Inhibition of Src kinase activity by 4-anilino-7-thienyl-3-quinolinecarbonitriles.

abstract：:Four new peptidyl aldehydes bearing proline mimetics at the P(2)-position were synthesized and studied as inhibitors of calpain I, cathepsin B, and selected serine proteases. The ring size of the P(2)-constraining residue influenced the inhibitory potency and selectivity of the compounds for calpain I compared to the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Donkor IO,Korukonda R,Huang TL,LeCour L Jr

更新日期：2003-03-10 00:00:00

abstract：:The synthesis and structure-activity relationships of zygosporamide, a known potent and selective cytotoxic natural product against SF-268 and RXF 393 cell lines, are described. The potencies of the synthetic zygosporamide are similar to those reported for the natural product toward all cancer cell lines examined with...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang Y,Zhang F,Zhang Y,Liu JO,Ma D

更新日期：2008-08-01 00:00:00

abstract：:A series of N-(1-methyl-1H-indol-3-yl)methyleneamines and eight new 3,3-diaryl-4-(1-methyl-1H-indol-3-yl)azetidin-2-ones have been synthesized and screened for their antileishmanial activity against Leishmania major. 3,3-Diaryl-4-(1-methyl-1H-indol-3-yl)azetidin-2-ones have been synthesized by the Staudinger's ketene-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh GS,Al-Kahraman YM,Mpadi D,Yasinzai M

更新日期：2012-09-01 00:00:00

abstract：:QSAR models represent the relationship of biological activity with either physicochemical parameters or structural indices. QSAR study was performed on some arylpiperazines as 5-HT(1A)/alpha(1)-adrenergic receptor antagonists using E-state indices to identify the pharmacophoric requirements. It was found that some of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Debnath B,Samanta S,Naskar SK,Roy K,Jha T

更新日期：2003-09-01 00:00:00

abstract：:The synthesis of racemic tetrahydrocurcumin- (THC-), tetrahydrodemethoxycurcumin- (THDC-) and tetrahydrobisdemethoxycurcumin- (THBDC-) dihydropyrimidinone (DHPM) analogues was achieved by utilizing the multi-component Biginelli reaction in the presence of copper sulphate as a catalyst. The evaluation of acetylcholines...

journal_title：Bioorganic & medicinal chemistry letters

authors： Arunkhamkaew S,Athipornchai A,Apiratikul N,Suksamrarn A,Ajavakom V

更新日期：2013-05-15 00:00:00

abstract：:Synthesis and biological evaluation of novel and potent cyclohexylamine-based histamine H3 receptor inverse agonists are described. Compounds in this newly identified series exhibited subnanomolar binding affinities for human receptor and no significant interaction with hERG channel. One derivative (10t) demonstrated ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Labeeuw O,Levoin N,Poupardin-Olivier O,Calmels T,Ligneau X,Berrebi-Bertrand I,Robert P,Lecomte JM,Schwartz JC,Capet M

更新日期：2011-09-15 00:00:00

abstract：:Six 3'R,4'R-di-O-(S)-camphanoyl-2',2'-dimethyldihydropyrano[2,3-f]chromone (DCP) and two 3'R,4'R-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) derivatives were designed, synthesized, and evaluated for inhibition of HIV-1(NL4-3) replication in TZM-bl cells. 2-Ethyl-2'-monomethyl-1'-oxa- and -1'-thia-DCP (5a, 6a), as we...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu HS,Xu SQ,Cheng M,Chen Y,Xia P,Qian K,Xia Y,Yang ZY,Chen CH,Morris-Natschke SL,Lee KH

更新日期：2011-10-01 00:00:00

abstract：:A novel series of 4-arylphthalazin-1(2H)-one linked to arylpiperidines were synthesized and evaluated as MCH-R1 antagonists. The results of an extensive SAR study probing the effects of substituents on the 4-arylphthalazin-1(2H)-one C-4 aryl group led to the identification of the 4-(3,4-difluorophenyl) derivative as a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lim CJ,Kim SH,Lee BH,Oh KS,Yi KY

更新日期：2012-01-01 00:00:00

abstract：:Two novel series of small-molecule RGD mimetics containing either a substituted pyridone or pyrazinone central constraint were prepared. Modification of the beta-alanine 3-substituent produced compounds that are potent and selective alpha(v)beta(3) antagonists and exhibit a range of physicochemical properties. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Breslin MJ,Duggan ME,Halczenko W,Fernandez-Metzler C,Hunt CA,Leu CT,Merkle KM,Naylor-Olsen AM,Prueksaritanont T,Stump G,Wallace A,Rodan SB,Hutchinson JH

更新日期：2003-05-19 00:00:00

abstract：:Novel 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives have been prepared and their synthesis described herein. In vitro affinities for delta-, micro-, and kappa-opioid receptors are reported. Evaluation of some representative compounds from this series in the mouse neonatal ultrasonic vocalization test and the mo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Trabanco AA,Aerts N,Alvarez RM,Andrés JI,Boeckx I,Fernández J,Gómez A,Janssens FE,Leenaerts JE,De Lucas AI,Matesanz E,Steckler T,Pullan S

