Design, synthesis and bioactivity investigation of tetrandrine derivatives as potential anti-cancer agents.

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：:Zampanolide and dactylolide are microtubule-stabilizing polyketides possessing potent cytotoxicity towards a variety of cancer cell lines. Using our understanding of the conformational preferences of the macrolide core in both natural products, we hypothesized that analogues lacking the C17-methyl group would maintain...

journal_title：MedChemComm

authors： Henry JL,Wilson MR,Mulligan MP,Quinn TR,Sackett DL,Taylor RE

更新日期：2019-04-09 00:00:00

abstract：:A series of N-alkyl tethered C-5 functionalized bis-isatins were synthesized and evaluated for antimicrobial activity against pathogenic microorganisms. The preliminary evaluation studies revealed the compound 4t, with an optimal combination of bromo-substituent at the C-5 position of isatin ring along with propyl cha...

journal_title：MedChemComm

authors： Singh A,Nisha,Bains T,Hahn HJ,Liu N,Tam C,Cheng LW,Kim J,Debnath A,Land KM,Kumar V

更新日期：2017-01-01 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：: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：:A novel and simplified synthetic scaffold based on pladienolide was designed using a consensus pharmacophore hypothesis. An initial target was synthesized and evaluated to examine the role of the 3-hydroxy group and the methyl groups present at positions 10, 16, 20, 22 in 1, on biological activity. We report the first...

journal_title：MedChemComm

authors： Gundluru MK,Pourpak A,Cui X,Morris SW,Webb TR

更新日期：2011-01-01 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：:N-Acylethanolamine acid amidase (NAAA) is one of the key enzymes involved in the degradation of fatty acid ethanolamides (FAEs), especially for palmitoylethanolamide (PEA). Pharmacological blockage of NAAA restores PEA levels, providing therapeutic benefits in the management of inflammation and pain. In the current wo...

journal_title：MedChemComm

authors： Zhou P,Xiang L,Zhao D,Ren J,Qiu Y,Li Y

更新日期：2018-12-18 00:00:00

abstract：:The benzophenone scaffold represents a ubiquitous structure in medicinal chemistry because it is found in several naturally occurring molecules which exhibit a variety of biological activities, such as anticancer, anti-inflammatory, antimicrobial, and antiviral. In addition, various synthetic benzophenone motifs are p...

journal_title：MedChemComm

authors： Surana K,Chaudhary B,Diwaker M,Sharma S

更新日期：2018-08-23 00:00:00

abstract：:β-Carbolines have been assessed for osteoclastogenesis. However, their effect on osteoblasts during estrogen deficiency is still unclear. Here, a series of novel piperazine and tetrazole tag β-carbolines have been synthesized and examined for osteoblast differentiation in vitro. In vitro data suggest that compound 8g ...

journal_title：MedChemComm

authors： Karvande A,Khan S,Khan I,Singh D,Khedgikar V,Kushwaha P,Ahmad N,Kothari P,Dhasmana A,Kant R,Trivedi R,Chauhan PMS

更新日期：2018-06-12 00:00:00

abstract：:Novel primaquine-cell penetrating peptide conjugates were synthesised and tested in vitro against liver stage Plasmodium berghei parasites. Generally, the conjugates were more active than the parent peptides and, in some cases, than the parent drug. These are unprecedented findings that may open a new route towards an...

journal_title：MedChemComm

authors： Aguiar L,Machado M,Sanches-Vaz M,Prudêncio M,Vale N,Gomes P

更新日期：2018-11-16 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：:Two diazabicyclo analogues of maraviroc, in which the azabicyclooctane moiety is replaced by diazabicyclooctane or diazabicyclononane, were synthesized and tested, through a viral neutralization assay, on a panel of six pseudoviruses. The diazabicyclooctane derivative maintained a significant infectivity reduction pow...

journal_title：MedChemComm

authors： Legnani L,Colombo D,Venuti A,Pastori C,Lopalco L,Toma L,Mori M,Grazioso G,Villa S

更新日期：2016-12-16 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：:We previously reported that troponoid compounds profoundly inhibit replication of herpes simplex virus (HSV)-1 and HSV-2 in cell culture, including acyclovir-resistant mutants. Synthesis of 26 alpha-hydroxylated tropolones (αHTs) led to a preliminary structure-activity relationship highlighting the potency of bi-pheny...

journal_title：MedChemComm

authors： Berkowitz AJ,Franson AD,Gazquez Cassals A,Donald KA,Yu AJ,Garimallaprabhakaran AK,Morrison LA,Murelli RP

更新日期：2019-05-30 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：:Covalent probes and drugs have found widespread use as research tools and clinical agents. Covalent probes are useful because of their increased intracellular potency and because covalent labeling of cellular proteins can be tracked using click chemistry. Covalent drugs, on the other hand, can overcome drug resistance...

journal_title：MedChemComm

authors： Kathman SG,Statsyuk AV

更新日期：2016-04-01 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：:The type III secretion system injectisome is a syringe-like multimembrane spanning nanomachine that is essential to the pathogenicity but not viability of many clinically relevant Gram-negative bacteria, such as enteropathogenic Escherichia coli, Salmonella enterica and Pseudomonas aeruginosa. Due to the rise in antib...

journal_title：MedChemComm

authors： Lyons BJE,Strynadka NCJ

更新日期：2019-06-20 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：:Fungal infections directly affect millions of people each year. In addition to the invasive fungal infections of humans, the plants and animals that comprise our primary food source are also susceptible to diseases caused by these eukaryotic microbes. The need for antifungals, not only for our medical needs, but also ...

journal_title：MedChemComm

authors： Ngo HX,Garneau-Tsodikova S,Green KD

更新日期：2016-07-01 00:00:00

abstract：:In this review, we have focused on the recent progress in metal complexes that are able to bind to β-amyloid (Aβ) species. We have discussed various radioactive complexes of 99mTc, 68Ga, 64Cu, 89Zr, and 111In, which were designed as Aβ imaging agents for positron emission tomography (PET) and single photon emission co...

journal_title：MedChemComm

authors： Chen K,Cui M

更新日期：2017-05-16 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：: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：: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：: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：:Intrinsic and acquired resistance to conventional and targeted therapeutics is a fundamental reason for treatment failure in many cancer patients. Targeted approaches to overcome chemoresistance as well as resistance to targeted approaches require in depth understanding of the underlying molecular mechanisms. The anti...

journal_title：MedChemComm

authors： Ferreira BI,Lie MK,Engelsen AST,Machado S,Link W,Lorens JB

更新日期：2016-10-21 00:00:00

abstract：:The dopamine D3 receptor (D3R) is a proven therapeutic target for the treatment of neurological and neuropsychiatric disorders. In particular, D3R-selective ligands that can eliminate side effects associated with dopamine D2 receptor (D2R) therapeutics have been validated. However, the high homology in signaling pathw...

journal_title：MedChemComm

authors： Cao Y,Sun N,Zhang J,Liu Z,Tang YZ,Wu Z,Kim KM,Cheon SH

更新日期：2018-06-14 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：:Periodontal disease is an oral chronic immune-inflammatory disease highly prevalent worldwide that is initiated by specific oral bacterial species leading to local and systemic effects. The development of new preventive/therapeutic strategies to specifically target oral periodontopathogens without perturbing oral micr...

journal_title：MedChemComm

authors： Thamban Chandrika N,Fosso MY,Alimova Y,May A,Gonzalez OA,Garneau-Tsodikova S

更新日期：2019-06-10 00:00:00