⁹⁹mTc-(Me)FGCDEVD, a potential tracer for apoptosis detection.

abstract：:A selection of 76 nitroheterocycles and related compounds from our in-house compound library was screened in vitro against the parasite Trypanosoma brucei rhodesiense, causative agent of human African trypanosomiasis (HAT). The unspecific cytotoxicity of the compounds was also evaluated against rat myoblast L6-cells t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Arán VJ,Kaiser M,Dardonville C

更新日期：2012-07-15 00:00:00

abstract：:Compound 2 was previously identified as a potent inhibitor of factor XIa lacking oral bioavailability. A structure-based approach was used to design analogs of 2 with novel P1 moieties with good selectivity profiles and oral bioavailability. Further optimization of the P1 group led to the identification of a 4-chlorop...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pinto DJ,Smallheer JM,Corte JR,Austin EJ,Wang C,Fang T,Smith LM 2nd,Rossi KA,Rendina AR,Bozarth JM,Zhang G,Wei A,Ramamurthy V,Sheriff S,Myers JE Jr,Morin PE,Luettgen JM,Seiffert DA,Quan ML,Wexler RR

更新日期：2015-04-01 00:00:00

abstract：:A series of N-phenylnicotinamides (1-40) were designed and evaluated in vitro for their COX inhibitory activities. Most of the synthesized compounds were proved to be potent and selective inhibitors of COX-1. Compound 28 showed the most potent COX-1 inhibitory activity (COX-1 IC(50) = 0.68 ± 0.07 μM) and good selectiv...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shi L,Li ZL,Yang Y,Zhu ZW,Zhu HL

更新日期：2011-01-01 00:00:00

abstract：:A new family of poly-guanidinium species with a benzene core as the organising agent has been developed. Their antibacterial properties have been evaluated against reference Gram positive and Gram negative bacteria, and their cytotoxicity against eukaryotic cells. Most of these compounds exhibited Minimum Inhibitory C...

journal_title：Bioorganic & medicinal chemistry letters

authors： Massimba Dibama H,Mourer M,Duval RE,Regnouf-de-Vains JB

更新日期：2014-10-15 00:00:00

abstract：:Microsomal prostaglandin E(2) synthase-1 (mPGES-1) is a novel therapeutic target for the treatment of inflammation and pain. In the preceding letter, we detailed the discovery of clinical candidate PF-04693627, a potent mPGES-1 inhibitor possessing a novel benzoxazole structure. While PF-04693627 was undergoing furthe...

journal_title：Bioorganic & medicinal chemistry letters

authors： Walker DP,Arhancet GB,Lu HF,Heasley SE,Metz S,Kablaoui NM,Franco FM,Hanau CE,Scholten JA,Springer JR,Fobian YM,Carter JS,Xing L,Yang S,Shaffer AF,Jerome GM,Baratta MT,Moore WM,Vazquez ML

更新日期：2013-02-15 00:00:00

abstract：:An asymmetric synthesis of alpha-amino acids with novel beta-branched side chains has been implemented. The syntheses feature a p-toluenesulfinylimine induced chiral Strecker approach and were found to be applicable to the introduction of both aliphatic and aromatic beta-branched sidechains for preparation of previous...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang M,Porte A,Diamantidis G,Sogi K,Kubrak D,Resnick L,Mayer SC,Wang Z,Kreft AF,Harrison BL

更新日期：2007-05-01 00:00:00

abstract：:PIM1 is a proto-oncogene encoding the serine/threonine PIM1 kinase. PIM1 kinase plays important roles in regulating aspects of cell cycle progression, apoptosis resistance, and has been implicated in the development of such malignancies as prostate cancer and acute myeloid leukemia among others. Knockout of PIM1 kinas...

journal_title：Bioorganic & medicinal chemistry letters

authors： Schroeder RL,Goyal N,Bratton M,Townley I,Pham NA,Tram P,Stone T,Geathers J,Nguyen K,Sridhar J

更新日期：2016-07-01 00:00:00

abstract：:A novel caspase-3 substrate N-Ac-DEVD-N'-MC-R110, which is a fluorogenic substrate cleavable in a single step, has been prepared. It has a significantly higher enzyme turnover rate and sensitivity for detecting caspase-3 activity both in solution and living cells than existing fluorogenic substrates. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang ZQ,Liao J,Diwu Z

更新日期：2005-05-02 00:00:00

abstract：:Peptide-based alpha-ketoamides, alpha-ketoesters and alpha-diketones were designed, synthesized and evaluated against HCV NS3 protease. Alpha-ketoamides have the highest affinity among the three classes, with 8 being the most potent inhibitor with an IC50 of 340 nM. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Han W,Hu Z,Jiang X,Decicco CP

更新日期：2000-04-17 00:00:00

abstract：:A series of 5-aminomethylquinoxaline-2,3-diones have been identified as potent and selective AMPA antagonists. Some of these compounds are also active at the glycine-binding site of the NMDA receptors. A number of these novel, water-soluble quinoxaline-2,3-dione derivatives display protective effects in the electrosho...

