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Future Medicinal Chemistry

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https://www.readbyqxmd.com/read/28891315/development-of-pyridine-dicoumarols-as-potent-anti-hiv-1-leads-targeting-hiv-1-associated-topoisomeraseii%C3%AE-kinase
#1
Kurumurthy Kammari, Kiran Devaraya, Akhila Bommakanti, Anand K Kondapi
AIM: A structural study of a series of pyridine dicoumarol derivatives with potential activity against a novel Topoisomerase IIβ kinase which was identified in the HIV-1 viral lysate, compounds were designed and synthesized based on a 3D-QSAR study. MATERIALS & METHODS: Based on QSAR model we have designed and synthesized a series of pyridine dicoumarol derivatives and characterized by spectral studies, all the molecules are biologically evaluated by kinase assay, cytotoxicity assay, ELISA and PCR method...
September 11, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28884584/a-fruitful-decade-for-fungal-polyketides-from-2007-to-2016-antimicrobial-activity-chemotaxonomy-and-chemodiversity
#2
Hidayat Hussain, Abdullah M Al-Sadi, Barbara Schulz, Michael Steinert, Ajmal Khan, Ivan R Green, Ishtiaq Ahmed
The last three decades have shown that the fungi can be 'biofactories' of novel, bioactive secondary metabolites that produce numerous natural products with novel skeletons and biological activities. Particularly in the last 10 years, large numbers of antimicrobial fungal secondary metabolites have been discovered. This review provides an overview of key, defining developments of the last 10 years regarding the discovery of antimicrobial activity, chemotaxonomy and chemodiversity of fungal polyketides.
September 8, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28871831/identification-of-some-novel-xanthine-based-derivatives-with-bronchodilator-activity
#3
Abdalla R Mohamed, Hanan H Georgey, Riham F George, Wafaa I El-Eraky, Dalia O Saleh, Nagwa M Abdel Gawad
AIM: The discovery of new bronchodilators with higher efficacy than theophylline is an important issue for asthmatic patients. MATERIALS & METHODS: Theophylline 2, 8-bromotheophylline 4 and theobromine 6 were reacted with different 2/3-chloro-N-phenylacetamides 1a-d or their propanamide analogs 1e-g to obtain 3a-g, 5a-g and 7a-g, respectively. The target compounds were screened for their in vitro bronchodilator activity using isolated guinea pig tracheal rings precontracted with histamine and compared with their precursors...
September 5, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28869400/azide-alkyne-cycloaddition-en-route-to-4-aminoquinoline-ferrocenylchalcone-conjugates-synthesis-and-anti-tb-evaluation
#4
Amandeep Singh, Albertus Viljoen, Laurent Kremer, Vipan Kumar
AIM: Tuberculosis is responsible for 9.6 million infections and 1.5 million deaths in 2015. The development of multidrug-resistant and extensively drug-resistant strains has impeded the development of effective antitubercular therapy. Results/methodology: The present manuscript describes the synthesis of a series of 4-aminoquinoline-ferrocenylchalcone conjugates via Cu-promoted Huisgen's azide-alkyne cycloaddition reaction and evaluation of their antitubercular activities against mc(2)6230 strain of Mycobacterium tuberculosis...
September 4, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28869398/synthesis-and-evaluation-of-haloperidol-metabolite-ii-prodrugs-as-anticancer-agents
#5
Maria Dichiara, Emanuele Amata, Antonio Rescifina, Orazio Prezzavento, Giuseppe Floresta, Carmela Parenti, Valeria Pittalà, Agostino Marrazzo
The use of haloperidol metabolite II (HP-metabolite II) prodrugs is an emerging strategy in the treatment of cancer. HP-metabolite II exhibits antiproliferative properties at micromolar concentrations inducing apoptosis in different types of cancer. Thus, the application of the prodrug approach appears as a useful method leading to much more desirable pharmacokinetic and pharmacodynamic properties. Some studies have shown that the esterification of the hydroxyl group of HP-metabolite II with 4-phenylbutiric acid (4-PBA) or valproic acid enhances the anticancer therapeutic potency...
