Pyrrolo[3,2,1-ij]quinoline derivatives, a 5-HT2c receptor agonist with selectivity over the 5-HT2a receptor: potential therapeutic applications for epilepsy and obesity.

abstract：:We report a dimerization strategy to enhance the antibacterial potency of an otherwise weak cationic amphiphilic polyproline helical (CAPH) peptide. Overall, the dimeric CAPHs were more active against Escherichia coli and Staphylococcus aureus than the monomeric counterpart, reaching up to a 60-fold increase in potenc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hernandez-Gordillo V,Geisler I,Chmielewski J

更新日期：2014-01-15 00:00:00

abstract：:Pd(II), Cu(II) and Zn(II) complexes (1-3) based on 4'-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-2,2':6',2″-terpyridine were synthesized and characterized by UV, IR, NMR, EPR, HRMS, elemental analyses, and molar conductivity measurements. The cytotoxicity of these complexes against HL-60, BGC-823, KB, Bel-7402, A549, Hela, ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chu W,Wang Y,Liu S,Yang X,Wang S,Li S,Zhou G,Qin X,Zhou C,Zhang J

更新日期：2013-09-15 00:00:00

abstract：:A series of 3-chloro-4-substituted-1-(8-hydroxy-quinolin-5-yl)-azetidin-2-ones were synthesized and evaluated for their in vitro anti-filarial activity. To pre-assess the anti-filarial behavior of synthesized compounds (V(a-f)) on a structural basis, automated docking studies were carried out with Molecular Design Sui...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chhajed SS,Manisha P,Bastikar VA,Animeshchandra H,Ingle VN,Upasani CD,Wazalwar SS

更新日期：2010-06-15 00:00:00

abstract：:Sustained proliferative capacity and gene dysregulation are hallmarks of cancer. In mammalian cells, cyclin-dependent kinases (CDKs) control critical cell cycle checkpoints and key transcriptional events in response to extracellular and intracellular signals leading to proliferation. Significant clinical activity for ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sánchez-Martínez C,Lallena MJ,Sanfeliciano SG,de Dios A

更新日期：2019-10-15 00:00:00

abstract：:Tuberculosis (TB) continues to remain one of the most threatening diseases in the world. With the emergence of multi-drug resistant (MDR) and extensively drug resistant (XDR) strains, the need to develop new therapies is dire. The syntheses of a focused library of hydroxamates and hydroxamic acids is described, as wel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Majewski MW,Cho S,Miller PA,Franzblau SG,Miller MJ

更新日期：2015-11-01 00:00:00

abstract：:Human pancreatic cancer is resistant to almost all conventional chemotherapeutic agents. It is known to proliferate aggressively within hypovascular tumor microenvironment by exhibiting remarkable tolerance to nutrition starvation,  a phenomenon termed as "austerity". Search for the new agents that eliminate the toler...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tawila AM,Sun S,Kim MJ,Omar AM,Dibwe DF,Ueda JY,Toyooka N,Awale S

更新日期：2020-08-15 00:00:00

abstract：:Synthesis and characterization of an inert perchlorotriphenylmethyl triester radical, PTM-TE, are reported. PTM-TE was prepared by a facile 3-step synthesis using Friedel-Crafts reaction of tetrachlorobenzene with chloroform followed by ethoxycarbonylation and subsequent oxidation. PTM-TE is paramagnetic and exhibits ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dang V,Wang J,Feng S,Buron C,Villamena FA,Wang PG,Kuppusamy P

更新日期：2007-07-15 00:00:00

abstract：:HIV integrase catalyzes the integration of HIV DNA copy into the host cell DNA, which is essential for the production of progeny viruses. L-Chicoric acid and dicaffeoylquinic acids, isolated from plants, are well known potent inhibitors of HIV integrase. The common structural features of these inhibitors are caffeic a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee JY,Yoon KJ,Lee YS

更新日期：2003-12-15 00:00:00

abstract：:A scaffold hopping strategy was successfully applied in discovering 2-aminooxazole amides as potent DGAT1 inhibitors for the treatment of dyslipidemia. Further optimization in potency and PK properties resulted in a lead series with oral in vivo efficacy in a mouse postprandial triglyceridemia (PPTG) assay. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim HM,Smith MD,Kim JH,Caplen MA,Chan TY,McKittrick BA,Cook JA,van Heek M,Lachowicz J

更新日期：2013-12-01 00:00:00

abstract：:Eight hydroxyl-substituted Schiff bases with the different number and position of hydroxyl group on the two asymmetric aromatic rings (A and B rings) were prepared by the reaction between the corresponding aromatic aldehyde and aniline. Their antioxidant effects against the stable galvinoxyl radical (GO(.)) in ethyl a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cheng LX,Tang JJ,Luo H,Jin XL,Dai F,Yang J,Qian YP,Li XZ,Zhou B

