Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists.

abstract：:Resistance of malaria parasites has quickly developed to almost all used antimalarial drugs. Accordingly, the discovery of new effective drugs to counter the spread of malaria parasites that are resistant to existing agents, especially acting on multi-targets, is an urgent need. The cysteine protease falcipain-2 (FP-2...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang H,Lu W,Li X,Cong X,Ma H,Liu X,Zhang Y,Che P,Ma R,Li H,Shen X,Jiang H,Huang J,Zhu J

更新日期：2012-01-15 00:00:00

abstract：:The in vitro activity of novel 4-substituted imidazole antifungals was optimized by solid-phase chemistry and parallel synthesis. Potent yeast-selective as well as broad-spectrum antifungal compounds (32 and 20) were discovered. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Saha AK,Liu L,Marichal P,Odds F

更新日期：2000-12-18 00:00:00

abstract：:A few substituted piperazinylphenyloxazolidinone compounds 6-13 having substitution on the distant nitrogen atom of piperazine ring scaffold have been synthesized and evaluated for their antibacterial activity in Gram-positive bacteria. A few compounds showed superior in vitro antibacterial activity against Staphyloco...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lohray BB,Lohray VB,Srivastava BK,Gupta S,Solanki M,Pandya P,Kapadnis P

更新日期：2006-03-15 00:00:00

abstract：:A new halicyclamine derivative, tetradehydrohalicyclamine B (1), was isolated from the marine sponge Acanthostrongylophora ingens, along with halicyclamine B (2) as proteasome inhibitors. Compound 1 is the second example found to have a pyridinium ring in the halicyclamine family. Although the relative configuration o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kato H,El-Desoky AH,Takeishi Y,Nehira T,Angkouw ED,Mangindaan REP,de Voogd NJ,Tsukamoto S

更新日期：2019-01-01 00:00:00

abstract：:On the search for anti-cancer compounds from natural Korean medicinal sources, a bioassay-guided fractionation and chemical investigation of the MeOH extract from the rhizomes of Acorus gramineus resulted in the isolation and identification of thirteen phenolic derivatives (1-13) including two new 8-O-4'-neolignans, n...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim KH,Moon E,Kim HK,Oh JY,Kim SY,Choi SU,Lee KR

更新日期：2012-10-01 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：:A novel class of 2,3-tri- and tetrasubstituted γ-butyrolactones analogous to paraconic acids has been synthesized in one step using a straightforward three-component reaction among aryl bromides, dimethyl itaconate and carbonyl compounds. The in vitro cytotoxic activity of representative compounds has been evaluated a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Le Floch C,Le Gall E,Léonel E,Martens T,Cresteil T

更新日期：2011-12-01 00:00:00

abstract：:An efficient and simple polymer-assisted approach has been developed to biotinylate multifunctional compounds bearing an amino functionality. Biotin was immobilized on aminomethylated polystyrene via the Kenner safety catch linker, activated and subsequently transferred to the amino function of the target compounds ch...

journal_title：Bioorganic & medicinal chemistry letters

authors： Golisade A,Herforth C,Wieking K,Kunick C,Link A

更新日期：2001-07-09 00:00:00

abstract：:To discover new natural-product-based insecticidal agents, a series of novel oxime derivatives of podophyllotoxin-based phenazines modified in the C, D and E rings of podophyllotoxin were prepared and tested as insecticidal agents against the pre-third-instar larvae of oriental armyworm, Mythimna separata (Walker) in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhi X,Yang C,Yu X,Xu H

更新日期：2014-12-15 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：:Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites. In order to reduce attrition due to metabolism-induced toxicity and to improve the safety of drug candidates, we developed a simple cell viability assay by combining a bioactivation system (huma...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rana P,Will Y,Nadanaciva S,Jones LH

更新日期：2016-08-15 00:00:00

abstract：:The preparation and structure-activity-relationships of novel pyrrolidine-carboxamides and oxadiazoles are described. Compounds in this series were found to be potent hNK(1) antagonists in vitro and efficacious in vivo with minimal interactions with P(450) liver enzymes. Oxadiazole analog 22 was determined to have exc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Young JR,Eid R,Turner C,DeVita RJ,Kurtz MM,Tsao KL,Chicchi GG,Wheeldon A,Carlson E,Mills SG

