Hepatocellular targeted α-tocopherol based pH sensitive galactosylated lipids: design, synthesis and transfection studies.

abstract：:Recently, there has been an emergence of significant interest in silver-based antimicrobials. Our goal was to develop a radioactive tracer for investigating the biological fate of such compounds. Purified 111Ag was incorporated into the methylated caffeine analogue, IC1 to yield the silver carbene complex designated a...

journal_title：MedChemComm

authors： Aweda TA,Ikotun O,Mastren T,Cannon CL,Wright B,Youngs WJ,Cutler C,Guthrie J,Lapi SE

更新日期：2013-06-01 00:00:00

abstract：:Transcriptomic phenotypes defined for melanoma have been reported to correlate with sensitivity to various drugs. In this study, we aimed to define a minimal signature that could be used to distinguish melanoma sub-types in vitro, and to determine suitable drugs by which these sub-types can be targeted. By using prima...

journal_title：MedChemComm

authors： Senses KM,Ghasemi M,Akbar MW,Isbilen M,Fallacara AL,Frankenburg S,Schenone S,Lotem M,Botta M,Gure AO

更新日期：2017-01-01 00:00:00

abstract：:Tuberculosis is an ever-evolving infectious disease that urgently needs new drugs. In the search for new antituberculosis agents, a library of 3-cinnamoyl-4-hydroxy-6-methyl-2H-pyran-2-ones (CHPs) (2a-2y) was synthesized and evaluated against a standard virulent laboratory strain of Mycobacterium tuberculosis H37Rv. O...

journal_title：MedChemComm

authors： Bhat ZS,Ul Lah H,Rather MA,Maqbool M,Ara T,Ahmad Z,Yousuf SK

更新日期：2017-12-06 00:00:00

abstract：:Human African trypanosomiasis (HAT), also known as African sleeping sickness, is caused by parasitic protozoa of the genus Trypanosoma. As the disease progresses, the parasites cross the blood brain barrier and are lethal for the patients if the disease is left untreated. Current therapies suffer from several drawback...

journal_title：MedChemComm

authors： Berninger M,Schmidt I,Ponte-Sucre A,Holzgrabe U

更新日期：2017-07-31 00:00:00

abstract：:Bruton's tyrosine kinase (BTK) plays a critical role in B cell receptor (BCR)-mediated signaling pathways responsible for the development and function of B cells, which makes it an attractive target for the treatment of many types of B-cell malignancies. Herein, a series of N5-substituted 6,7-dioxo-6,7-dihydropteridin...

journal_title：MedChemComm

authors： Chen H,Song P,Diao Y,Hao Y,Dou D,Wang W,Fang X,Wang Y,Zhao Z,Ding J,Li H,Xie H,Xu Y

更新日期：2018-03-13 00:00:00

abstract：:Malaria is a serious tropical disease that kills thousands of people every year, mainly in Africa, due to Plasmodium falciparum infections. Salirasib is a promising cancer drug candidate that interferes with the post-translational modification of Ras. This S-farnesyl thiosalicylate inhibits isoprenylcysteine carboxyl ...

journal_title：MedChemComm

authors： Porta EOJ,Bofill Verdaguer I,Perez C,Banchio C,Ferreira de Azevedo M,Katzin AM,Labadie GR

更新日期：2019-06-21 00:00:00

abstract：:The dynamic and crucial role of tubulin in different cellular functions rendered it a promising target in anticancer drug development. Combretastatin A-4 (CA-4), an inhibitor of tubulin polymerization isolated from natural sources, is a lead molecule with significant cytotoxicity against tumour cells. Owing to its non...

journal_title：MedChemComm

authors： Seddigi ZS,Malik MS,Saraswati AP,Ahmed SA,Babalghith AO,Lamfon HA,Kamal A

