Substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles as Src kinase inhibitors.

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：:A series of novel pyrimidone analogues have been designed and synthesized as HIV-1 integrase (IN) inhibitors. This study demonstrated that introducing a substituent in the N1-position of the pyrimidone scaffold does not significantly influence IN inhibitory activity. Molecular docking studies showed these compounds co...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yu S,Sanchez TW,Liu Y,Yin Y,Neamati N,Zhao G

更新日期：2013-11-15 00:00:00

abstract：:Potential prodrugs for the TRH-like tripeptide pGlu-Glu-Pro-NH(2) were synthesized either by esterifying the Glu side-chain of the parent peptide in solution with alcohols in the presence of resin-bound dicyclohexylcarbodiimide or by solid-phase peptide chemistry. Affinities of these ester prodrugs to lipid membranes ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Prokai-Tatrai K,Nguyen V,Zharikova AD,Braddy AC,Stevens SM,Prokai L

更新日期：2003-03-24 00:00:00

abstract：:We disclose a new compound class of potent and selective alpha-1A adrenergic receptor antagonists exemplified by the geminally, disubstituted cyclic imide 7. The optimization of lead compounds resulting in the cyclic imide motif is highlighted. The results of in vitro and in vivo studies of selected compounds are pres...

journal_title：Bioorganic & medicinal chemistry letters

authors： DiPardo RM,Patane MA,Newton RC,Price R,Broten TP,Chang RS,Ransom RW,Di Salvo J,Freidinger RM,Bock MG

更新日期：2001-07-23 00:00:00

abstract：:Resveratrol (Rsv) is widely reported to possess anticarcinogenic properties in a plethora of cellular and animal models having limited toxicity toward normal cells. In the molecular level, Rsv can act as a suppressive agent for several impaired signaling pathways on cancer cells. However, Fukuhara and Miyata have show...

journal_title：Bioorganic & medicinal chemistry letters

authors： Andrade Volkart P,Benedetti Gassen R,Mühlen Nogueira B,Nery Porto B,Eduardo Vargas J,Arigony Souto A

更新日期：2017-08-01 00:00:00

abstract：:A number of molecular recognition features have been exploited in structure-based design of selective Cathepsin inhibitors. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bethel PA,Gerhardt S,Jones EV,Kenny PW,Karoutchi GI,Morley AD,Oldham K,Rankine N,Augustin M,Krapp S,Simader H,Steinbacher S

更新日期：2009-08-15 00:00:00

abstract：:The four 2,2,5-regioisomer counterparts of SCH 51048 were synthesized and evaluated. As with the parent series, only the two cis isomers possessed any in vitro activity, and only the activity of the isomer with the R-configuration at the tetrahydrofuran 2-carbon was significant. The activity data suggests that oxygen ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lovey RG,Saksena AK,Girijavallabhan VM,Blundell P,Guzik H,Loebenberg D,Parmegiani RM,Cacciapuoti A

更新日期：2002-07-08 00:00:00

abstract：:A series of compounds based on a 4-phenyl-2-phenylaminopyridine scaffold that are potent and selective inhibitors of Traf2- and Nck-interacting kinase (TNIK) activity are described. These compounds were used as tools to test the importance of TNIK kinase activity in signaling and proliferation in Wnt-activated colorec...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ho KK,Parnell KM,Yuan Y,Xu Y,Kultgen SG,Hamblin S,Hendrickson TF,Luo B,Foulks JM,McCullar MV,Kanner SB

更新日期：2013-01-15 00:00:00

abstract：:Conformationally restricted analogues of the central linker unit of bacterial methionyl tRNA synthetase (MRS) inhibitors have been prepared. The (1S,2R)-cyclopentylmethyl moiety was identified as the preferred cyclic linker, with significant diastereo- and enantioselectivity of activity. Combination of this linker wit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jarvest RL,Berge JM,Brown P,Houge-Frydrych CS,O'Hanlon PJ,McNair DJ,Pope AJ,Rittenhouse S

更新日期：2003-04-07 00:00:00

abstract：:Using iron(III)porphyrins in combination with (diacetoxyiodo)benzene allows for the conversion of 2,9-bis(bromomethyl)-4,7-diphenyl-1,10-phenanthroline into 4,7-diphenyl-1,10-phenanthroline-2,9-dicarboxylic acid. This method provides a cost-effective and environmentally-friendly oxidation procedure using less toxic Ph...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhong QD,Xue YZ,Yan H,Song XQ,Zhong RG