更新日期：2007-07-15 00:00:00

abstract：:The title compound was prepared by enzymatic transfer of oligosaccharide to a synthetic pentapeptide containing the Glc-Asn linkage. The compound was not hydrolyzed by glycoamidases from plant and bacterial sources, but it inhibited both enzymes in the micromolar range. Its activity is compared to other potential inhi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Deras IL,Takegawa K,Kondo A,Kato I,Lee YC

更新日期：1998-07-07 00:00:00

abstract：:The advancement of a series of ligand efficient 2-amino-[1,2,4]triazolo[1,5-a]pyridines, initially identified from high-throughput screening, to a JAK2 inhibitor with pharmacodynamic activity in a mouse xenograft model is disclosed. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Siu M,Pastor R,Liu W,Barrett K,Berry M,Blair WS,Chang C,Chen JZ,Eigenbrot C,Ghilardi N,Gibbons P,He H,Hurley CA,Kenny JR,Cyrus Khojasteh S,Le H,Lee L,Lyssikatos JP,Magnuson S,Pulk R,Tsui V,Ultsch M,Xiao Y,Zh

更新日期：2013-09-01 00:00:00

abstract：:Based on the findings that cholest-4-en-3-one, an intestinal metabolite of cholesterol, has an anti-obesity effect on animals, the structure-effect relationship of its 3-oxo derivatives and related compounds were investigated. Cholesten-3-ones, which possesses an enone structure with a carbonyl group at C3, markedly i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Suzuki K,Shimizu T,Nakata T

更新日期：1998-08-18 00:00:00

abstract：:A series of novel 2,3-dihydro-4H-1-benzoselenin-4-one (thio)semicarbazone derivatives were designed and synthesized by using molecular hybridization approach. All the target compounds were characterized by HRMS and NMR and evaluated in vitro antifungal activity against five pathogenic strains. In comparison with precu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu H,Su X,Liu XQ,Zhang KP,Hou Z,Guo C

更新日期：2019-12-01 00:00:00

abstract：:The NMR structures of gentamicin and paromomycin in complex with the A-site of Escherichia coli 16S ribosomal RNA were modified with molecular modeling to 12 analogues. The intermolecular interactions between these molecules and RNA were examined using the HINT (Hydropathic INTeractions) computational model to obtain ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cashman DJ,Rife JP,Kellogg GE

更新日期：2001-01-22 00:00:00

abstract：:Regioselective synthesis, biological evaluation and 3D-molecular modeling for a series of novel diastereomeric 2-thioxo-5H-dispiro[imidazolidine-4,3-pyrrolidine-2,3-indole]-2,5(1H)-diones are described. The studied compounds have been tentatively identified as potent small molecule MDM2/p53 PPI inhibitors and can ther...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ivanenkov YA,Vasilevski SV,Beloglazkina EK,Kukushkin ME,Machulkin AE,Veselov MS,Chufarova NV,Chernyaginab ES,Vanzcool AS,Zyk NV,Skvortsov DA,Khutornenko AA,Rusanov AL,Tonevitsky AG,Dontsova OA,Majouga AG

更新日期：2015-01-15 00:00:00

abstract：:The structure-based approaches were implemented to design and rationally select the molecules for synthesis and anti-HCV activity evaluation. The systematic structure-activity relationships of previously discovered molecules (types I, II, III) were analyzed to design new molecules (type IV) by bioisosteric replacement...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thiyagarajan A,Salim MT,Balaraju T,Bal C,Baba M,Sharon A

更新日期：2012-12-15 00:00:00

abstract：:RNA regulation and maintenance are critical for proper cell function. Small molecules that specifically alter RNA sequence would be exceptionally useful as probes of RNA structure and function or as potential therapeutics. Here, we demonstrate a photochemical approach for altering the trinucleotide expanded repeat cau...

journal_title：Bioorganic & medicinal chemistry letters

authors： Guan L,Luo Y,Ja WW,Disney MD

更新日期：2018-09-01 00:00:00

abstract：:MDM2 and MDMX are oncoproteins that negatively regulate the activity and stability of the tumor suppressor protein p53. The inhibitors of protein-protein interactions (PPIs) of MDM2-p53 and MDMX-p53 represent potential anticancer agents. In this study, a novel approach for identifying MDM2-p53 and MDMX-p53 PPI inhibit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Noguchi T,Oishi S,Honda K,Kondoh Y,Saito T,Kubo T,Kaneda M,Ohno H,Osada H,Fujii N

更新日期：2013-07-01 00:00:00

abstract：:In search of effective antidiabetic agents having therapeutic effect by inhibiting α-glucosidase and preventive effect by scavenging free radicals, Horsfieldia macrobotrys showed promising bioactivity required for the proposed criteria. Bioassay-guided isolation of the stem bark extract resulted in two new arylalkanon...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ramadhan R,Phuwapraisirisan P

