journal
https://read.qxmd.com/read/31803393/quinolone-antibiotics
#41
REVIEW
Thu D M Pham, Zyta M Ziora, Mark A T Blaskovich
The quinolone antibiotics arose in the early 1960s, with the first examples possessing a narrow-spectrum of activity with unfavorable pharmacokinetic properties. Over time, the development of new quinolone antibiotics has led to improved analogues with an expanded spectrum and high efficacy. Nowadays, quinolones are widely used for treating a variety of infections. Quinolones are broad-spectrum antibiotics that are active against both Gram-positive and Gram-negative bacteria, including mycobacteria, and anaerobes...
October 1, 2019: MedChemComm
https://read.qxmd.com/read/31803392/is-it-time-for-artificial-intelligence-to-predict-the-function-of-natural-products-based-on-2d-structure
#42
REVIEW
Miaomiao Liu, Peter Karuso, Yunjiang Feng, Esther Kellenberger, Fei Liu, Can Wang, Ronald J Quinn
Currently, there is no established technique that allows the function of a compound produced by nature to be predicted by looking at its 2-dimensional chemical structure. One of chemistry's grand challenges: to find a function for every known metabolite. We explore the opportunity for Artificial Intelligence to provide rationale interrogation of metabolites to predict their function.
October 1, 2019: MedChemComm
https://read.qxmd.com/read/31762965/synthesis-and-structure-activity-relationship-studies-of-igg-binding-peptides-focused-on-the-c-terminal-histidine-residue
#43
JOURNAL ARTICLE
Kyohei Muguruma, Mayu Ito, Akane Fukuda, Satoshi Kishimoto, Akihiro Taguchi, Kentaro Takayama, Atsuhiko Taniguchi, Yuji Ito, Yoshio Hayashi
Currently, IgG-binding peptides are widely utilized as a research tool, as molecules that guide substrates to the Fc site for site-selective antibody modification, leading to preparation of a homogeneous antibody-drug conjugate. In this study, a structure-activity relationship study of an IgG-binding peptide, 15-IgBP, that is focused on its C-terminal His residue was performed in an attempt to create more potent peptides. A peptide with a substitution of His17 by 2-pyridylalanine (2-Pya) showed a good binding affinity (15-His17(2-Pya), K d = 75...
October 1, 2019: MedChemComm
https://read.qxmd.com/read/32952999/selective-in-vitro-anti-cancer-activity-of-non-alkylating-minor-groove-binders
#44
JOURNAL ARTICLE
Ryan J O Nichol, Abedawn I Khalaf, Kartheek Sooda, Omar Hussain, Hollie B S Griffiths, Roger Phillips, Farideh A Javid, Colin J Suckling, Simon J Allison, Fraser J Scott
Traditional cytotoxic agents which act through a DNA-alkylating mechanism are relatively non-specific, resulting in a small therapeutic window and thus limiting their effectiveness. In this study, we evaluate a panel of 24 non-alkylating Strathclyde Minor Groove Binders (S-MGBs), including 14 novel compounds, for in vitro anti-cancer activity against a human colon carcinoma cell line, a cisplatin-sensitive ovarian cancer cell line and a cisplatin-resistant ovarian cancer cell line. A human non-cancerous retinal epithelial cell line was used to measure selectivity of any response...
September 1, 2019: MedChemComm
https://read.qxmd.com/read/31814957/benzoazacrown-compound-a-highly-effective-chelator-for-therapeutic-bismuth-radioisotopes
#45
JOURNAL ARTICLE
Ekaterina V Matazova, Bayirta V Egorova, Ekaterina A Konopkina, Gleb Yu Aleshin, Anastasia D Zubenko, Artem A Mitrofanov, Kirill V Karpov, Olga A Fedorova, Yuri V Fedorov, Stepan N Kalmykov
A new benzoazacrown ligand H4 BATA was synthesized and its complexation ability towards bismuth cations was evaluated. Binding of cation occurs at room temperature in a few minutes and formed complex exhibits the same level of inertness as highly stable complex with the well-known H4 DOTA in biologically relevant and challenging media under in vivo conditions.
