycles cis-6-oxo-hexahydro-2-oxa-1,4-diazapentalene 3 and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole 4 were designed as rotationally restricted templates towards the preparation of inhibitors of CAC1 cysteinyl proteinases. The design strategy was exemplified through the solution and solid phase preparation of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang Y,Benn A,Flinn N,Monk T,Ramjee M,Watts J,Quibell M

更新日期：2005-03-01 00:00:00

abstract：:Screening of the Merck sample collection for non-peptide compounds with binding affinity for the rat GnRH receptor led to the identification of the substituted quinolone (1) as a lead compound in the search for a non-peptide GnRH receptor antagonist. Substantial improvements in potency (approximately 300 fold) were ac...

journal_title：Bioorganic & medicinal chemistry letters

authors： DeVita RJ,Hollings DD,Goulet MT,Wyvratt MJ,Fisher MH,Lo JL,Yang YT,Cheng K,Smith RG

更新日期：1999-09-06 00:00:00

abstract：:In this study, a series of bis(4-hydroxy)benzophenone oxime ether derivatives such as 12c, 12e and 12h were identified as novel estrogen receptor (ER) agonists that have additional and complementary anti-proliferative activities via ER-independent mechanism in cancer cells. These compounds are expected to overcome the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim T,Kim HI,An JY,Lee J,Lee NR,Heo J,Kim JE,Yu J,Lee YS,Inn KS,Kim NJ

更新日期：2016-04-01 00:00:00

abstract：:The synthesis of three series of quinol fatty alcohols (QFAs) and their biological activities on the promotion of axonal growth are described. Interestingly, the 15-(2,5-dimethoxyphenyl)pentadecan-1-ol, the QFA bearing 15 carbon atoms on the side chain (n=15), shows the most potent promotion of axonal growth in the pr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hanbali M,Vela-Ruiz M,Bagnard D,Luu B

更新日期：2006-05-15 00:00:00

abstract：:Knoevenagel condensation was employed to generate a set of molecules potentially capable of inhibiting the RNA polymerase-σ70/σA interaction in bacteria. Synthesis was achieved via reactions between a variety of indole-7-carbaldehydes and rhodanine, N-allylrhodanine, barbituric acid or thiobarbituric acid. A library o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wenholz DS,Zeng M,Ma C,Mielczarek M,Yang X,Bhadbhade M,Black DSC,Lewis PJ,Griffith R,Kumar N

更新日期：2017-09-15 00:00:00

abstract：:A dynamic target-based pharmacophoric model mapping the CD4 binding site on HIV-1 gp120 was built and used to identify new hits able to inhibit gp120-CD4 protein-protein interactions. Two compounds showed micromolar inhibition of HIV-1 replication in cells attributable to an interference with the entry step of infecti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Caporuscio F,Tafi A,González E,Manetti F,Esté JA,Botta M

更新日期：2009-11-01 00:00:00

abstract：:Cu(II) complexes with 4,6-di(tert-butyl)-2-aminophenol (I) and 2-anilino-4,6-di(tert-butyl)phenol (II) have been synthesized and characterized by means of elemental analysis, TG/DTA, FT-IR, UV-vis, ESR, and conductance measurements. The compounds I and II can coordinate in their singly deprotonated forms and behave as...

journal_title：Bioorganic & medicinal chemistry letters

authors： Loginova NV,Koval'chuk TV,Zheldakova RA,Osipovich NP,Sorokin VL,Polozov GI,Ksendzova GA,Glushonok GK,Chernyavskaya AA,Shadyro OI

更新日期：2006-10-15 00:00:00

abstract：:Owning to the promising neuroprotective profile and the ability to cross the blood-brain barrier, triptolide has attracted extensive attention. Although its limited solubility and toxicity have greatly hindered clinical translation, triptolide has nonetheless emerged as a promising candidate for structure-activity rel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ning C,Mo L,Chen X,Tu W,Wu J,Hou S,Xu J