更新日期：2017-07-04 00:00:00

abstract：:Classical aminoglycoside antibiotics are obsolete or hampered by the emergence of drug resistant bacteria. Recent discoveries of antifungal amphiphilic kanamycins offer new strategies for reviving and repurposing these old drugs. A simple structural modification turns the clinically obsolete antibacterial kanamycin in...

journal_title：MedChemComm

authors： Subedi YP,AlFindee MN,Takemoto JY,Chang CT

更新日期：2018-04-17 00:00:00

abstract：:Glutamine and tyrosine-based amino acid conjugates of monocarboxylate transporter types 1 and 2 inhibitors (MCT1/2) were designed, synthesized and evaluated for their potency in blocking the proliferation of a human B lymphoma cell line that expresses the transporters Asct2, LAT1 and MCT1. Appropriate placement of an ...

journal_title：MedChemComm

authors： Nair RN,Mishra JK,Li F,Tortosa M,Yang C,Doherty JR,Cameron M,Cleveland JL,Roush WR,Bannister TD

更新日期：2016-05-01 00:00:00

abstract：:Diabetes mellitus is a chronic, complex and multifactorial disease associated characteristically with hyperglycemia. One of the most recently approved antidiabetic drug classes for clinical use are sodium-glucose cotransporter type 2 (SGLT-2) inhibitors. SGLT-2 is a protein expressed in the kidneys, responsible for gl...

journal_title：MedChemComm

authors： da Silva PN,da Conceição RA,do Couto Maia R,de Castro Barbosa ML

更新日期：2018-06-06 00:00:00

abstract：:It was previously reported that 6β-aminomorphinan derivatives show high affinity for opiate receptors. Novel 6β-heteroarylamidomorphinanes were designed based on the MOR selective antagonist NAP. The 6β-aminomorphinanes were prepared with stereoselective Mitsunobu reaction and subsequently acylated with nicotinic acid...

journal_title：MedChemComm

authors： Urai Á,Váradi A,Szőcs L,Komjáti B,Le Rouzic V,Hunkele A,Pasternak GW,Majumdar S,Hosztafi S

更新日期：2017-01-01 00:00:00

abstract：:The potential for carbon monoxide-releasing molecules (CO-RMs) as antimicrobials represents an exciting prospective in the fight against antibiotic resistance. Trypto-CORM, a tryptophan-containing manganese(i) carbonyl, is toxic against E. coli following photo-activation. Here, we demonstrate that Trypto-CORM is toxic...

journal_title：MedChemComm

authors： Ward JS,Morgan R,Lynam JM,Fairlamb IJS,Moir JWB

更新日期：2016-12-06 00:00:00

abstract：:The phenol of 1-(3-(1H-imidazol-1-yl)propyl)-3-(4-hydroxy-3-methoxyphenyl)thiourea was selectively carbon-11 labelled to generate [11C]PBD150 in 7.3% yield from [11C]methyl triflate (non-decay corrected; radiochemical purity ≥95%, specific activity = 5.7 Ci/µmol, n=5). Evaluation of [11C]PBD150 by small animal PET ima...

journal_title：MedChemComm

authors： Brooks AF,Jackson IM,Shao X,Kropog GW,Sherman P,Quesada CA,Scott PJ

更新日期：2015-06-01 00:00:00

abstract：:Herein, we disclose the development of a catalyst- and protecting-group-free microwave-enhanced Friedländer synthesis which permits the single-step, convergent assembly of diverse 8-hydroxyquinolines with greatly improved reaction yields over traditional oil bath heating (increased from 34% to 72%). This rapid synthes...

journal_title：MedChemComm

authors： Garrison AT,Abouelhassan Y,Yang H,Yousaf HH,Nguyen TJ,Huigens Iii RW

更新日期：2016-07-27 00:00:00

abstract：:We used quantum mechanics/molecular mechanics calculations to test if antimalarial primaquine (PQ) and its derivatives aid the conversion of hemoglobin to methemoglobin by binding to hemoglobin and merely lowering hemoglobin's ionization potential (IP). Our results showed that PQ and its derivatives do not significant...