journal_title：Bioorganic & medicinal chemistry letters

authors： Auberson YP,Bischoff S,Moretti R,Schmutz M,Veenstra SJ

更新日期：1998-01-06 00:00:00

abstract：:The protein-tyrosine phosphatase (PTP) 'YopH' is a virulence factor of Yersinia pestis, the causative agent of plague. Potential use of Yersinia as a bioterrorism agent renders YopH inhibitors of therapeutic importance. Previously, we had examined the inhibitory potencies of a variety of phosphotyrosyl (pTyr) mimetics...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee K,Gao Y,Yao ZJ,Phan J,Wu L,Liang J,Waugh DS,Zhang ZY,Burke TR Jr

更新日期：2003-08-04 00:00:00

abstract：:A novel series of 1,2,3-thiadiazole thioacetanilide (TTA) derivatives have been designed, synthesized and evaluated for its anti-HIV activities in MT-4 cells. Some derivatives proved to be highly effective in inhibiting HIV-1 replication at nanomolar concentrations. Among them, 2-[4-(2,4-dichlorophenyl)-1,2,3-thiadiaz...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhan P,Liu X,Cao Y,Wang Y,Pannecouque C,De Clercq E

更新日期：2008-10-15 00:00:00

abstract：:A phytochemical investigation on crude extract of Gentianella azurea led to the isolation of ten new (1-10) and one known (11) secoiridoid glycosides. Their structures were unambiguously elucidated by analysis of 1D and 2D NMR. Compounds 2, 5 and 11 were found to inhibit nitric oxide (NO) production in RAW 264.7 macro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang YJ,Lu H,Yu XL,Song WB,Zhang SW,Fen LY,Xuan LJ

更新日期：2014-11-15 00:00:00

abstract：:A series of carboxamide derivatives of 5'-amino-2',5'-dideoxy-5-ethyluridine has been prepared as inhibitors of HSV-TK (herpes simplex virus thymidine kinase). The most potent compounds were derived from xanthene, thioxanthene and dihydroanthracene carboxylic acids. The lead compounds show subnanomolar IC(50) values a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Martin JA,Lambert RW,Merrett JH,Parkes KE,Thomas GJ,Baker SJ,Bushnell DJ,Cansfield JE,Dunsdon SJ,Freeman AC,Hopkins RA,Johns IR,Keech E,Simmonite H,Walmsley A,Wong Kai-In P,Holland M

更新日期：2001-07-09 00:00:00

abstract：:DNA G-quadruplex is an attractive drug target for anticancer therapy. Most G-quadruplex ligands have little selectivity, due to π-stacking interaction with common G-tetrads surface. Thanks to the varieties of G-quadruplex grooves, the groove-binding ligand is expected to create high selectivity. Therefore, developing ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li J,Jin X,Hu L,Wang J,Su Z

更新日期：2011-12-01 00:00:00

abstract：:We designed and synthesized an estrogen receptor (ER) down-regulator (5), which is a derivative of tamoxifen with a long alkyl side chain. Compound 5 effectively reduced ER protein levels in MCF-7 cells and had an antagonistic effect. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shoda T,Okuhira K,Kato M,Demizu Y,Inoue H,Naito M,Kurihara M

更新日期：2014-01-01 00:00:00

abstract：:Antagonists of the TRPV4 receptor were identified using a focused screen, followed by a limited optimization program. The leading compounds obtained from this exercise, RN-1665 23 and RN-9893 26, showed moderate oral bioavailability when dosed to rats. The lead molecule, RN-9893 26, inhibited human, rat and murine var...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wei ZL,Nguyen MT,O'Mahony DJ,Acevedo A,Zipfel S,Zhang Q,Liu L,Dourado M,Chi C,Yip V,DeFalco J,Gustafson A,Emerling DE,Kelly MG,Kincaid J,Vincent F,Duncton MA

更新日期：2015-09-15 00:00:00

abstract：:Three groups of non-camptothecin compounds with four to five fused rings have been designed and synthesized. Their in vitro anti-proliferative activity has been evaluated with five different cancer cell lines (HCT116, PC3, U87MG, HepG2, SK-OV-3). Compounds B-2 and B-3 showed the most potent cell growth inhibition with...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang C,Li S,Ji L,Liu S,Li Z,Li S,Meng X

更新日期：2015-10-15 00:00:00

abstract：:New cis-fused tetrahydrochromeno[4,3-b]quinolines have been synthesized by intramolecular [4+2] imino-Diels-Alder reactions of 2-azadienes derived in situ from aromatic amines and 7-O-prenyl derivatives of 8-formyl-2,3-disubstituted chromenones in the presence of 20mol% Yb(OTf)(3) in acetonitrile under reflux conditio...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nagaiah K,Venkatesham A,Srinivasa Rao R,Saddanapu V,Yadav JS,Basha SJ,Sarma AV,Sridhar B,Addlagatta A