更新日期：2010-09-15 00:00:00

abstract：:Nicotinic acid (niacin) has been used for decades as an antidyslipidemic drug in man. Its main target is the hydroxy-carboxylic acid receptor HCA2 (GPR109A), a G protein-coupled receptor. Other acids and esters such as methyl fumarate also interact with the receptor, which constituted the basis for the current study. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： van Veldhoven JP,Blad CC,Artsen CM,Klopman C,Wolfram DR,Abdelkadir MJ,Lane JR,Brussee J,Ijzerman AP

更新日期：2011-05-01 00:00:00

abstract：:Novel bioreductive and long-wavelength fluorescent markers for hypoxic cells in solid tumor, 9-isocyano-8H-acenaphtho[l,2-b]pyrrol-8-one with the side chain of 2-nitroimidazole, were designed, synthesized, and evaluated in V79 379A Chinese hamster cells in vitro. Compounds A(2) and A(4) showed good hypoxic-oxic fluore...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu Y,Xu Y,Qian X,Xiao Y,Liu J,Shen L,Li J,Zhang Y

更新日期：2006-03-15 00:00:00

abstract：:Current biosynthetic methods for producing proteins containing site-specifically incorporated unnatural amino acids are inefficient because the majority of the amino acid goes unused. Here we present a universal approach to improve the efficiency of such processes using condensed Escherichia coli cultures. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu J,Castañeda CA,Wilkins BJ,Fushman D,Cropp TA

更新日期：2010-10-01 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：:This paper documents a serious problem met during the testing of Gi protein-activating properties of a new series of synthetic compounds by measuring the induced binding of [(35)S]GTPgammaS to different subtypes of Gi protein. The problem arose from the strong affinity between [(35)S]GTPgammaS and the tested compounds...

journal_title：Bioorganic & medicinal chemistry letters

authors： Manetti D,Di Cesare Mannelli L,Dei S,Guandalini L,Martini E,Banchelli M,Ghelardini C

更新日期：2009-04-15 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：:A series of NN703 analogues with lysine mimetics combined with naphthyl- or biphenylalanine in the core has been prepared and tested in vitro in a rat pituitary cell based assay and subsequently in vivo in pigs in a single dose at 50 nmol/kg. Re-introduction of certain pharmacophores in the C-terminal of NN703, which ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hansen TK,Ankersen M,Raun K,Hansen BS

更新日期：2001-07-23 00:00:00

abstract：:Poly(ADP-ribose) polymerases (PARPs) play significant roles in various cellular functions including DNA repair and control of RNA transcription. PARP inhibitors have been demonstrated to potentiate the effect of cytotoxic agents or radiation in a number of animal tumor models. Utilizing a benzimidazole carboxamide sca...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhu GD,Gandhi VB,Gong J,Thomas S,Luo Y,Liu X,Shi Y,Klinghofer V,Johnson EF,Frost D,Donawho C,Jarvis K,Bouska J,Marsh KC,Rosenberg SH,Giranda VL,Penning TD

更新日期：2008-07-15 00:00:00

abstract：:A series of indene analogs of the H(1)-antihistamine (-)-R-dimethindene was evaluated for selectivity in the search for potentially improved sedative-hypnotics. Variation of the 6-substitutent in the indene core in combination with a pendant electron rich heterocycle led to the identification of several potent H(1)-an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li BF,Moree WJ,Yu J,Coon T,Zamani-Kord S,Malany S,Jalali K,Wen J,Wang H,Yang C,Hoare SR,Petroski RE,Madan A,Crowe PD,Beaton G

更新日期：2010-04-15 00:00:00

abstract：:Twenty-six novel pyrazolo[3,4-b]pyridine-bridged analogues of combretastatin A-4 possessing 3,4,5-trimethoxylphenyl groups, were synthesized and evaluated for their antiproliferative and tubulin polymerization inhibitory activities. Preliminary biological evaluation demonstrated that some of the target compounds displ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jian XE,Yang F,Jiang CS,You WW,Zhao PL

更新日期：2020-04-15 00:00:00

abstract：:Cyclic azobenzene carboxylic acid was synthesized using a shortened route. After reaction with D-threolinol, the resulting cyclic azobenzene-D-threolinol (cAB-Thr) building block was transformed into the corresponding DMTr-protected phosphoramidite, and incorporated into oligodeoxynucleotides at various positions and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Eljabu F,Dhruval J,Yan H