更新日期：2015-10-15 00:00:00

abstract：:Positive allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) is regarded as a potential novel treatment for schizophrenic patients. Herein we report the synthesis and SAR of 4-aryl piperazine and piperidine amides as potent mGluR5 positive allosteric modulators (PAMs). Several analogs have excellent ac...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiong H,Brugel TA,Balestra M,Brown DG,Brush KA,Hightower C,Hinkley L,Hoesch V,Kang J,Koether GM,McCauley JP Jr,McLaren FM,Panko LM,Simpson TR,Smith RW,Woods JM,Brockel B,Chhajlani V,Gadient RA,Spear N,Sygowski LA

更新日期：2010-12-15 00:00:00

abstract：:We have designed and synthesized a novel series of 3-biphenylamino acid amides as cathepsin K inhibitors based on compound I. In these inhibitors, we have discovered 4-aminophenoxyacetic acids 43 and 47 with good IC(50) values, although lipophilic groups are favorable for the hydrophobic S1' pocket. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shinozuka T,Shimada K,Matsui S,Yamane T,Ama M,Fukuda T,Taki M,Naito S

更新日期：2006-03-15 00:00:00

abstract：:Ligand-based virtual screening led to the discovery of a new class of potent inverse agonists of the human cannabinoid receptor 1, hCB(1), which are selective versus hCB(2). These CB(1) ligands present intriguing departures from a classical CB(1) antagonist pharmacophore. Elements of SAR are discussed in this context....

journal_title：Bioorganic & medicinal chemistry letters

authors： Foloppe N,Allen NH,Bentley CH,Brooks TD,Kennett G,Knight AR,Leonardi S,Misra A,Monck NJ,Sellwood DM

更新日期：2008-02-01 00:00:00

abstract：:Mimetics of phosphotyrosine (pTyr) such as phosphonomethylphenylalanine (Pmp) have traditionally retained alpha-amino functionality. However, beta-amino acids represent isomeric variants, which may exhibit properties that are distinct from the parent. Reported herein is the first beta-amino pTyr mimetic (Pmp(beta)) be...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee K,Zhang M,Yang D,Burke TR Jr

更新日期：2002-12-02 00:00:00

abstract：:The efflux transporter protein P-glycoprotein (P-gp) is capable of affecting the central distribution of diverse neurotherapeutics, including opioid analgesics, through their active removal from the brain. P-gp located at the blood brain barrier has been implicated in the development of tolerance to opioids and demons...

journal_title：Bioorganic & medicinal chemistry letters

authors： Metcalf MD,Rosicky AD,Hassan HE,Eddington ND,Coop A,Cunningham CW,Mercer SL

更新日期：2014-08-01 00:00:00

abstract：:Substituted benzimidazoles were profiled as inhibitors of kinesin spindle protein (KSP), an increasingly important target for the development of anticancer drugs. This series demonstrated the monoastral phenotypic response and was found to be active in both enzymatic and cellular-based assays. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lahue BR,Ma Y,Shipps GW Jr,Seghezzi W,Herbst R

更新日期：2009-07-01 00:00:00

abstract：:Various 1,3,4-oxadiazole derivatives have been synthesized and their antiproliferative properties have been studied. The in vitro screening was performed against androgen dependent (LNCaP) and androgen independent (PC-3) prostate cancer cell lines. Most of the compounds showed promising activity. Among them, compounds...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mochona B,Qi X,Euynni S,Sikazwi D,Mateeva N,Soliman KF

更新日期：2016-06-15 00:00:00

abstract：:The discovery, SAR, and X-ray crystal structure of novel biarylaminoacyl-(S)-2-cyano-pyrrolidines and biarylaminoacylthiazolidines as potent inhibitors of dipeptidyl peptidase IV (DPP IV) are reported. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qiao L,Baumann CA,Crysler CS,Ninan NS,Abad MC,Spurlino JC,Desjarlais RL,Kervinen J,Neeper MP,Bayoumy SS,Williams R,Deckman IC,Dasgupta M,Reed RL,Huebert ND,Tomczuk BE,Moriarty KJ

更新日期：2006-01-01 00:00:00

abstract：:Viral transcription has not been routinely targeted in the development of new antiviral drugs. This crucial step of the viral cycle depends on the concerted action of cellular and viral proteins such as NF-kappaB and Tat. In the present study, stilbene-related heterocyclic compounds including benzalphthalide, phthalaz...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bedoya LM,del Olmo E,Sancho R,Barboza B,Beltrán M,García-Cadenas AE,Sánchez-Palomino S,López-Pérez JL,Muñoz E,San Feliciano A,Alcamí J

更新日期：2006-08-01 00:00:00

abstract：:An efficient synthesis of [D-lysine](8)cyclosporin A has been developed. Several analogs of [D-lysine](8)cyclosporin A have been synthesized and show promising anti-HCV activity, particularly compounds 39 and 43, which each exhibit an anti-HCV EC(50)<200 nM, and are each ≥50-fold less immunosuppressive than cyclospori...

journal_title：Bioorganic & medicinal chemistry letters

authors： Scribner A,Houck D,Huang Z,Mosier S,Peel M,Scorneaux B

更新日期：2010-11-15 00:00:00