Turn-on fluorescent probe with visible light excitation for labeling of hexahistidine tagged protein.

abstract：:The synthesis and SAR of benzylamine side chain analogs of the NK-1 receptor antagonist CP-99,994 are described. The 5-trifluoromethoxy analog, CP-122,721, shows superior in vivo blockade of NK-1 receptor mediated responses. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rosen TJ,Coffman KJ,McLean S,Crawford RT,Bryce DK,Gohda Y,Tsuchiya M,Nagahisa A,Nakane M,Lowe JA 3rd

更新日期：1998-02-03 00:00:00

abstract：:Alkaline phosphatase (AP) isozymes are present in a wide range of species from bacteria to man and are capable of dephosphorylation and transphosphorylation of a wide spectrum of substrates in vitro. In humans, four AP isozymes have been identified-one tissue-nonspecific (TNAP) and three tissue-specific-named accordin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ardecky RJ,Bobkova EV,Kiffer-Moreira T,Brown B,Ganji S,Zou J,Pass I,Narisawa S,Iano FG,Rosenstein C,Cheltsov A,Rascon J,Hedrick M,Gasior C,Forster A,Shi S,Dahl R,Vasile S,Su Y,Sergienko E,Chung TDY,Kaunitz J,H

更新日期：2014-02-01 00:00:00

abstract：:The stereochemical effects of the hydrocarbon crosslink on the conformation and cellular uptake of i,i+4 stapled peptides were studied. Compared to its S,S-configurated counterpart, the crosslink bearing the R,R-configuration provided a significantly diminished helix stabilizing effect and conferred less efficient cel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim YW,Verdine GL

更新日期：2009-05-01 00:00:00

abstract：:In a previous study, we found that the 3,4-dihydroquinazoline derivative, 4-(Benzylcarbamoylmethyl)-2-(biphenyl-4-ylamino)-3-(5-tert-butyloxycarbamoyl-1-pentyl)-3,4-dihydroquinazoline (KYS05047), was a selective T-type Ca(2+) channel blocker with anti-proliferative effects against various cancer cells. However, the me...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rim HK,Lee HW,Choi IS,Park JY,Choi HW,Choi JH,Cho YW,Lee JY,Lee KT

更新日期：2012-12-01 00:00:00

abstract：:Lactimidomycin (LTM, 1), iso-migrastatin (iso-MGS, 2) and migrastatin (MGS, 3) are macrolide antitumor antibiotics differing in macrolide ring size but all bearing a glutarimide side chain. To further develop these natural products and related analogs as drug candidates we have produced and evaluated the biological ac...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ju J,Rajski SR,Lim SK,Seo JW,Peters NR,Hoffmann FM,Shen B

更新日期：2008-11-15 00:00:00

abstract：:Structure-activity relationships and efforts to optimize the pharmacokinetic profile of isosteric analogs of 2-arylimino-5,6-dihydro-4H-1,3-thiazines as cannabinoid receptor agonists are described. Among those examined, compound 25 showed potent affinity for cannabinoid receptor 1 (CB1) and receptor 2 (CB2). This comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kai H,Morioka Y,Koriyama Y,Okamoto K,Hasegawa Y,Hattori M,Koike K,Chiba H,Shinohara S,Iwamoto Y,Takahashi K,Tanimoto N

更新日期：2008-12-15 00:00:00

abstract：:Twenty-six new hydrophilic chiral 2-alkoxy-1,4-butanediamine platinum (II) complexes having a seven-membered ring structure between a bidentate carrier ligand and a platinum atom have been synthesized and most of them were evaluated for their in vitro cytotoxicity toward A549 human non-small cell lung carcinoma and HC...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhu H,Cui K,Wang L,Gou S

更新日期：2005-11-15 00:00:00

abstract：:4'-Modified noraristeromycin (NAM) analogs, 4'-sulfo-, 4'-sulfamoy, 4'-azido and 4'-amino-NAM, were systematically synthesized. The inhibitory activities of these analogs and related compounds against Plasmodium falciparum and human S-adenosyl-L-homocysteine hydrolase were investigated. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ando T,Kojima K,Chahota P,Kozaki A,Milind ND,Kitade Y

更新日期：2008-04-15 00:00:00

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：:A catalyst-free synthesis of 6,9-dihydro-[1,3]dioxolo[4,5-g]thieno[3,4-b]quinolin-8(5H)-ones as novel analogues of podophyllotoxins was developed by a three-component reaction of aldehydes, ethyl 2,4-dioxotetrahydrothiophene-3-carboxylate and 3,4-(methylenedioxy)aniline. This methodology not only provides new chemical...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li T,Lu T,Yu C,Yao C

更新日期：2015-04-01 00:00:00

abstract：:RO4396686 is a small molecule KDR, FGFR, and PDGFR inhibitor with good pharmacokinetic properties in rodents. In a mouse corneal neovascularization assay, this compound inhibited VEGF-induced angiogenesis. Tested in a H460a xenograft tumor model this agent effected significant tumor growth inhibition at doses as low a...