更新日期：2007-10-01 00:00:00

abstract：:A series of 3,4-dihydroquinazoline derivatives consisting of the selected compounds from our chemical library on the diversity basis and the new synthetic compounds were in vitro tested for their inhibitory activities for both acetylcholinesterase (AChE, from electric eel) and butyrylcholinesterase (BChE, from equine ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park B,Nam JH,Kim JH,Kim HJ,Onnis V,Balboni G,Lee KT,Park JH,Catto M,Carotti A,Lee JY

更新日期：2017-03-01 00:00:00

abstract：:Thirty-five novel chromone derivatives containing dithioacetal moiety were designed, synthesized, and their anti-TMV activities were evaluated through half-leaf method. The results showed compound c23 illustrates highly curative, protective and inactivating activities against TMV at 500 mg/L, with the values of 68.8%,...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li M,Zan N,Huang M,Jiang D,Hu D,Song B

更新日期：2020-03-01 00:00:00

abstract：:A series of novel cyclic analogues of curcumin were synthesized and analyzed for in vitro cytostatic activity. Condensation of 2-acetylcycloalkanones with a variety of aromatic aldehydes resulted in the formation of 2-arylidene-6-(3-arylacryoyl)-cycloalkanone derivatives. A number of these analogues were found to have...

journal_title：Bioorganic & medicinal chemistry letters

authors： Youssef D,Nichols CE,Cameron TS,Balzarini J,De Clercq E,Jha A

更新日期：2007-10-15 00:00:00

abstract：:A series of pyrimidine derivatives as acid pump antagonists (APAs) was synthesized and the inhibitory activities against H(+)/K(+) ATPase isolated from hog gastric mucosa were determined. After elaborating on substituents at C2 and C4 position of the pyrimidine scaffold, we have observed that the compound 7h is a pote...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yoon YA,Park CS,Cha MH,Choi H,Sim JY,Kim JG

更新日期：2010-10-01 00:00:00

abstract：:Incorporation of a 4-hydroxy-N-acetylprolinol nucleotide analogue at the 3'-terminus of DNA or 2-5A-DNA sequences resulted in a significantly enhanced 3'-exonuclease resistance while the affinity for complementary RNA was only slightly decreased. Furthermore, the binding to and activation of human RNase L by thus modi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Verheijen JC,van Roon AM,Meeuwenoord NJ,Stuivenberg HR,Bayly SF,Chen L,van der Marel GA,Torrence PF,van Boom JH

更新日期：2000-04-17 00:00:00

abstract：:Relying on the high affinities of the benz-indolo-azecine LE 300 (1) and the hydroxylated dibenz-azecine LE 404 (2b) for the D1/D5 receptor subtypes, we synthesized methoxylated, hydroxylated and an indole-N methylated derivatives of 1 (Fig. 1). Hydroxylation of azecine derivatives is beneficial with regard to the aff...

journal_title：Bioorganic & medicinal chemistry letters

authors： Enzensperger C,Kilian S,Ackermann M,Koch A,Kelch K,Lehmann J

更新日期：2007-03-01 00:00:00

abstract：:The underlying mechanisms of urocanic acid (UA) to induce immune suppression remain elusive until the recent finding that cis-UA acts via the serotonin, 5-hydroxytryptamine (5-HT) receptor subtype 5-HT(2A). In the present study, the interactions of cis-UA to 5-HT(2A) receptor were explored and compared with those of 5...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shen L,Ji HF

更新日期：2009-09-15 00:00:00

abstract：:Clausenamide, isolated from aqueous extract of dry leaves of Clausena lansium, a Chinese folk medicine, was found to have potent activity in enhancing LTP and show nootropic activity in animal tests. In order to discovery more potent stereoisomers and to analyze the relationship of structure-activity, the synthesis of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Feng Z,Li X,Zheng G,Huang L

