Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acid.

abstract：:Isoxazoles are frequently used amide isosteres, as shown in the context of discovery of CRTh2 antagonists from amide 1 to isoxazole 2. However, persistent agonism and poor solubility in isoxazole series presented challenges to its further development. Based on the concept of quality by design (QbD), 5,5-disubstituted ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiao D,Zhu X,Yu Y,Shao N,Wu J,McCormick KD,Dhondi P,Qin J,Mazzola R,Tang H,Rao A,Siliphaivanh P,Qiu H,Yang X,Rivelli M,Garlisi CG,Eckel S,Mukhopadhyay G,Correll C,Rindgen D,Aslanian R,Palani A

更新日期：2014-03-15 00:00:00

abstract：:Eight esters of 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinone with melphalan were prepared and tested for their antitumor activity (S-180) and cytotoxicity. 2-[1-[4-(p-Bis(2-chloroethyl)-aminophenyl)-butanoyloxy]methyl]-1,4-dihydroxy-9,10-anthraquinone and 2-[1-[4-(p-bis(2-chloroethyl)-aminophenyl)-butanoyloxy]e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jin G,You Y,Ahn B

更新日期：2001-06-04 00:00:00

abstract：:A computer-aided drug design strategy leads to the identification of a new class of p38 inhibitors based on the 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) scaffold. The tolyl triazole amides provided a potent platform amenable to optimization. Further exploration leads to compounds with greater than 100-fold improveme...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cogan DA,Aungst R,Breinlinger EC,Fadra T,Goldberg DR,Hao MH,Kroe R,Moss N,Pargellis C,Qian KC,Swinamer AD

更新日期：2008-06-01 00:00:00

abstract：:The bacterial protein tyrosine phosphatase YopH is an essential virulence determinant in Yersinia pestis and a potential antibacterial drug target. Here we report our studies of screening for small molecule inhibitors of YopH using both high throughput and in silico approaches. The identified inhibitors represent a di...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hu X,Vujanac M,Southall N,Stebbins CE

更新日期：2013-02-15 00:00:00

abstract：:A versatile route for the synthesis of homochiral alpha-ketoamide analogues of amino acids is described. Incorporation of this functionality into peptide sequences using either solution or solid-phase chemistry resulted in potent inhibitors of the Hepatitis C Virus NS3 proteinase. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Beevers R,Carr MG,Jones PS,Jordan S,Kay PB,Lazell RC,Raynham TM

更新日期：2002-02-25 00:00:00

abstract：:A new series of 1,2,4-triazole-linked urea and thiourea conjugates have been synthesized and evaluated for their in vitro cytotoxicity against selected human cancer cell lines namely, breast (MCF-7, MDA-MB-231), lung (A549) prostate (DU145) and one mouse melanoma (B16-F10) cell line and compared with reference drug. T...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tokala R,Bale S,Janrao IP,Vennela A,Kumar NP,Senwar KR,Godugu C,Shankaraiah N

更新日期：2018-06-01 00:00:00

abstract：:In the present communication we prepared a series of six 4-hydroxycoumarin derivatives, isosters of quercetin, recognized as an antioxidant natural compound, with the aim of evaluating the antitrypanosomal activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, and the antioxidant properties. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pérez-Cruz F,Serra S,Delogu G,Lapier M,Maya JD,Olea-Azar C,Santana L,Uriarte E

更新日期：2012-09-01 00:00:00

abstract：:Three novel metabolites of the angiotensin-II (A-II) receptor antagonist tasosartan have been identified in humans, and the syntheses and pharmacologic profiling of these metabolites are reported. Each metabolite bound the human A-II receptor with IC(50)s between 20 and 45nM. The in vivo effects of these compounds in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Elokdah HM,Friedrichs GS,Chai SY,Harrison BL,Primeau J,Chlenov M,Crandall DL

更新日期：2002-08-05 00:00:00

abstract：:The identification of a novel pyrazolidine-3,5-dione based scaffold hit compound as Farnesoid X receptor (FXR) partial or full agonist has been accomplished by means of virtual screening techniques. A series of pyrazolidine-3,5-dione derivatives (1a-u and 7) was designed, synthesized, and evaluated by a cell-based luc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Deng G,Li W,Shen J,Jiang H,Chen K,Liu H

更新日期：2008-10-15 00:00:00

abstract：:A novel series of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles has been synthesized. The ability of these compounds to act as antagonists of the androgen receptor was investigated and several were found to have potent activity in vitro and in vivo. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiao HY,Balog A,Attar RM,Fairfax D,Fleming LB,Holst CL,Martin GS,Rossiter LM,Chen J,Cvjic ME,Dell-John J,Geng J,Gottardis MM,Han WC,Nation A,Obermeier M,Rizzo CA,Schweizer L,Spires T Jr,Shan W,Gavai A,Salvati ME