更新日期：2015-12-01 00:00:00

abstract：:In order to define the structural requirements of phenylthiourea (PTU), a series of thiourea and thiosemicarbazone analogs were prepared and evaluated as inhibitors of melanogenesis in melanoma B16 cells. The most potent analog was 2-(4-tert-butylbenzylidene)hydrazinecarbothioamide (1u) with an IC(50) value of 2.7 mic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thanigaimalai P,Hoang TA,Lee KC,Bang SC,Sharma VK,Yun CY,Roh E,Hwang BY,Kim Y,Jung SH

更新日期：2010-05-01 00:00:00

abstract：:Novel derivatives of the highly potent and selective histamine H3-receptor antagonist ciproxifan (3) with different chain lengths as well as with structural variants of the cyclopropyl ketone moiety have been prepared and screened for their antagonist H3-receptor potencies in vitro and in vivo. Some derivatives (2, 6-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Stark H,Ligneau X,Sadek B,Ganellin CR,Arrang JM,Schwartz JC,Schunack W

更新日期：2000-10-16 00:00:00

abstract：:We have optimized 2-aminomethylphenylamine derivative as a factor Xa inhibitor. Several polar functional groups were introduced in the central phenyl ring, and we focused on zwitter ionic compound showing continuous inhibitory activity in oral administration test. In vitro and oral activities were improved by optimiza...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mochizuki A,Nagata T,Kanno H,Takano D,Kishida M,Suzuki M,Ohta T

更新日期：2011-12-15 00:00:00

abstract：:Dantrolene, the only therapeutic agent for malignant hyperthermia, is known to have not only a muscle relaxant effect, but also a neuroprotective effect and Alzheimer's disease improving effect. Recently, it has been reported that dantrolene has a weak inhibitory effect on acetylcholinesterase (AChE), which is a thera...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aoyama H,Doura T

更新日期：2020-02-15 00:00:00

abstract：:The selective inhibition of coagulation factor Xa has emerged as an attractive strategy for the discovery of novel antithrombotic agents. Here we describe highly potent benzamidine factor Xa inhibitors based on a vicinally-substituted heterocyclic core. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fevig JM,Pinto DJ,Han Q,Quan ML,Pruitt JR,Jacobson IC,Galemmo RA Jr,Wang S,Orwat MJ,Bostrom LL,Knabb RM,Wong PC,Lam PYS,Wexler RR

更新日期：2001-03-12 00:00:00

abstract：:A series of methoxycarbonyl group modified nidulalin A analogs were synthesized to improve stability against esterases. The amide derivatives showed cytotoxic activity along with inhibitory activity against DNA topoisomerase II. Among the analogs, amide 9a exhibited antitumor activity in Colon 26 murine tumor model. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sato S,Suga Y,Yoshimura T,Nakagawa R,Tsuji T,Umemura K,Andoh T

更新日期：1999-09-20 00:00:00

abstract：:Mifepristone is a non-selective antagonist of 3-oxosteroid receptors with both abortifacient and anti-endometriotic activities. Non-steroidal mimetics of mifepristone and progesterone are important templates for modulation of the progesterone receptor (PR). For our PR program, we sought an unexplored, synthetically ac...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jones DG,Liang X,Stewart EL,Noe RA,Kallander LS,Madauss KP,Williams SP,Thompson SK,Gray DW,Hoekstra WJ

更新日期：2005-07-01 00:00:00

abstract：:Elevation of glycine levels and activation of the NMDA receptor by inhibition of the glycine transporter 1 (GlyT-1) is a potential strategy for the treatment of schizophrenia. A novel series of GlyT-1 inhibitors have been identified containing the 2-arylsulfanyl-phenylpiperazine motif. The most prominent member of thi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Smith G,Ruhland T,Mikkelsen G,Andersen K,Christoffersen CT,Alifrangis LH,Mørk A,Wren SP,Harris N,Wyman BM,Brandt G

更新日期：2004-08-02 00:00:00

abstract：:Recently, a disulfide-based cyclic RGD peptide called iRGD, that is, c(CRGDKGPDC), has been reported to interact with both integrin and neuropilin-1 receptors for cellular and deep tissue penetration to improve the imaging sensitivity and therapeutic efficacy. In this study, two new near-infrared fluorescent iRGD conj...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ye Y,Zhu L,Ma Y,Niu G,Chen X

更新日期：2011-02-15 00:00:00