解剖学和形态学
麻醉学
听力与言语-语言病理学
行为科学
心脏和心血管系统
细胞和组织工程学
临床神经病学
危重症监护医学
牙科,口腔外科和医学
皮肤病学
急诊医学
内分泌学和新陈代谢
肠胃学和肝脏学
老人病学和老年医学
卫生保健科学和服务
血液学
免疫学
传染病
综合和补充性医学
医学伦理学
医学信息学
医学实验室技术
医学,全科和内科
医学,法律
医学,研究和试验
神经系统科学
护理
营养学和饮食学
产科医学和妇科医学
肿瘤学
眼科学
整形外科学
耳鼻喉科学
病理学
儿科学
周围血管疾病
药理学和药剂学
生理学
基本医疗保健
精神病学
公共、环境和职业卫生
放射学,核医学和医学成像
康复学
生殖生物学
呼吸系统
风湿病学
运动科学
外科学
毒理学
热带医学
泌尿学和肾脏学
病毒学
老年医学
健康政策和服务
心理学,临床
abstract::Rigidification of the isobutyl side chain of drug-like AT2 receptor agonists and antagonists that are structurally related to the first reported selective AT2 receptor agonist 1 (C21) delivered bioactive indane derivatives. Four enantiomer pairs were synthesized and the enantiomers were isolated in an optical purity >...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c9md00402e
更新日期:2019-11-18 00:00:00
abstract::The high storage capacities and excellent biocompatibilities of zinc(ii) metal-organic frameworks (Zn-MOFs) have made them outstanding candidates as drug delivery carriers. Recent studies on the pH-responsive processes based on carrier-drug interactions have proven them to be the most efficient and effective way to co...
journal_title:MedChemComm
pub_type: 杂志文章,评审
doi:10.1039/c9md00400a
更新日期:2019-10-17 00:00:00
abstract::Tetrahydroisoquinoline (THIQ) is a key structural component in many biologically active molecules including natural products and synthetic pharmaceuticals. Here, we report on the use of transition-metal mediated [2 + 2 + 2] cyclotrimerisation of alkynes to generate tricyclic THIQs with potential to selectively inhibit...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c9md00201d
更新日期:2019-06-27 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
pub_type: 杂志文章
doi:10.1039/c9md00298g
更新日期:2019-06-21 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
pub_type: 杂志文章,评审
doi:10.1039/c9md00146h
更新日期:2019-06-20 00:00:00
abstract::The development of novel nanoscale vehicles for drug delivery promotes the growth of interest in investigations of interaction between nanomaterials. In this paper, we report the in vitro studies of eukaryotic cell physiological response to incubation with graphene oxide and planar kaolin nanoclay. Graphene family mat...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00633d
更新日期:2019-06-10 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
pub_type: 杂志文章
doi:10.1039/c9md00074g
更新日期:2019-06-10 00:00:00
abstract::A focused library of 24 N-aryl urea derivatives was prepared and evaluated against serine esterases of Mycobacterium tuberculosis (Mtb) Rv3802c and Mtb Ag85C. The members of the library were evaluated for both selectivity and mode of inhibition. Furan-based urea derivative 6c was found to be the most potent non-covale...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c9md00122k
更新日期:2019-06-04 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
pub_type: 杂志文章
doi:10.1039/c9md00225a
更新日期:2019-05-30 00:00:00
abstract::A novel series of 2-pyrazoline derivatives were designed, synthesized, and evaluated for cholinesterase (ChE) inhibitory, Aβ anti-aggregating and neuroprotective activities. Among these, 3d, 3e, 3g, and 3h were established as the most potent and selective BChE inhibitors (IC50 = 0.5-3.9 μM), while 3f presented dual in...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c9md00030e
更新日期:2019-05-09 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
pub_type: 杂志文章
doi:10.1039/c9md00164f
更新日期:2019-04-09 00:00:00
abstract::Based on the scaffold of astemizole, three novel turn-on fluorescent probes (N1-N3) for human ether-a-go-go-related gene (hERG) potassium channel were developed herein. These probes have reasonable fluorescence properties, acceptable cell toxicity, and potent inhibitory activity, all of which contribute to cell imagin...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00562a
更新日期:2019-02-26 00:00:00
abstract::DNA-encoded libraries of chemically synthesized compounds are an important small molecule screening technology. The synthesis of encoded compounds in solution is currently restricted to a few DNA-compatible and water-tolerant reactions. Encoded compound synthesis of short DNA-barcodes covalently connected to solid sup...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c9md00042a
更新日期:2019-02-26 00:00:00
abstract::Urinary tract infections (UTIs) are amongst the most common and prevalent infectious diseases worldwide, with uropathogenic Escherichia coli (UPEC) reported as the main causative pathogen. Fluoroquinolone antibiotics are commonly used to treat UTIs but for infections involving UPEC biofilms, which are commonly associa...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c9md00062c
更新日期:2019-02-25 00:00:00
abstract::Three series of compounds were designed, synthesized and evaluated for their in vitro anticancer activity against a procaspase-3 over-expression cancer cell line (U937) and a procaspase-3 no-expression cancer cell line (MCF-7) to rule out off-target effects. Biological evaluation led to the identification of a series ...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00624e
更新日期:2019-02-25 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
pub_type: 杂志文章
doi:10.1039/c8md00559a
更新日期:2019-02-22 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
pub_type: 杂志文章
doi:10.1039/c8md00537k
更新日期:2019-01-25 00:00:00