更新日期：2018-02-15 00:00:00

abstract：:The isopolar nonisosteric phosphonate analogs of ApA differing in the position of extra methylene group introduced into the sugar-phosphate backbone, featuring both possible 2',5'- and 3',5'- pairs as well as their conformationally restricted congeners, were investigated for their ability to form complexes with polyU....

journal_title：Bioorganic & medicinal chemistry letters

authors： Pressová M,Endová M,Toĉík Z,Liboska R,Rosenberg I

更新日期：1998-05-19 00:00:00

abstract：:The present studies have identified a series of diaminopyrimidines and diaminopyridines as novel 5-HT(7) receptor ligands. Three regiosiomeric classes of pyrimidines and four regioisomeric classes of pyridines were synthesized and analyzed for binding to the 5-HT(7) receptor. The 5-HT(7) binding affinities of differen...

journal_title：Bioorganic & medicinal chemistry letters

authors： Denhart DJ,Purandare AV,Catt JD,King HD,Gao A,Deskus JA,Poss MA,Stark AD,Torrente JR,Johnson G,Mattson RJ

更新日期：2004-08-16 00:00:00

abstract：:In an effort to rapidly access vancomycin analogues bearing diverse functionality at the 6c-Cl (the 'in-chloride') position, a two-step dechlorination/cross-coupling protocol was developed. Conditions for efficient cross-coupling of the relatively unreactive 6c-Cl group were found that ensure high conversion with mini...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wadzinski TJ,Gea KD,Miller SJ

更新日期：2016-02-01 00:00:00

abstract：:Herein, we reported the synthesis of 16 novel steroidal thiosemicarbazone derivatives via the condensation of steroidal ketones and substituted thiosemicarbazides under solvent-free conditions using microwave irradiation. The yields obtained are in the range of 84-96% using microwave method and 46-62% using convention...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhao Z,Shi Z,Liu M,Liu X

更新日期：2012-12-15 00:00:00

abstract：:Macrocarpins A (1), B (2), C (3) and D (4), four new nor-triterpenes, have been isolated from the roots of Maytenus macrocarpa. The structures were established by spectroscopic examinations. Natural compounds 1, 2, 4 and the acetyl derivative 1a are cytotoxic against four tumoral cell lines with IC50 values ranging be...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chávez H,Rodríguez G,Estévez-Braun A,Ravelo AG,Estévez-Reyes R,González AG,Fdez-Puente JL,García-Grávalos D

更新日期：2000-04-17 00:00:00

abstract：:A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands is reported. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu KG,Lo JR,Comery TA,Zhang GM,Zhang JY,Kowal DM,Smith DL,Di L,Kerns EH,Schechter LE,Robichaud AJ

更新日期：2008-07-15 00:00:00

abstract：:A novel cys-annexin A5 with a single cysteine-residue at its concave side has been developed by site-directed mutagenesis to allow conjugation through thiol-chemistry without affecting its apoptotic cell binding properties and was derivatized with HYNIC in a 1:1 stoichiometry. Similar to that of the 1st generation 99m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fonge H,de Saint Hubert M,Vunckx K,Rattat D,Nuyts J,Bormans G,Ni Y,Reutelingsperger C,Verbruggen A

更新日期：2008-07-01 00:00:00

abstract：:A novel series of aminopyrimidinylisoindoline derivatives 1a-w having an aminopyrimidine scaffold as a hinge region binding motif were designed and synthesized. Among them, six compounds showed potent inhibitory activities against AXL kinase with IC50 values of submicromolar range. Especially, compound 1u possessing (...

journal_title：Bioorganic & medicinal chemistry letters

authors： Choi MJ,Roh EJ,Hur W,Lee SH,Sim T,Oh CH,Lee SH,Kim JS,Yoo KH

更新日期：2018-12-15 00:00:00

abstract：:The human epidermal growth factor receptor (EGFR) family is known to be involved in cell signaling pathways. The extracellular domain of EGFR consists of four domains, of which domain II and domain IV are known to be involved in the dimerization process. Overexpression of these receptors is known to play a significant...

journal_title：Bioorganic & medicinal chemistry letters

authors： Naik H,Gauthier T,Singh S,Jois S

更新日期：2018-12-01 00:00:00