September 1, 2019: MedChemComm
https://read.qxmd.com/read/31814956/discovery-of-napabucasin-derivatives-for-the-treatment-of-tuberculosis
#46
JOURNAL ARTICLE
Chungen Li, Yunxiang Tang, Zitai Sang, Yang Yang, Yamin Gao, Tao Yang, Cuiting Fang, Tianyu Zhang, Youfu Luo
Tuberculosis is the contagious disease responsible for the highest number of deaths worldwide. Here, we screened a commercially available compound library and found napabucasin to possess a moderate anti-tubercular activity against M. tuberculosis H37Ra (MIC 2.5 μg mL-1 , 10.4 μM). Three series of napabucasin derivatives were further evaluated for their in vitro anti-tubercular activities against Mtb H37Ra. The activity of most derivatives was either retained or enhanced compared with that of napabucasin...
September 1, 2019: MedChemComm
https://read.qxmd.com/read/31803403/piperidine-carbamate-peptidomimetic-inhibitors-of-the-serine-proteases-hgfa-matriptase-and-hepsin
#47
JOURNAL ARTICLE
Vishnu C Damalanka, Scott A Wildman, James W Janetka
Matriptase and hepsin are type II transmembrane serine proteases (TTSPs). Along with related S1 trypsin like serine protease HGFA (hepatocyte growth factor activator), their unregulated proteolytic activity has been associated with cancer including tumor progression and metastasis. These three proteases have two substrates in common, hepatocyte growth factor (HGF) and macrophage stimulating protein (MSP), the ligands for MET and recepteur d'origine nantais (RON) receptor tyrosine kinases. Mechanism-based tetrapeptide and benzamidine inhibitors of these proteases have been shown to block HGF/MET and MSP/RON cancer cell signaling...
September 1, 2019: MedChemComm
https://read.qxmd.com/read/31803402/bivalent-ampa-receptor-positive-allosteric-modulators-of-the-bis-pyrimidine-series
#48
JOURNAL ARTICLE
Anna A Nazarova, Kseniya N Sedenkova, Dmitry S Karlov, Mstislav I Lavrov, Yuri K Grishin, Tamara S Kuznetsova, Vladimir L Zamoyski, Vladimir V Grigoriev, Elena B Averina, Vladimir A Palyulin
The first example of a novel class of AMPA receptor positive allosteric modulators of the bis(pyrimidine) series having a hydroquinone linker has been obtained and showed a potency to increase kainate-induced currents at subnanomolar concentrations.
September 1, 2019: MedChemComm
https://read.qxmd.com/read/31803401/development-of-benzochalcone-derivatives-as-selective-cyp1b1-inhibitors-and-anticancer-agents
#49
JOURNAL ARTICLE
Jinyun Dong, Guang Huang, Qijing Zhang, Zengtao Wang, Jiahua Cui, Yan Wu, Qingqing Meng, Shaoshun Li
A series of benzochalcone derivatives have been synthesized and evaluated for CYP1 inhibitory activity and cytotoxic properties against wild type cell lines (MCF-7 and MDA-MB-231) and drug resistant cell lines (LCC6/P-gp and MCF-7/1B1). All of these compounds were found to have selective inhibition towards CYP1B1 and the most potent two possessed single-digit nanomolar CYP1B1 potency. In addition, some of them showed promising cytotoxic activities not only against wild type cells, but also against drug resistant cells at low micromolar concentrations...
September 1, 2019: MedChemComm
https://read.qxmd.com/read/31803400/repositioning-salirasib-as-a-new-antimalarial-agent
#50
JOURNAL ARTICLE
Exequiel O J Porta, Ignasi Bofill Verdaguer, Consuelo Perez, Claudia Banchio, Mauro Ferreira de Azevedo, Alejandro M Katzin, Guillermo R Labadie
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 methyltransferase (ICMT), a validated target for cancer drug development. There is a high homology between the human and the parasite enzyme isoforms, in addition to being a druggable target. Looking to repurpose its structure as an antimalarial drug, a collection of S -substituted derivatives of thiosalicylic acid were prepared by introducing 1,2,3-triazole as a diversity entry point or by direct alkylation of the thiol...