更新日期：2010-04-15 00:00:00

abstract：:By means of functional interconversions in ring D of the tetracyclic diterpene isosteviol (ent-16-ketobeyeran-19-oic acid 1), various 15- and 16-substituted isosteviol derivatives were stereoselectively prepared. The cytotoxic activities in vitro of these new isosteviol derivatives were investigated, and some of them ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wu Y,Dai GF,Yang JH,Zhang YX,Zhu Y,Tao JC

更新日期：2009-03-15 00:00:00

abstract：:Carbonic anhydrase inhibitors AZA, EZA, and 4-acetamidobenzsulfonamide were found to inhibit human AQP4-M23 mediated water transport by 80%, 68%, and 23%, respectively, at 20 microM in an in vitro functional assay. AZA was found to have an IC50 against AQP4 of 0.9 microM. Phloretin was inactive under the same conditio...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huber VJ,Tsujita M,Yamazaki M,Sakimura K,Nakada T

更新日期：2007-03-01 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：:The enzymatic synthesis of Gal-beta 1,3[GlcNAc-beta 1,6]-GalNAc-alpha 1-OBn (core 2-Bn) using a multi-enzyme system consisting of a beta-galactosidase (EC 3.2.1.23) from bovine testes and a recombinant core 2 beta 1,6-GlcNAc transferase (C2GnT, EC 2.4.1.102) was empirically optimized by the use of a genetic algorithm....

journal_title：Bioorganic & medicinal chemistry letters

authors： Hoh C,Dudziak G,Liese A

更新日期：2002-04-08 00:00:00

abstract：:A series of diaryl ureas with an amide substitution at the 4-position was prepared and found to be potent and selective FLT3 inhibitors with good oral bioavailability and efficacy in a tumor xenograft model. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patel HK,Grotzfeld RM,Lai AG,Mehta SA,Milanov ZV,Chao Q,Sprankle KG,Carter TA,Velasco AM,Fabian MA,James J,Treiber DK,Lockhart DJ,Zarrinkar PP,Bhagwat SS

更新日期：2009-09-01 00:00:00

abstract：:Substituted dihydroquinozalin-2-ones (1-16) have been synthesized easily by the use of copper-catalyzed coupling method. The reactions of 2-haloanilines with a variety of alpha-amino acids in the presence of copper (I) iodide gave corresponding 3-substituted dihydroquinozalin-2-ones in up to 86% yield. Some new quinox...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tanimori S,Nishimura T,Kirihata M

更新日期：2009-08-01 00:00:00

abstract：:Tylophorine B exhibits pronounced cytotoxicity and antitumor activity. In order to survey the structure selectivity to DNA afforded by tylophorine B, we have synthesized a variety of duplex, bulge- and hairpin-containing oligodeoxyribonucleotides. Their binding to tylophorine B has been assayed by fluorescence spectro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xi Z,Zhang R,Yu Z,Ouyang D,Huang R

更新日期：2005-05-16 00:00:00

abstract：:Using molecular modeling and rationally designed structural modifications, the multi-target structure-activity relationship for a series of ranitidine analogs has been investigated. Incorporation of a variety of isosteric groups indicated that appropriate aromatic moieties provide optimal interactions with the hydroph...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gao J,Midde N,Zhu J,Terry AV,McInnes C,Chapman JM

更新日期：2016-11-15 00:00:00

abstract：:Developing targeted validation probes that can interrogate biology is of interest for both chemists and biologists. The synthesis of suitable compounds provides a means for avoiding the costly labeling of cells with specific antibodies and the bias associated with the interpretation of biological validation experiment...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ho LA,Thomas E,McLaughlin RA,Flematti GR,Fuller RO

更新日期：2016-10-15 00:00:00

abstract：:A class of small molecules displaying comparable activities with peptide ligands BAM22 and corticostatin-14 at both the human and rhesus monkey MrgX1 and MrgX2 receptors, respectively, was discovered. A comparative study to compare solid-phase and solution-phase chemistries for the efficient synthesis of the active cl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Malik L,Kelly NM,Ma JN,Currier EA,Burstein ES,Olsson R

更新日期：2009-03-15 00:00:00

abstract：:EZH2 is the core subunit of Polycomb repressive complex 2 catalyzing the methylation of histone H3 lysine-27 and closely involved in tumorigenesis. To discover small molecule inhibitors for EZH2 methyltransferase activity, we performed an inhibitor screen with catalytically active EZH2 protein complex and identified t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Woo J,Kim HY,Byun BJ,Chae CH,Lee JY,Ryu SY,Park WK,Cho H,Choi G