journal_title：Bioorganic & medicinal chemistry letters

authors： McDermott LA,Higgins B,Simcox M,Luk KC,Nevins T,Kolinsky K,Smith M,Yang H,Li JK,Chen Y,Ke J,Mallalieu N,Egan T,Kolis S,Railkar A,Gerber L,Liu JJ,Konzelmann F,Zhang Z,Flynn T,Morales O,Chen Y

更新日期：2006-04-01 00:00:00

abstract：:The synthesis of the beta-peptide 1 by the postsynthetic modification of the corresponding amino-containing peptide 3 is described. The potential of 1 to act as a template for the ligation of complementary negatively-charged peptides is discussed. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wen K,Han H,Hoffman TZ,Janda KD,Orgel LE

更新日期：2001-03-12 00:00:00

abstract：:Two classes of compounds, thiocarbamates 1 and triazoles 2, have been identified as HIV RT RNase H inhibitors using a novel FRET-based HTS assay. The potent analogs in each series exhibited selectivity and were active in cell-based assays. In addition, saturable, 1:1 stoichiometric binding to target was established an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Di Grandi M,Olson M,Prashad AS,Bebernitz G,Luckay A,Mullen S,Hu Y,Krishnamurthy G,Pitts K,O'Connell J

更新日期：2010-01-01 00:00:00

abstract：:In the course of our studies of the structure-activity relationships of himbacine 1, a potent antagonist of the M(2) subtype of muscarinic receptor, the four title compounds, 2, ent-2, 3, and ent-3, were synthesized with a highly stereoselective intermolecular Diels-Alder reaction of tetrahydroisobenzofuran 4 with ach...

journal_title：Bioorganic & medicinal chemistry letters

authors： Takadoi M,Yamaguchi K,Terashima S

更新日期：2002-11-18 00:00:00

abstract：:Human isoprenylcysteine carboxyl methyltransferase (hIcmt) is a promising anticancer target as it is important for the post-translational modification of oncogenic Ras proteins. We herein report the synthesis and biochemical activity of 41 farnesyl-cysteine based analogs versus hIcmt. We have demonstrated that the ami...

journal_title：Bioorganic & medicinal chemistry letters

authors： Majmudar JD,Hahne K,Hrycyna CA,Gibbs RA

更新日期：2011-05-01 00:00:00

abstract：:The synthesis and in vitro Class III antiarrhythmic activity of several 4-aroyl (and aryl)-1-aralkylpiperazine and piperidine derivatives are described. Among several potent compounds identified in the series, RWJ-28810 (3), with its EC20 of 3 nM, ranks as one of the most potent (in vitro) compounds reported. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kanojia RM,Salata JJ,Kauffman J

更新日期：2000-12-18 00:00:00

abstract：:The selectivity and the binding affinity of previously reported carborane-containing ligands 2 and 3 toward ERβ remains to be optimized. To improve their biological profiles, a series of iodinated carboranyl phenol derivatives (4-6) were designed and synthesized as prospective ERβ-selective ligands with high affinity....

journal_title：Bioorganic & medicinal chemistry letters

authors： Ohta K,Ogawa T,Endo Y

更新日期：2017-09-01 00:00:00

abstract：:In this study, five novel triterpenes were isolated from hydrolyzate of total saponins from Gynostemma pentaphyllum and identified as gypensapogenin H (1), gypensapogenin I (2), gypensapogenin L (3), gypensapogenin J (4) and gypensapogenin K (5), three of which (1-3) possess unprecedented ring A. All the isolated comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang XS,Cao JQ,Zhao C,Wang XD,Wu XJ,Zhao YQ

更新日期：2015-08-15 00:00:00

abstract：:NCSi-gb is a neocarzinostatin chromophore (NCS-chrom) metabolite which binds strongly to certain two-base DNA bulges. Compared with previously reported NCSi-gb analogues, a new analogue with a different aminoglycoside position was synthesized, and it showed strong fluorescence and improved binding and sequence selecti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiao Z,Kappen LS,Goldberg IH

更新日期：2006-06-01 00:00:00

abstract：:The chemical resolution, using N-tosyl-L-proline as a chiral auxiliary, of a racemate of the pyrazole analog (+/-)-N-Boc-CPzI of the left hand segment (CPI) of the antitumor agent CC-1065, and the cytotoxic evaluation of both enantiomers are described. The reported results further validate the direct relationship betw...