September 1, 2019: MedChemComm
https://read.qxmd.com/read/31803399/molecular-evolution-of-peptides-by-yeast-surface-display-technology
#51
REVIEW
Sara Linciano, Stefano Pluda, Arianna Bacchin, Alessandro Angelini
Genetically encoded peptides possess unique properties, such as a small molecular weight and ease of synthesis and modification, that make them suitable to a large variety of applications. However, despite these favorable qualities, naturally occurring peptides are often limited by intrinsic weak binding affinities, poor selectivity and low stability that ultimately restrain their final use. To overcome these limitations, a large variety of in vitro display methodologies have been developed over the past few decades to evolve genetically encoded peptide molecules with superior properties...
September 1, 2019: MedChemComm
https://read.qxmd.com/read/31803398/resisting-resistance-gearing-up-for-war
#52
REVIEW
Aurijit Sarkar, Sylvie Garneau-Tsodikova
Where do we stand in our fight against antimicrobial resistance (AMR)? Many antimicrobials may lose their clinical efficacy, particularly due to the rise of multidrug-resistant (MDR) and extended drug-resistant (XDR) pathogens, including bacteria, fungi, and parasites. We need weapons against them all. Society must come together against these pathogens, just like we did against HIV, cancer, and heart disease. This opinion piece is, first and foremost, a call to arms for all partners involved in the war against AMR...
September 1, 2019: MedChemComm
https://read.qxmd.com/read/31673316/dihydropyrimidine-2-thiones-as-eg5-inhibitors-and-l-type-calcium-channel-blockers-potential-antitumour-dual-agents
#53
JOURNAL ARTICLE
Elena González-Hernández, Rubén Aparicio, Mercedes Garayoa, M José Montero, M Ángeles Sevilla, Concepción Pérez-Melero
The use of multitarget drugs has evolved as an alternative to "magic bullets" for the treatment of complex diseases such as cancer, in order to affect simultaneously several targets relevant to the disease. We have designed and synthesized a series of dual agents as both Eg5 inhibitors and calcium channel blockers, bearing a 4-aryldihydropyrimidine core. Compound 2 (aryl: 3-nitrophenyl) was selected as potential dual agent due to displaying both activities: it is a vasorelaxant agent (>90% relaxation at 10-5 M in KCl-precontracted aorta rings), it decreases the response to calcium and it is cytotoxic to MCF-7 (breast), HCT-116 (colon) and A-549 (lung) cancer cell lines...
September 1, 2019: MedChemComm
https://read.qxmd.com/read/31673315/emerging-modes-of-action-in-drug-discovery
#54
REVIEW
Eric Valeur, Frank Narjes, Christian Ottmann, Alleyn T Plowright
An increasing focus on complex biology to cure diseases rather than merely treat symptoms has transformed how drug discovery can be approached. Instead of activating or blocking protein function, a growing repertoire of drug modalities can be leveraged or engineered to hijack cellular processes, such as translational regulation or degradation mechanisms. Drug hunters can therefore access a wider arsenal of modes-of-action to modulate biological processes and this review summarises these emerging strategies by highlighting the most representative examples of these approaches...
September 1, 2019: MedChemComm
https://read.qxmd.com/read/31673314/prodrug-strategies-for-targeted-therapy-triggered-by-reactive-oxygen-species
#55
REVIEW
Jorge Peiró Cadahía, Viola Previtali, Nikolaj S Troelsen, Mads H Clausen
Increased levels of reactive oxygen species (ROS) have been associated with numerous pathophysiological conditions including cancer and inflammation and the ROS stimulus constitutes a potential trigger for drug delivery strategies. Over the past decade, a number of ROS-sensitive functionalities have been identified with the purpose of introducing disease-targeting properties into small molecule drugs - a prodrug strategy that offers a promising approach for increasing the selectivity and efficacy of treatments...
September 1, 2019: MedChemComm
https://read.qxmd.com/read/31673313/3-ketoacyl-acp-synthase-kas-iii-homologues-and-their-roles-in-natural-product-biosynthesis
#56
REVIEW
Risa Nofiani, Benjamin Philmus, Yosi Nindita, Taifo Mahmud
The 3-ketoacyl-ACP synthase (KAS) III proteins are one of the most abundant enzymes in nature, as they are involved in the biosynthesis of fatty acids and natural products. KAS III enzymes catalyse a carbon-carbon bond formation reaction that involves the α-carbon of a thioester and the carbonyl carbon of another thioester. In addition to the typical KAS III enzymes involved in fatty acid and polyketide biosynthesis, there are proteins homologous to KAS III enzymes that catalyse reactions that are different from that of the traditional KAS III enzymes...