更新日期：2010-06-01 00:00:00

abstract：:A series of 3-aryl-2-propenoates including cinnamates, (E)-methyl/ethyl 3-[2-(1,4-dimethoxy-5,8-dione)naphthalenyl]-2-propenoates (8ba, 8bb) and (E)-methyl/ethyl 3-[2-(1,4-dihydroxy-9,10-dione)anthracenyl]-2-propenoates (9aa,9ab) was synthesized and evaluated for antitumor cytotoxicity. It was found that the ortho- or...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nam NH,You YJ,Kim Y,Hong DH,Kim HM,Ahn BZ

更新日期：2001-05-07 00:00:00

abstract：:Polymyxin B (1) monohydrochloride was converted to the tetra-BOC derivatives 1b and 1c by reaction with di-tert-butyl dicarbonate. The structures of these protected intermediates were established utilizing a degradative sequence that afforded 3 and 5. A method for the deprotection 2,4-dinitrophenylamines to the free a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Weinstein J,Afonso A,Moss E Jr,Miller GH

更新日期：1998-12-01 00:00:00

abstract：:Synthesis and structure-activity relationships (SAR) of a novel series of vasopressin V(1b) (V(3)) antagonists are described. 2-(4-Oxo-2-aryl-quinazolin-3(4H)-yl)acetamides have been identified with low nanomolar affinity for the V(1b) receptor and good selectivity with respect to related receptors V(1a), V(2) and oxy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Napier SE,Letourneau JJ,Ansari N,Auld DS,Baker J,Best S,Campbell-Wan L,Chan JH,Craighead M,Desai H,Goan KA,Ho KK,Hulskotte EG,MacSweeney CP,Milne R,Morphy JR,Neagu I,Ohlmeyer MH,Peeters AW,Presland J,Riviello C,

更新日期：2011-03-15 00:00:00

abstract：:Herein, we report the design and synthesis of the novel 12-membered non-antibiotic macrolide (8R,9S)-8,9-dihydro-6,9-epoxy-8,9-anhydropseudoerythromycin A (EM900), which was found to be a potent anti-inflammatory and/or immunomodulatory agent, capable of promoting monocyte to macrophage differentiation. This molecule ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sugawara A,Sueki A,Hirose T,Nagai K,Gouda H,Hirono S,Shima H,Akagawa KS,Omura S,Sunazuka T

更新日期：2011-06-01 00:00:00

abstract：:The synthesis of N-(O,O-diisopropylphosphoryl)-benzyltetrahydroisoquinoline (3) has been achieved in a 'one pot' procedure from imine (2) and diisopropyl-phosphorochloridate (1) generated in situ (POCl3 + iPrOH). Compound 3 is the first benzyltetrahydroisoquinoline derivative found to be a potent inhibitor of mitochon...

journal_title：Bioorganic & medicinal chemistry letters

authors： Andreu I,Cabedo N,Tormo JR,Bermejo A,Mello R,Cortes D

更新日期：2000-07-03 00:00:00

abstract：:The design, synthesis, and IMPDH inhibitory activity of a series of phosphonic acid-containing analogues of mycophenolic acid are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Watkins WJ,Chen JM,Cho A,Chong L,Collins N,Fardis M,Huang W,Hung M,Kirschberg T,Lee WA,Liu X,Thomas W,Xu J,Zeynalzadegan A,Zhang J

更新日期：2006-07-01 00:00:00

abstract：:The convergent synthesis of C35-fluorinated analogues of solamin, a mono-THF Annonaceous acetogenin, has been achieved by the Sonogashira coupling of the THF ring fragment and the fluorinated γ-lactone fragment. It was revealed that the number of fluorine atoms on the γ-lactone moiety affects the growth inhibitory act...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kojima N,Suga Y,Hayashi H,Yamori T,Yoshimitsu T,Tanaka T

更新日期：2011-10-01 00:00:00

abstract：:Pyrazolopyrimidines were discovered as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A. In addition to its intrinsic activity, compound 9n significantly enhances nicotinic acid binding to the receptor, thereby potentiating the functional efficacy of nicotinic acid. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shen HC,Taggart AK,Wilsie LC,Waters MG,Hammond ML,Tata JR,Colletti SL

更新日期：2008-09-15 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：:The mechanism of edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one) to scavenge DPPH radical is clarified by density functional theory (DFT) calculations. It is revealed that H-atom-abstraction rather than electron-transfer reaction is involved in the radical-scavenging process of edaravone, and H-atom at position 4 is r...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang LF,Zhang HY

更新日期：2003-11-03 00:00:00

abstract：:We demonstrated an intriguing method to discriminate adenine by incident appearance of an intense new emission via exciplex formation in hybridization of target DNA with newly designed fluorescent 8-arylethynylated deoxyguanosine derivatives. We described the synthesis of such highly electron donating fluorescent guan...

journal_title：Bioorganic & medicinal chemistry letters

authors： Saito Y,Kugenuma K,Tanaka M,Suzuki A,Saito I

更新日期：2012-06-01 00:00:00