更新日期：2014-06-01 00:00:00

abstract：:Brønsted acid-induced fragmentation of a triazoline is used as a tool to identify Brønsted base additives capable of playing the role of a proton shuttle. Relative to water, dimethyl formamide accelerates proton transfer substantially under these conditions. A series of alcohols and ethers were also used to demonstrat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Donahue MG,Hong KB,Johnston JN

更新日期：2009-09-01 00:00:00

abstract：:Novel 8-aryl and 8-aroyl substituted derivatives of 3-(dipropylamino)chroman are described. The compounds have been prepared by a palladium catalyzed reaction of iodoarenes and a stannylated derivative of [eta6-3-(dipropylamino)chroman]Cr(CO)3. Several of the compounds have high affinity for 5-HT1A receptors whereas t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Caldirola P,Chowdhury R,Unelius L,Mohell N,Hacksell U,Johansson AM

更新日期：1999-06-07 00:00:00

abstract：:We describe the synthesis and potency of a novel series of N-substituted 2-phenyl- and 2-methyl-2-phenyl-1,4-diaminobutane- based CCR5 antagonists. Compounds 7a and 12f were found to be potent in anti-HIV assays and bioavailable in the low-dose rat PK model. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tallant MD,Duan M,Freeman GA,Ferris RG,Edelstein MP,Kazmierski WM,Wheelan PJ

更新日期：2011-03-01 00:00:00

abstract：:We report the discovery and structure-activity relationship of 2,6-disubstituted pyrazines, which are potent and selective CK2 inhibitors. Lead compound 1 was identified, and derivatives were prepared to develop potent inhibitory activity. As a result, we obtained compound 7, which was the smallest unit that retained ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fuchi N,Iura Y,Kaneko H,Nitta A,Suyama K,Ueda H,Yamaguchi S,Nishimura K,Fujii S,Sekiya Y,Yamada M,Takahashi T

更新日期：2012-07-01 00:00:00

abstract：:A set of 15mer linear oligoDNA probes bearing a modified nucleoside conjugated with a polyamine/fluorescein/anthraquinone reporting moiety were synthesized. In a single-stranded form, the fluorescence generated by the excitation of fluorescein was efficiently quenched, while marked recovery of the fluorescence was obs...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kodama S,Asano S,Moriguchi T,Sawai H,Shinozuka K

更新日期：2006-05-15 00:00:00

abstract：:Inhibition of intestinal brush border DMT1 offers a novel therapeutic approach to the prevention and treatment of disorders of iron overload. Several series of diaryl and tricyclic benzylisothiourea compounds as novel and potent DMT1 inhibitors were discovered from the original hit compound 1. These compounds demonstr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang Z,Kodumuru V,Sviridov S,Liu S,Chafeev M,Chowdhury S,Chakka N,Sun J,Gauthier SJ,Mattice M,Ratkay LG,Kwan R,Thompson J,Cutts AB,Fu J,Kamboj R,Goldberg YP,Cadieux JA

更新日期：2012-08-01 00:00:00

abstract：:Using structure-based optimization procedures on in silico hits, dibenzosuberyl- and benzoate substituted tropines were designed as ligands for acetylcholine-binding protein (AChBP). This protein is a homolog to the ligand binding domain of the nicotinic acetylcholine receptor (nAChR). Distinct SAR is observed between...

journal_title：Bioorganic & medicinal chemistry letters

authors： Edink E,Akdemir A,Jansen C,van Elk R,Zuiderveld O,de Kanter FJ,van Muijlwijk-Koezen JE,Smit AB,Leurs R,de Esch IJ

更新日期：2012-02-01 00:00:00

abstract：:Vismodegib is the first FDA approved cancer therapy based on inhibition of aberrant hedgehog signaling. Like most cancer therapies, vismodegib suffered from resistance, even during clinical development. Numerous reports demonstrated that simultaneous blockage of hedgehog and PI3K/AKT/mTOR pathways resulted in signific...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang Z,Ma H,Sun Z,Luo L,Tian S,Zheng J,Zhang X

更新日期：2015-09-01 00:00:00

abstract：:A series of 3-substituted benzamide derivatives structurally related to STI-571 (imatinib mesylate), a Bcr-Abl tyrosine kinase inhibitor used to treat chronic myeloid leukemia (CML), was prepared and evaluated for antiproliferative activity against the Bcr-Abl-positive leukemia cell line K562. About ten 3-halogenated ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Asaki T,Sugiyama Y,Hamamoto T,Higashioka M,Umehara M,Naito H,Niwa T

更新日期：2006-03-01 00:00:00