September 1, 2019: MedChemComm
https://read.qxmd.com/read/32952998/derivatisation-of-parthenolide-to-address-chemoresistant-chronic-lymphocytic-leukaemia
#57
JOURNAL ARTICLE
Xingjian Li, Daniel T Payne, Badarinath Ampolu, Nicholas Bland, Jane T Brown, Mark J Dutton, Catherine A Fitton, Abigail Gulliver, Lee Hale, Daniel Hamza, Geraint Jones, Rebecca Lane, Andrew G Leach, Louise Male, Elena G Merisor, Michael J Morton, Alex S Quy, Ruth Roberts, Rosanna Scarll, Timothy Schulz-Utermoehl, Tatjana Stankovic, Brett Stevenson, John S Fossey, Angelo Agathanggelou
Parthenolide is a natural product that exhibits anti-leukaemic activity, however, its clinical use is limited by its poor bioavailability. It may be extracted from feverfew and protocols for growing, extracting and derivatising it are reported . A novel parthenolide derivative with good bioavailability and pharmacological properties was identified through a screening cascade based on in vitro anti-leukaemic activity and calculated "drug-likeness" properties, in vitro and in vivo pharmacokinetics studies and hERG liability testing...
August 1, 2019: MedChemComm
https://read.qxmd.com/read/32180918/diversification-of-polyketide-structures-via-synthase-engineering
#58
REVIEW
Taylor Kornfuehrer, Alessandra S Eustáquio
Polyketide natural products possess diverse biological activities including antibiotic, anticancer, and immunosuppressive. Their equally varied and complex structures arise from head-to-tail condensation of simple carboxyacyl monomers. Since the seminal discovery that biosynthesis of polyketides such as the macrolide erythromycin is catalyzed by uncharacteristically large, multifunctional enzymes, termed modular type I polyketide synthases, chemists and biologists alike have been inspired to harness the apparent modularity of the synthases to further diversify polyketide structures...
August 1, 2019: MedChemComm
https://read.qxmd.com/read/31803397/gramicidin-s-inspired-antimicrobial-cyclodextrin-to-disrupt-gram-negative-and-gram-positive-bacterial-membranes
#59
JOURNAL ARTICLE
Hatsuo Yamamura, Kana Isshiki, Yusuke Fujita, Hisato Kato, Takashi Katsu, Kazufumi Masuda, Kayo Osawa, Atsushi Miyagawa
A membrane-active antimicrobial peptide gramicidin S-like amphiphilic structure was prepared from cyclodextrin. The mimic was a cyclic oligomer composed of 6-amino-modified glucose 2,3-di- O -propanoates and it exhibited antimicrobial activity against Gram-positive and Gram-negative bacteria, together with no resistance development and low haemolytic activity against red blood cells.
August 1, 2019: MedChemComm
https://read.qxmd.com/read/31673312/synthesis-and-anti-cancer-activities-of-glycosides-and-glycoconjugates-of-diterpenoid-isosteviol
#60
JOURNAL ARTICLE
Radmila R Sharipova, Mayya G Belenok, Bulat F Garifullin, Anastasiya S Sapunova, Alexandra D Voloshina, Olga V Andreeva, Irina Yu Strobykina, Polina V Skvortsova, Yuriy F Zuev, Vladimir E Kataev
A series of glycosides and glycoconjugates of diterpenoid isosteviol (16-oxo- ent -beyeran-19-oic acid) with various monosaccharide residues were synthesized and their cytotoxicity against some human cancer and normal cell lines was assayed. Most of the synthesized compounds demonstrated moderate to significant cytotoxicity against human cancer cell lines M-HeLa and MCF-7. Three lead compounds exhibited selective cytotoxic activities against M-HeLa (IC50 = 10.0-15.1 μM) that were three times better than the cytotoxicity of the anti-cancer drug Tamoxifen (IC50 = 28...
August 1, 2019: MedChemComm
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