September 4, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28857617/recent-advances-and-novel-treatments-for-sphingolipidoses
#6
Christoph Arenz
Sphingolipidoses are genetically inherited diseases in which genetic mutations lead to functional deficiencies in the enzymes needed for lysosomal degradation of sphingolipid substrates. As a consequence, nondegradable lipids enrich in the lysosomes and lead to fatal pathological phenotypes in affected individuals. In this review, different drug-based treatment strategies including enzyme replacement therapy and substrate reduction therapy are discussed. A special focus is on the concept of pharmacological chaperones, one of which recently acquired clinical approval within the EU...
August 31, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28841048/the-potential-role-of-in-silico-approaches-to-identify-novel-bioactive-molecules-from-natural-resources
#7
Abdurrahman Olğaç, Ilkay Erdogan Orhan, Erden Banoglu
In recent years, integration of in silico approaches to natural product (NP) research reawakened the declined interest in NP-based drug discovery efforts. In particular, advancements in cheminformatics enabled comparison of NP databases with contemporary small-molecule libraries in terms of molecular properties and chemical space localizations. Virtual screening and target fishing approaches were successful in recognizing the untold macromolecular targets for NPs to exploit the unmet therapeutic needs. Developments in molecular docking and scoring methods along with molecular dynamics enabled to predict the target-ligand interactions more accurately taking into consideration the remarkable structural complexity of NPs...
August 25, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28841047/synthesis-and-biological-evaluation-of-curcumin-analogs-as-%C3%AE-amyloid-imaging-agents
#8
Changsheng Gan, Jingyi Hu, Dou-Dou Nan, Shanshan Wang, Hong Li
AIM: Detection of β-amyloid (Aβ) plaques in the brain is a very promising biomarker approach for early diagnosis of Alzheimer's disease (AD). MATERIALS & METHODS: A series of curcumin analogs (1,5-diphenyl-1,4-pentadien-3-one derivatives) were synthesized and evaluated. Specific binding to Aβ plaques was demonstrated in vitro using postmortem AD homogenates, and the fluorescent staining and autoradiography in vitro of postmortem AD brain sections were performed...
August 25, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28841037/dual-abrogation-of-mnk-and-mtor-a-novel-therapeutic-approach-for-the-treatment-of-aggressive-cancers
#9
Ella Lineham, John Spencer, Simon J Morley
Targeting the translational machinery has emerged as a promising therapeutic option for cancer treatment. Cancer cells require elevated protein synthesis and exhibit augmented activity to meet the increased metabolic demand. Eukaryotic translation initiation factor 4E is necessary for mRNA translation, its availability and phosphorylation are regulated by the PI3K/AKT/mTOR and MNK1/2 pathways. The phosphorylated form of eIF4E drives the expression of oncogenic proteins including those involved in metastasis...
August 25, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28832190/corrigendum
#10
(no author information available yet)
No abstract text is available yet for this article.
August 23, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28832188/dual-multitargeted-xanthone-derivatives-for-alzheimer-s-disease-where-do-we-stand
#11
Maria I Cruz, Honorina Cidade, Madalena Pinto
To date, the current therapy for Alzheimer's disease (AD) based on acetylcholinesterase inhibitors is only symptomatic, being its efficacy limited. Hence, the recent research has been focused in the development of different pharmacological approaches. Here we discuss the potential of xanthone derivatives as new anti-Alzheimer agents. The interference of xanthone derivatives with acetylcholinesterase and other molecular targets and cellular mechanisms associated with AD have been recently systematically reported...
August 23, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28828898/how-can-the-structure-of-germinal-center-kinase-like-kinase-help-us-in-drug-discovery
#12
Laura Silvian
No abstract text is available yet for this article.
August 22, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28828889/small-molecules-and-their-role-in-effective-preclinical-target-validation
#13
Michael A Clegg, Nicholas Co Tomkinson, Rab K Prinjha, Philip G Humphreys
No abstract text is available yet for this article.