更新日期：2010-08-01 00:00:00

abstract：:A high-throughput screening effort on 45,000 compounds resulted in the discovery of a disubstituted oxazole as a new structural class inhibitor of Mycobacterium tuberculosis (Mtb). In order to improve the activity and investigate the SAR of this scaffold, a series of disubstituted azole analogues have been designed an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li D,Gao N,Zhu N,Lin Y,Li Y,Chen M,You X,Lu Y,Wan K,Jiang JD,Jiang W,Si S

更新日期：2015-11-15 00:00:00

abstract：:Dimethylallyl (DMA) derivatives of a naturally occurring xanthone (decussatin 1) were prepared. Their activity as potential P-glycoprotein inhibitors was monitored by affinity of direct binding and compared to that of corresponding DMA-flavones. Both classes of compounds exhibited the same structure-activity relations...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tchamo DN,Dijoux-Franca MG,Mariotte AM,Tsamo E,Daskiewicz JB,Bayet C,Barron D,Conseil G,Di Pietro A

更新日期：2000-06-19 00:00:00

abstract：:We have described herein the syntheses of three novel series of aromatic ring containing pseudomycin side-chain analogues. Preliminary biological evaluations of these analogues clearly indicate that it is possible to synthesize rigid pseudomycin side-chain analogues without compromising in vitro antifungal activity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jamison J,Levy S,Sun X,Zeckner D,Current W,Zweifel M,Rodriguez M,Turner W,Chen SH

更新日期：2000-09-18 00:00:00

abstract：:Several unnatural derivatives of narciclasine were prepared in which the C-7 carbon was replaced with nitrogen. The 7-aza derivative and its N-oxide were prepared by the coupling of iodopicolinic acid with a conduramine unit derived chemoenzymatically from bromobenzene. Intramolecular Heck reaction was used to constru...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vshyvenko S,Reisenauer MR,Rogelj S,Hudlicky T

更新日期：2014-09-01 00:00:00

abstract：:The synthesis of a 20 member 2-aminoimidazole/triazole pilot library is reported. Each member of the library was screened for its ability to inhibit or promote biofilm development of either Escherichia coli and Acinetobacter baumannii. From this screen, E. coli-selective 2-aminoimidazoles were discovered, with the bes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Reed CS,Huigens RW 3rd,Rogers SA,Melander C

更新日期：2010-11-01 00:00:00

abstract：:Millettia pachycarpa Benth, a widely used anthelminthic drug in folk, is rich in flavonoids with various bioactivities. This study aimed to identify active flavonoids with anti-Alzheimer's disease (AD) effect from its seeds by a bioassay-guided isolation. A novel rotenoid with unusual oxidative ring-opening skeleton (...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tu Y,Wu C,Kang Y,Li Q,Zhu C,Li Y

更新日期：2019-05-15 00:00:00

abstract：:The synthesis and biological activity of novel CD-ring modified analogues of 22-oxa-1alpha,25-dihydroxyvitamin D(3), lacking the D-ring and featuring a connection between C-12 and C-21 (cis-perhydrindane CE-ring analogues), is described. The synthesis of the CE-ring system follows Meyers' methodology for the preparati...

journal_title：Bioorganic & medicinal chemistry letters

authors： Demin S,Van Haver D,Vandewalle M,De Clercq PJ,Bouillon R,Verstuyf A

更新日期：2004-08-02 00:00:00

abstract：:Gynostemma pentaphyllum has been widely used as a traditional herb for its antioxidant and immunostimulatory activities. We have previously reported several useful dammarane-type saponins with cytotoxicity against A549 human lung cancer cells from heat-processed G. pentaphyllum. In this study, a new dammarane-type sap...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xing SF,Jang M,Wang YR,Piao XL

更新日期：2016-04-01 00:00:00

abstract：:We have demonstrated that the p-trifluoromethylphenylpropionylamino residue at the 2-position of the core structure leads to an active benzophenone-type anti-malarial agent. The attempt to improve water solubility by introduction of an amino group into the alpha-position of the arylpropionyl residue resulted in decrea...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wiesner J,Fucik K,Kettler K,Sakowski J,Ortmann R,Jomaa H,Schlitzer M

更新日期：2003-05-05 00:00:00

abstract：:The 1,2,3-triazole ring fused with pyridine/pyrimidine was explored as new template for the identification of potential antimicrobial agents. The regioselective synthesis of these pre-designed N-heteroarenes was achieved via exploring the application of Buchwald's strategy (i.e. C-N bond formation/reduction/diazotizat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Marepu N,Yeturu S,Pal M

更新日期：2018-11-01 00:00:00

abstract：:β-Sitosterol is the most abundant plant sterol in the human diet. It is also the major component of several traditional medicines, including saw palmetto and devil's claw. Although β-sitosterol is effective against enlarged prostate in human clinical trials and has anti-cancer and anti-inflammatory activities, the mec...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lomenick B,Shi H,Huang J,Chen C