journal_title：Bioorganic & medicinal chemistry letters

authors： Baraldi PG,Cacciari B,Romagnoli R,Spalluto G,Boyce CW,Boger DL

更新日期：1999-11-01 00:00:00

abstract：:Mirror-image screening using d-proteins is a powerful approach to provide mirror-image structures of chiral natural products for drug screening. During the course of our screening study for novel MDM2-p53 interaction inhibitors, we identified that NPD6878 (R-(-)-apomorphine) inhibited both the native l-MDM2-l-p53 inte...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ishiba H,Noguchi T,Shu K,Ohno H,Honda K,Kondoh Y,Osada H,Fujii N,Oishi S

更新日期：2017-06-01 00:00:00

abstract：:Nine new monoterpene glycosides (1-9), together with 18 known compounds were obtained from the n-butanol soluble fraction of ethanol extract from Paeonia suffruticosa Andrews. Their structures were determined on the basis of chemical methods and spectroscopic data. The inhibitory effects of these compounds (except com...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ding L,Zhao F,Chen L,Jiang Z,Liu Y,Li Z,Qiu F,Yao X

更新日期：2012-12-01 00:00:00

abstract：:A two-step reaction cascade is applied to the sequence-specific detection of single-stranded DNA, including analyte-triggered re-activation of apo-aldolase by its cofactor Zn(2+) and catalytic conversion of a chromophore. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Graf N,Kassube S,Krämer R

更新日期：2008-09-01 00:00:00

abstract：:A series of novel 5-(substituted benzylidene)thiazolidine-2,4-dione derivatives was designed, and synthesized based on our previous studies. Also their activities were evaluated as competitive inhibitors of protein tyrosine phosphatase 1B (PTP1B). Compounds 6d-6g, 7b, 7c, 7e, 7j, 7k, 7m, 14b and 14e-14f showed potent ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang Z,Liu Z,Lee W,Kim SN,Yoon G,Cheon SH

更新日期：2014-08-01 00:00:00

abstract：:High throughput screening of the corporate compound collection led to the discovery of a novel series of substituted aminoalkoxybenzyl pyrrolidines as human urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, and optimization of the initial hit that led to the identification of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jin J,Dhanak D,Knight SD,Widdowson K,Aiyar N,Naselsky D,Sarau HM,Foley JJ,Schmidt DB,Bennett CD,Wang B,Warren GL,Moore ML,Keenan RM,Rivero RA,Douglas SA

更新日期：2005-07-01 00:00:00

abstract：:A series of 5-HT(6) ligands derived from (R)-1-(amino)methyl-6-(phenyl)sulfonyltetralin was prepared that yielded several non-basic analogs having sub-nanomolar affinity. Ligand structure-activity relationships, receptor point mutation studies, and molecular modeling of these novel ligands all combined to reveal a new...

journal_title：Bioorganic & medicinal chemistry letters

authors： Harris RN 3rd,Stabler RS,Repke DB,Kress JM,Walker KA,Martin RS,Brothers JM,Ilnicka M,Lee SW,Mirzadegan T

更新日期：2010-06-01 00:00:00

abstract：:This report describes the design and synthesis of a series of CCR2 antagonists incorporating novel non-aryl/heteroaryl RHS (right hand side) motifs. Previous SAR in the area has suggested an aryl/heteroaryl substituent as a necessary structural feature for binding to the CCR2 receptor. Herein we describe the SAR with ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Trujillo JI,Huang W,Hughes RO,Rogier DJ,Turner SR,Devraj R,Morton PA,Xue CB,Chao G,Covington MB,Newton RC,Metcalf B

更新日期：2011-03-15 00:00:00

abstract：:The diacylglycerol acyltransferase enzyme, DGAT1, presents itself as a potential target for obesity as this enzyme is dedicated to the final committed step in triglyceride biosynthesis. Biphenyl ureas, exemplified by compound 4, have been reported to be potent hDGAT1 inhibitors. We have synthesized and evaluated 2-pyr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Motiwala H,Kandre S,Birar V,Kadam KS,Rodge A,Jadhav RD,Mahesh Kumar Reddy M,Brahma MK,Deshmukh NJ,Dixit A,Doshi L,Gupte A,Gangopadhyay AK,Vishwakarma RA,Srinivasan S,Sharma M,Nemmani KV,Sharma R

更新日期：2011-10-01 00:00:00

abstract：:Aspartic protease analogues synthesized by covering the surface of silica gel with carboxyl groups effectively hydrolyzed hemoglobin and gamma-globulin. It is proposed that the carboxyl group is involved in both complexation of the protein substrate and the catalytic cleavage of the peptide bonds of the complexed prot...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim H,Chung YS,Paik H,Kim MS,Suh J

更新日期：2002-10-07 00:00:00

abstract：:A series of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors was discovered. Several compounds such as 15 and 20 showed good hNET potency. Compounds 15 and 20 also displayed excellent selectivity at hNET that appeared superior to those of reboxe...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang P,Terefenko EA,McComas CC,Mahaney PE,Vu A,Trybulski E,Koury E,Johnston G,Bray J,Deecher D

更新日期：2008-12-01 00:00:00