journal_title：MedChemComm

authors： Liu H,Ding Y,Walker LA,Doerksen RJ

更新日期：2013-08-01 00:00:00

abstract：:In this paper, synthesis and characterization of metal complexes [Cu2(L)3]ClO4 (1), [Ga(L)2]NO3·2H2O (2) and [In(L)2]NO3·H2O (3) (HL = 2-acetylpyridine N(4)-phenylthiosemicarbazone) was carried out, including elemental analysis, spectral analysis (IR, UV-vis, NMR), and X-ray crystallography. Complex 1 contains one S-b...

journal_title：MedChemComm

authors： Wang YT,Fang Y,Zhao M,Li MX,Ji YM,Han QX

更新日期：2017-10-09 00:00:00

abstract：:The cytotoxic drug gemcitabine (GEM) has been conjugated to receptor-binding peptides to target melanoma tumors. A hexapeptide having a Lys-Gly-His-Lys sequence (pep-1), an octapeptide with an Arg-Gly-Asp-Lys-Gly-His-Lys sequence (pep-2), a GEM-conjugated Lys-Gly-His-Lys peptide (GEM-pep-3) and a GEM-conjugated Asp-Gl...

journal_title：MedChemComm

authors： Gaonkar RH,Baishya R,Paul B,Dewanjee S,Ganguly S,Debnath MC,Ganguly S

更新日期：2018-03-06 00:00:00

abstract：:Herein, we present the design and synthesis of a series of novel heterocyclic derivatives of (-)-borneol and (-)-isoborneol as potent inhibitors of the influenza A virus. All compounds were tested for their toxicity against MDCK cells and for virus-inhibiting activity against the influenza virus A/Puerto Rico/8/34 (H1...

journal_title：MedChemComm

authors： Sokolova AS,Yarovaya OI,Semenova MD,Shtro AA,Orshanskaya IR,Zarubaev VV,Salakhutdinov NF

更新日期：2017-03-03 00:00:00

abstract：:The benzisoxazole analogs represent one of the privileged structures in medicinal chemistry and there has been an increasing number of studies on benzisoxazole-containing compounds. The unique benzisoxazole scaffold also exhibits an impressive potential as antimicrobial, anticancer, anti-inflammatory, anti-glycation a...

journal_title：MedChemComm

authors： Rakesh KP,Shantharam CS,Sridhara MB,Manukumar HM,Qin HL

更新日期：2017-10-31 00:00:00

abstract：:A series of 4-thiazolidinone derivatives were synthesized and evaluated as novel human dihydroorotate dehydrogenase (hDHODH) inhibitors. Compounds 26 and 31 displayed IC50 values of 1.75 and 1.12 μM, respectively. The structure-activity relationship was summarized. Further binding mode analysis revealed that compound ...

journal_title：MedChemComm

authors： Zeng F,Qi T,Li C,Li T,Li H,Li S,Zhu L,Xu X

更新日期：2017-04-26 00:00:00

abstract：:A library of 33 compounds was screened for potentiation of the antibiotic FR 900098 against the Francisella tularensis surrogate Francisella novicida. From the screen a highly potent 2-oxazoline adjuvant was discovered capable of potentiating FR 900098 with a 1000-fold reduction in MIC against the Francisella sub-spec...

journal_title：MedChemComm

authors： Stephens MD,Yodsanit N,Melander C

更新日期：2016-01-01 00:00:00

abstract：:Twenty-three monoketone derivatives of curcumin were synthesized to investigate the synergy with fluconazole against fluconazole-resistant Candida spp. The minimal inhibitory concentration (MIC80) and the fractional inhibitory concentration index (FICI) of the antifungal synergist fluconazole were measured against flu...