更新日期：2015-11-01 00:00:00

abstract：:Silybin is the major flavonolignan of silymarin and it displays a plethora of biological effects, generally ascribed to its antioxidant properties. Herein we shall describe an efficient synthetic strategy to obtain a variety of new and more water-soluble silybin and 2,3-dehydrosilybin (DHS) derivatives in which the 23...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zarrelli A,Sgambato A,Petito V,De Napoli L,Previtera L,Di Fabio G

更新日期：2011-08-01 00:00:00

abstract：:Incorporation of 5-propynylamino and 5-propynyl alpha-2'-deoxyuridine into alpha-oligonucleotides (alpha-ON) allows high-affinity targeting of complementary DNA for alpha-ON with anionic and neutral backbone but not for cationic alpha-ON, revealing clues on the role of the amino group of the propynylamino on the forma...

journal_title：Bioorganic & medicinal chemistry letters

authors： Deglane G,Morvan F,Debart F,Vasseur JJ

更新日期：2007-02-15 00:00:00

abstract：:In an effort to expand the spectrum of antibacterial activity associated with piperidin-4-one derivatives, we have synthesized two series of 3-carboxyethyl-2,6-diphenyl-4-hydroxy-Delta(3)-tetrahydropyridine derivatives bearing diversified heterocyclic and aromatic systems at the nitrogen atom through acetyl (6-18) and...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aridoss G,Amirthaganesan S,Jeong YT

更新日期：2010-04-01 00:00:00

abstract：:Heteroaromatic analogs of DMU-212 (8-15) have been synthesized and evaluated for their anti-cancer activity against a panel of 60 human cancer cell lines. These novel analogs contain a trans-3,4,5-trimethoxystyryl moiety attached to the C2 position of indole, benzofuran, benzothiazole or benzothiophene ring (8, 11, 13...

journal_title：Bioorganic & medicinal chemistry letters

authors： Penthala NR,Thakkar S,Crooks PA

更新日期：2015-07-15 00:00:00

abstract：:This Letter describes the further chemical optimization of the M5 PAM MLPCN probes ML129 and ML172. A multi-dimensional iterative parallel synthesis effort quickly explored isatin replacements and a number of southern heterobiaryl variations with no improvement over ML129 and ML172. An HTS campaign identified several ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gentry PR,Bridges TM,Lamsal A,Vinson PN,Smith E,Chase P,Hodder PS,Engers JL,Niswender CM,Daniels JS,Conn PJ,Wood MR,Lindsley CW

更新日期：2013-05-15 00:00:00

abstract：:Sodium channel blocking, anticonvulsant activity, and sigma (sigma) binding of selected leads in a series of alpha-amino amide anticonvulsants were examined. While anticonvulsant compounds were always endowed with low micromolar sodium (Na+) channel site-2 binding, compounds with low site-2 Na+ channel affinity failed...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pevarello P,Bonsignori A,Caccia C,Amici R,McArthur RA,Fariello RG,Salvati P,Varasi M

更新日期：1999-09-06 00:00:00

abstract：:Several benzyloxybenzaldehyde analogues were prepared and found to have significant inhibitory activity toward neutrophil superoxide formation. Consequently, these compounds were evaluated for cAMP-elevating capability. Among them, benzyloxybenzaldehyde (7), exhibiting activity equivalent to forskolin, was determined ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chang C,Kuo S,Lin Y,Wang J,Huang L

更新日期：2001-08-06 00:00:00

abstract：:A potent family of spirocyclic nicotinyl aminobenzamide selective HDAC1/HDAC2 inhibitors (SHI-1:2) is profiled. The incorporation of a biaryl zinc-binding motif into a nicotinyl scaffold resulted in enhanced potency and selectivity versus HDAC3, but also imparted hERG activity. It was discovered that increasing polar ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Methot JL,Hamblett CL,Mampreian DM,Jung J,Harsch A,Szewczak AA,Dahlberg WK,Middleton RE,Hughes B,Fleming JC,Wang H,Kral AM,Ozerova N,Cruz JC,Haines B,Chenard M,Kenific CM,Secrist JP,Miller TA

更新日期：2008-12-01 00:00:00

abstract：:The synthesis of bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines is described and their structure-activity-relationship to anaplastic lymphoma kinase (ALK) is presented. KRCA-0008 is selective and potent to ALK and Ack1, and displays drug-like properties without hERG liability. KRCA-0008 demonstra...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park CH,Choe H,Jang IY,Kwon SY,Latif M,Lee HK,Lee HJ,Yang EH,Yun JI,Chae CH,Cho SY,Choi SU,Ha JD,Jung H,Kim HR,Kim P,Lee CO,Yun CS,Lee K

更新日期：2013-11-15 00:00:00