更新日期：2009-04-15 00:00:00

abstract：:2-Octyl gamma-bromoacetoacetate (O gamma Br), an endogenous compound originally isolated from human cerebrospinal fluid (CSF), has previously been demonstrated to increase REM sleep duration in cats. Based on the chemical structure of O gamma Br and its reported sleep-inducing effects, we synthesized O gamma Br along ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patricelli MP,Patterson JE,Boger DL,Cravatt BF

更新日期：1998-03-17 00:00:00

abstract：:2-(Anilino)imidazolines were identified as novel human 5-HT(1D) receptor ligands, but offered no particular advantage over previously reported 2-(benzyl)imidazolines. Pharmacokinetic and functional data were obtained for selected 2-(benzyl)imidazoline derivatives. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Prisinzano T,Dukat M,Law H,Slassi A,MacLean N,DeLannoy I,Glennon RA

更新日期：2004-09-20 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：:In order to define the structural requirements of quinazoline-2(1H)-thiones 1 for their inhibitory activity on melanogenesis, a novel series of 3,4-dihydroquinazoline-2(1H)-thiones (3a-h) were prepared and screened for their melanogenesis inhibition on melanoma B16 cell line under the stimulant of alpha-MSH. The anti-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thanigaimalai P,Sharma VK,Lee KC,Yun CY,Kim Y,Jung SH

更新日期：2010-08-15 00:00:00

abstract：:Five new p-terphenyls named prenylterphenyllin D (1), prenylterphenyllin E (2), 2'-O-methylprenylterphenyllin (3), 4-O-methylprenylterphenyllin (4) and 3'-O-methylterphenyllin (5) together with seven known compounds (6-12), were isolated from cultures of Aspergillus sp. YXf3. The structures of the new compounds were e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yan W,Wuringege,Li SJ,Guo ZK,Zhang WJ,Wei W,Tan RX,Jiao RH

更新日期：2017-01-01 00:00:00

abstract：:Novel, metabolically stable and centrally acting TRH analogues with substituted pyridinium moieties replacing the [His(2)] residue of the endogenous peptide were prepared by solid-phase Zincke reaction. The 1,4-dihydropyridine prodrugs of these analogues obtained after reducing the pyridinium moiety were able to reach...

journal_title：Bioorganic & medicinal chemistry letters

authors： Prokai-Tatrai K,Perjési P,Zharikova AD,Li X,Prokai L

更新日期：2002-08-19 00:00:00

abstract：:Optically active phenylpropanoic acid derivatives [(S)-5, and (R)-5] were prepared, and their affinities for peroxisome proliferator-activated receptor (PPAR)alpha and PPAR gamma were evaluated. Binding assay and cell-based reporter assay indicated that the activity of these compounds is enantio-dependent, and resides...

journal_title：Bioorganic & medicinal chemistry letters

authors： Miyachi H,Nomura M,Tanase T,Suzuki M,Murakami K,Awano K

更新日期：2002-02-11 00:00:00

abstract：:A new cytotoxic β-carboline alkaloid, 1-methyl-3-(2-hydroxypropan-2-yl)-2-(5-methoxy-9H-β-carbolin-1-yl)-cyclopentanol (1), was isolated from roots of Galianthe thalictroides, together with the alkaloid 1-(hydroxymethyl)-3-(2-hydroxypropan-2-yl)-2-(5-methoxy-9H-β-carbolin-1-yl)-cyclopentanol (2), the anthraquinones 1-...

journal_title：Bioorganic & medicinal chemistry letters

authors： de Oliveira Figueiredo P,Perdomo RT,Garcez FR,de Fatima Cepa Matos M,de Carvalho JE,Garcez WS

更新日期：2014-03-01 00:00:00

abstract：:A polyphemusin peptide analogue, T22 ([Tyr(5,12), Lys7]-polyphemusin II), and its shortened potent analogues, T134 (des-[Cys(8,13), Tyr(9,12)]-[D-Lys10, Pro11, L-citrulline16]-T22 without C-terminal amide) and T140 [[L-3-(2-naphthyl)alanine3]-T134], strongly inhibit the T-cell line-tropic (T-tropic) HIV-1 infection th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tamamura H,Omagari A,Oishi S,Kanamoto T,Yamamoto N,Peiper SC,Nakashima H,Otaka A,Fujii N

更新日期：2000-12-04 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