Correction: Recent updates in the discovery and development of novel antimalarial drug candidates.

abstract：:Previous studies have demonstrated that natural steroid compounds containing a peroxide bridge exhibited potential anti-hepatitis B virus activity. To continue our research, a simple and regioselective methodology, using Eosin Y as a clean photosensitized oxidation catalyst, was developed for the synthesis of a peroxi...

journal_title：MedChemComm

authors： Jia M,Zhao R,Xu B,Yan W,Chu F,Gu H,Xie T,Xiang H,Ren J,Chen D,Wang P,Lei H

更新日期：2016-10-19 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：: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：: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

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：: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

authors： Potowski M,Kunig VBK,Losch F,Brunschweiger A

更新日期：2019-02-26 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：: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：: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

authors： Yang Z,Usama SM,Li F,Burgess K,Li Z

更新日期：2018-08-03 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：:Receptor mediated gene delivery to the liver offers advantages in treating genetic disorders such as hemophilia and hereditary tyrosinemia type I (HTI). Prior findings demonstrated that tethering the d-galactose head group to cationic lipids directs genes to the liver via asialoglycoprotein receptors (ASGPRs). In our ...

journal_title：MedChemComm

authors： Muripiti V,Lohchania B,Marepally SK,Patri SV

更新日期：2017-12-06 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：: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：: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：: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：: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：: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

authors： Zhang X,Liu T,Wang B,Gao Y,Liu P,Li M,Du L

更新日期：2019-02-26 00:00:00

abstract：:To increase the diversity of estrogen receptor (ER) ligands having novel structures and activities, series of selenophene derivatives with a basic side chain (BSC) were synthesized and their biological activity as subtype-selective antagonists for the ER was explored. Compared with the selenophenes without a BSC, most...

journal_title：MedChemComm

authors： Luo J,Hu Z,Xiao Y,Yang T,Dong C,Huang J,Zhou HB

更新日期：2017-05-24 00:00:00

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

authors： Wallinder C,Sköld C,Sundholm S,Guimond MO,Yahiaoui S,Lindeberg G,Gallo-Payet N,Hallberg M,Alterman M

更新日期：2019-11-18 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：: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：: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

authors： Verderosa AD,Harris J,Dhouib R,Totsika M,Fairfull-Smith KE

更新日期：2019-02-25 00:00:00

abstract：:A new iron(iii) complex with 5,7-dichloro-2-methyl-8-quinolinol (HClMQ) as ligands, i.e., [Fe(ClMQ)2Cl] (1), was synthesized and evaluated for its anticancer activity. Compared to the HClMQ ligand, complex 1 showed a higher cytotoxicity towards a series of tumor cell lines, including Hep-G2, BEL-7404, NCI-H460, A549, ...

journal_title：MedChemComm

authors： Zou BQ,Qin QP,Bai YX,Cao QQ,Zhang Y,Liu YC,Chen ZF,Liang H

更新日期：2017-02-01 00:00:00

abstract：:The synthesis, biological evaluation and molecular modeling of a series of pyrrole compounds related to 3,5-dibromo-4-(3,4-dimethoxyphenyl)-1H-pyrrole-2-carboxylic acid that evaluates and optimizes C-4 substituents are reported. The key factor for microtubule depolymerization activity appears to be the presence of an ...

journal_title：MedChemComm

authors： Da C,Telang N,Hall K,Kluball E,Barelli P,Finzel K,Jia X,Gupton JT,Mooberry SL,Kellogg GE

更新日期：2013-01-01 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

authors： Maguire CJ,Chen Z,Mocharla VP,Sriram M,Strecker TE,Hamel E,Zhou H,Lopez R,Wang Y,Mason RP,Chaplin DJ,Trawick ML,Pinney KG

更新日期：2018-08-24 00:00:00

abstract：:[This corrects the article DOI: 10.1039/C0MD00060D.]. ...

journal_title：MedChemComm

authors： Chen T,Mei WJ,Wong YS,Liu J,Liu Y,Xie HS,Zheng WJ

更新日期：2018-03-19 00:00:00

abstract：:In the last three decades, protein and nucleic acid structure determination and comprehension of the mechanisms, leading to their physiological and pathological functions, have become a cornerstone of biomedical sciences. A deep understanding of the principles governing the fates of cells and tissue at the molecular l...

journal_title：MedChemComm

authors： Bernetti M,Cavalli A,Mollica L

更新日期：2017-01-30 00:00:00

abstract：:The introduction of proteins into dendritic cells (DCs) ex vivo is a critical step for the DC-based immunotherapy of cancer. Here, we developed a biotin-modified polymer with multiple hydrophobic membrane anchors for cells that functions as a synthetic receptor for an antigen protein, ovalbumin (OVA), to introduce it ...

journal_title：MedChemComm

authors： Li C,Takeo M,Matsuda M,Nagai H,Xizheng S,Hatanaka W,Kishimura A,Inoue H,Tani K,Mori T,Katayama Y

更新日期：2017-05-12 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

authors： Depetter Y,Geurs S,Vanden Bussche F,De Vreese R,Franceus J,Desmet T,De Wever O,D'hooghe M

更新日期：2018-05-18 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

authors： Wells CI,Kapadia NR,Couñago RM,Drewry DH

更新日期：2017-12-08 00:00:00