abstract::In the present work, coumarin based pyrazolines (7a-g) have been synthesized and investigated for their in vitro and in vivo anti-inflammatory potential. Amongst the synthesized compounds, compounds 7a, 7d and 7f exhibited significant in vitro anti-inflammatory activity as compared to the standard etoricoxib. Keeping ...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00457a
更新日期:2019-01-23 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
pub_type: 杂志文章
doi:10.1039/c8md00432c
更新日期:2018-12-18 00:00:00
abstract::A series of novel indazole-pyrone hybrids were synthesized by a one pot reaction between N-alkyl-6(5)-nitroindazoles and 2-pyrone (4-hydroxy-6-methyl-2H-pyran-2-one) using indium or stannous chloride as the reducing system in the presence of acetic acid in tetrahydrofuran. The hybrid molecules were obtained in good to...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00475g
更新日期:2018-11-19 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
pub_type: 杂志文章
doi:10.1039/c8md00447a
更新日期:2018-11-16 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
pub_type: 杂志文章
doi:10.1039/c8md00317c
更新日期:2018-10-18 00:00:00
abstract::Herein we continued our previous work on the development of CB2 ligands, reporting the design and synthesis of a series of benzimidazole-containing derivatives that were explored as selective CB2 ligands with binding affinity towards both CB1 and CB2 receptors. Seven out of eighteen compounds exhibited preferential bi...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00461g
更新日期:2018-10-10 00:00:00
abstract::The natural products colchicine and combretastatin A-4 (CA4) have provided inspiration for the discovery and development of a wide array of derivatives and analogues that inhibit tubulin polymerization through a binding interaction at the colchicine site on β-tubulin. A water-soluble phosphate prodrug salt of CA4 (ref...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00322j
更新日期:2018-08-24 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
pub_type: 杂志文章,评审
doi:10.1039/c8md00300a
更新日期:2018-08-23 00:00:00
abstract::Much effort has been devoted to targeting agents for imaging and chemotherapy of tumors in cancer research, but there remain significant unmet needs in that area. We have reported a series of preclinical TrkC targeting agents for diagnoses and treatment of metastatic breast cancer; however, with respect to optical ima...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00190a
更新日期:2018-08-03 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
pub_type: 杂志文章
doi:10.1039/c8md00162f
更新日期:2018-06-29 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
pub_type: 杂志文章
doi:10.1039/c8md00237a
更新日期:2018-06-14 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
pub_type: 杂志文章
doi:10.1039/c8md00109j
更新日期:2018-06-12 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
pub_type: 杂志文章,评审
doi:10.1039/c8md00183a
更新日期:2018-06-06 00:00:00
abstract::Recent studies point towards the possible disadvantages of using hydroxamic acid-based zinc-binding groups in HDAC inhibitors due to e.g. mutagenicity issues. In this work, we elaborated on our previously developed Tubathian series, a class of highly selective thiaheterocyclic HDAC6 inhibitors, by replacing the benzoh...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00107c
更新日期:2018-05-18 00:00:00
abstract::Twenty-four 14-sulfonamide-tetrandrine derivatives as potential anti-cancer agents were synthesized. The synthetic derivatives were investigated for their cytotoxic activity against human cancer cell lines MDA-MB-231, PC3, WM9, HEL and K562. Initially, the IC50 values (50% inhibitory concentrations) of all of the comp...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00125a
更新日期:2018-05-04 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
pub_type: 杂志文章,评审
doi:10.1039/c8md00155c
更新日期:2018-04-17 00:00:00
abstract::[This corrects the article DOI: 10.1039/C0MD00060D.]. ...
journal_title:MedChemComm
pub_type: 已发布勘误
doi:10.1039/c8md90010h
更新日期:2018-03-19 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
pub_type: 杂志文章
doi:10.1039/c8md00019k
更新日期:2018-03-13 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
pub_type: 杂志文章
doi:10.1039/c7md00638a
更新日期:2018-03-06 00:00:00
abstract::[This corrects the article DOI: 10.1039/C7MD00637C.]. ...
journal_title:MedChemComm
pub_type: 杂志文章,已发布勘误
doi:10.1039/c8md90009d
更新日期:2018-03-02 00:00:00
abstract::New derivatives of aminoglycosides containing 6'-carboxylic acid or 6'-amide on their ring I were designed, synthesized and their ability to readthrough nonsense mutations was examined in vitro, along with the protein translation inhibition in prokaryotic and eukaryotic systems. The observed structure-activity relatio...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c8md00001h
更新日期:2018-02-02 00:00:00
abstract::A series of indole derivatives was designed and synthesised to improve on activity and circumvent pharmacokinetic limitations experienced with the structurally related compound, ladostigil. The compounds consisted of a propargylamine moiety (a known MAO inhibitor and neuroprotector) at the N1 position and a ChE inhibi...
journal_title:MedChemComm
pub_type: 杂志文章
doi:10.1039/c7md00569e
更新日期:2018-01-16 00:00:00
abstract::Potent, selective, and cell active small molecule kinase inhibitors are useful tools to help unravel the complexities of kinase signaling. As the biological functions of individual kinases become better understood, they can become targets of drug discovery efforts. The small molecules used to shed light on function ca...
journal_title:MedChemComm
pub_type: 杂志文章,评审
doi:10.1039/c7md00510e
更新日期:2017-12-08 00:00:00