August 22, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28819994/the-mechanistic-antitumor-study-of-myricanol-5-fluorobenzyloxy-ether-in-human-leukemic-cell-hl-60
#14
Guan-Hai Dai, Chen-Jie Fan, Ze-Ming Ren, Xuan Chen, Ye-Ling Tong, Zhen-Hua Li, Xiao-Jing Nie, Ke-Qun Chai
AIM: The aim of the study was to explore the growth inhibitory effect of myricanol 5-fluorobenzyloxy ether (5FEM) and the underlying mechanism in human leukemic cells HL-60. MATERIALS & METHODS: 5FEM was obtained by chemical modification of myricanol with fluorobenzyloxy ether at the OH(5) position. The cytotoxicity, cell apoptosis, cell cycle and the expression of key apoptosis-related genes in HL-60 were evaluated. RESULTS & CONCLUSION: 5FEM can significantly inhibited growth of HL-60 cells, increased the G2/M population and upregulated the expression of Bax, Fas, FasL, caspase-9 and p21 and downregulated that of Bcl-2 and survivin...
August 18, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28795599/antimicrobial-2-aminothiazolyl-quinolones-what-is-their-potential-in-the-clinic
#15
Wei-Wei Gao, Cheng-He Zhou
No abstract text is available yet for this article.
August 10, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28795598/inhibition-studies-of-dna-methyltransferases-by-maleimide-derivatives-of-rg108-as-non-nucleoside-inhibitors
#16
Grégoire Rondelet, Laurence Fleury, Céline Faux, Véronique Masson, Jean Dubois, Paola B Arimondo, Luc Willems, Johan Wouters
AIM: DNA methyltransferases (DNMTs) are important drug targets for epigenetic therapy of cancer. Nowadays, non-nucleoside DNMT inhibitors are in development to address high toxicity of nucleoside analogs. However, these compounds still have low activity in cancer cells and mode of action of these compounds remains unclear. MATERIALS & METHODS: In this work, we studied maleimide derivatives of RG108 by biochemical, structural and computational approaches to highlight their inhibition mechanism on DNMTs...
August 10, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28795595/what-is-the-future-for-fragment-based-drug-discovery
#17
György M Keserű, Michael M Hann
No abstract text is available yet for this article.
August 10, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28795593/small-molecule-inhibitors-for-acute-myeloid-leukemia-where-is-the-field-heading
#18
Paul C Trippier
No abstract text is available yet for this article.
August 10, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28795592/semi-synthetic-thymoquinone-analogs-new-prototypes-as-potential-antihyperlipidemics-in-irradiated-rats
#19
Nashwa H Zaher, Engy R Rashed, Mona A El-Ghazaly
AIM: Thymoquinone (TQ), has been reported to possess strong antihyperlipidemic properties. However, a variety of serious side effects has been reported for TQ. The present study aimed to evaluate the potential antihyperlipidemic activity of newly synthesized TQ analogs. METHODS & RESULTS: first, novel TQ derivatives were studied against radiation-induced dyslipidemia in male rats. Second, the most promising sulfur derivatives (4-7), were further tested to elucidate their possible mechanism(s) of actions...
August 10, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28795589/a-novel-series-of-n-pyridin-2-yl-4-thiazol-5-yl-pyrimidin-2-amines-as-highly-potent-cdk4-6-inhibitors
#20
Solomon Tadesse, Ge Zhu, Laychiluh B Mekonnen, Jimma L Lenjisa, Mingfeng Yu, Michael P Brown, Shudong Wang
AIM: Inhibitors of CDK4/6 have emerged as a powerful class of therapeutics for treatment of several malignancies. We herein describe the identification of a new series of molecules that demonstrated excellent selectivity for CDK4/6 over CDKs1, 7 and 9. RESULTS: Medicinal chemistry optimization led to the discovery of 58 and 69 that inhibited CDK4 and CDK4/6, respectively, with high potency and selectivity, and 58 and 69 exhibited potent antiproliferative activities in a panel of human cancer cell lines including leukemia, and cancers of the breast, colon, ovary, pancreas and prostate...
August 10, 2017: Future Medicinal Chemistry
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