journal_title：MedChemComm

authors： Zhao F,Dong HH,Wang YH,Wang TY,Yan ZH,Yan F,Zhang DZ,Cao YY,Jin YS

更新日期：2017-03-17 00:00:00

abstract：:Porphyrins are tetrapyrrolic macrocyclic ligands known for their affinity towards neoplastic tissues and once radiolabeled with a suitable diagnostic radioisotope could potentially be used for the imaging of tumorous lesions. In the present study, an unsymmetrically substituted porphyrin derivative namely 5-(p-amino-p...

journal_title：MedChemComm

authors： Guleria M,Das T,Vats K,Amirdhanayagam J,Mathur A,Sarma HD,Dash A

更新日期：2019-02-22 00:00:00

abstract：:A combinatorial library of 6 × 106 cyclic peptides was synthesized in the one bead-two compound format, with each bead displaying a unique cyclic peptide on its surface and a linear peptide encoding tag in its interior. Screening of the library against K-Ras identified compounds that bound K-Ras with submicromolar aff...

journal_title：MedChemComm

authors： Wu X,Upadhyaya P,Villalona-Calero MA,Briesewitz R,Pei D

更新日期：2013-02-01 00:00:00

abstract：:Many reports have suggested that NRP-1 acts as a co-receptor for VEGF-A165 and boosts tumour growth and metastasis. This NRP-1, due to its important role in tumour progression, triggered interest in the design of new molecules able to significantly inhibit NRP-1/VEGF-A165 interaction to suppress pathological angiogene...

journal_title：MedChemComm

authors： Puszko AK,Sosnowski P,Tymecka D,Raynaud F,Hermine O,Lepelletier Y,Misicka A

更新日期：2019-01-25 00:00:00

abstract：:Previous studies on the large-scale glycomics of more than 3500 human serum samples revealed that the serum glycoproteins of cancer patients often have more dominant and specific glycoforms, namely, branched tri- and tetra-antennary N-glycans, most cancer patient groups than normal control groups. We herein establishe...

journal_title：MedChemComm

authors： Yogesh KV,Kamiyama T,Ohyama C,Yoneyama T,Nouso K,Kimura S,Hinou H,Nishimura SI

更新日期：2018-06-29 00:00:00

abstract：:Bile acids have emerged as strong signaling molecules capable of influencing various biological processes like inflammation, apoptosis, cancer progression and atherosclerosis depending on their chemistry. In the present study, we investigated the effect of major hydrophobic bile acids lithocholic acid (LCA) and deoxyc...

journal_title：MedChemComm

authors： Kundu S,Bansal S,Muthukumarasamy KM,Sachidanandan C,Motiani RK,Bajaj A

更新日期：2017-10-31 00:00:00

abstract：:Recognition of nucleosides at adenosine receptors (ARs) is supported by multiple X-ray structures, but the structure of an adenine complex is unknown. We examined the selectivity of predicted A1AR and A3AR adenine antagonists that incorporated known agonist affinity-enhancing N6 and C2 substituents. Adenines with A1AR...

journal_title：MedChemComm

authors： Yu J,Mannes P,Jung YH,Ciancetta A,Bitant A,Lieberman DI,Khaznadar S,Auchampach JA,Gao ZG,Jacobson KA

更新日期：2018-10-18 00:00:00

abstract：:[This corrects the article DOI: 10.1039/C7MD00637C.]. ...

journal_title：MedChemComm

authors： Okombo J,Chibale K

更新日期：2018-03-02 00:00:00

abstract：:A series of cyclic peptides were designed and prepared to investigate the physicochemical properties that affect oral bioavailabilty of this chemotype in rats. In particular, the ionization state of the peptide was examined by the incorporation of naturally occurring amino acid residues that are charged in differing r...

journal_title：MedChemComm

authors： Rand AC,Leung SS,Eng H,Rotter CJ,Sharma R,Kalgutkar AS,Zhang Y,Varma MV,Farley KA,Khunte B,Limberakis C,Price DA,Liras S,Mathiowetz AM,Jacobson MP,Lokey RS

更新日期：2012-10-01 00:00:00