Discovery of fingolimod, the sphingosine 1-phosphate receptor modulator and its application for the therapy of multiple sclerosis.

abstract：:MRI has been recognized as one of the most applied medical imaging techniques in clinical practice. However, the presence of background signal coming from water protons in surrounding tissues makes sometimes the visualization of local contrast agents difficult. To remedy this, fluorine has been introduced as a reliabl...

journal_title：Future medicinal chemistry

authors： Hequet E,Henoumont C,Muller RN,Laurent S

更新日期：2019-05-01 00:00:00

abstract：AIM:There is little information available on the monoamine oxidase isoform selectivity of N-alkyl harmine analogs, which exhibit a myriad of activities including MAO-A, DYRK1A and cytotoxicity to several select cancer cell lines. RESULTS:Compounds 3e and 4c exhibited an IC50 of 0.83 ± 0.03 and 0.43 ± 0.002 μM against ...

journal_title：Future medicinal chemistry

authors： Haider S,Alhusban M,Chaurasiya ND,Tekwani BL,Chittiboyina AG,Khan IA

更新日期：2018-06-01 00:00:00

abstract：AIM:The undeniable indomethacin potency has always suffered serious obstacles such as gastric damage. Continuous attempts to develop potent yet safe indomethacin analogs have never ceased. RESULTS:Herein are new indole derivatives 4a-h and 5a-c, which were synthesized via Fisher indole reaction, evaluated for both the...

journal_title：Future medicinal chemistry

authors： Amin NH,El-Saadi MT,Hefny AA,Abdelazeem AH,Elshemy HA,Abdellatif KR

更新日期：2018-12-06 00:00:00

abstract：:The cystic fibrosis transmembrane conductance regulator (CFTR) is a cAMP-regulated chloride channel localized primarily at the apical surfaces of epithelial cells lining airway, gut and exocrine glands, where it is responsible for transepithelial salt and water transport. Several human diseases are associated with an ...

journal_title：Future medicinal chemistry

authors： Zhang W,Fujii N,Naren AP

更新日期：2012-03-01 00:00:00

abstract：:Cancer is a major devastating disease, and is a leading cause of death worldwide. Despite the progress in cancer treatment, cancer mortality rate remains high. Therefore, the discovery and development of improved anticancer drugs to treat cancer are needed. 4H-chromenes have strong cytotoxicity against a panel of huma...

journal_title：Future medicinal chemistry

authors： Patil SA,Patil R,Pfeffer LM,Miller DD

更新日期：2013-09-01 00:00:00

abstract：:The finding of promising drugs represents a huge challenge in cancer therapeutics, therefore it is important to seek out novel approaches and elucidate essential cellular processes in order to identify potential drug targets. Studies on DNA repair pathway suggested that an enzyme, PARP, which plays a significant role ...

journal_title：Future medicinal chemistry

authors： Kumar C,Rani N,Velan Lakshmi PT,Arunachalam A

更新日期：2017-01-01 00:00:00

abstract：:Aim: Eight coumarin derivatives (1a-h) obtained from natural (-)-mammea A/BB (1) and 13 synthetic coumarins (2-14) had their cytotoxicity and biological activity evaluated against Mycobacterium tuberculosis H37Rv reference strain and multidrug-resistant clinical isolates. Materials & methods: Anti-M. tuberculosis acti...

journal_title：Future medicinal chemistry

authors： Pires CT,Scodro RB,Cortez DA,Brenzan MA,Siqueira VL,Caleffi-Ferracioli KR,Vieira LC,Monteiro JL,Corrêa AG,Cardoso RF

更新日期：2020-09-01 00:00:00

abstract：:The dynamic nature of histone post-translational modifications such as methylation or acetylation makes possible the alteration of disease associated epigenetic states through the manipulation of the associated epigenetic machinery. One approach is through small molecule perturbation. Chemical probes of epigenetic rea...

journal_title：Future medicinal chemistry

authors： Waybright JM,James LI

更新日期：2020-01-10 00:00:00

abstract：:An accelerated rate of natural-product discovery is critical for the future of ion channel pharmacology. For the full potential of natural products to be realized, an interdisciplinary initiative is required that combines chemical ecology and ion channel physiology. A prime source of future drug leads targeted to ion ...

journal_title：Future medicinal chemistry

authors： Teichert RW,Olivera BM

更新日期：2010-05-01 00:00:00

abstract：:Chi-Chao Chan, an American board certified ophthalmologist, is the Chief of Immunopathology Section, Laboratory of Immunology and the Head of Histology Core at the National Eye Institute at National Institutes of Health (USA). In 1967, Dr Chan graduated from Chungzhan Medical College in Guangzhou, China and then earne...

journal_title：Future medicinal chemistry

authors： Chan CC

更新日期：2012-11-01 00:00:00

abstract：:Mammalian carbonic anhydrases (CAs; EC 4.2.1.1) of which 16 isoforms are known, are involved in important physiological functions. Their inhibition is exploited pharmacologically for the treatment of many diseases (glaucoma, edema, epilepsy, obesity, hypoxic tumors, neuropathic pain, etc.) but the activators were less...

journal_title：Future medicinal chemistry

authors： Supuran CT

更新日期：2018-03-01 00:00:00

abstract：:Alzheimer's disease is a multifactorial syndrome, for which effective cures are urgently needed. Seeking for enhanced therapeutic efficacy, multitarget drugs have been increasingly sought after over the last decades. They offer the attractive prospect of tackling intricate network effects, but with the benefits of a s...

journal_title：Future medicinal chemistry

authors： Rosini M,Simoni E,Caporaso R,Minarini A

更新日期：2016-04-01 00:00:00

abstract：:Endomorphins, the endogenous ligands of the µ-opioid receptor, are attractive candidates for opioid-based pain-relieving agents. These tetrapeptides, with their remarkable affinity for the µ-opioid receptor, display favorable antinociceptive activity when injected directly into the brain of experimental animals. Howev...

journal_title：Future medicinal chemistry

authors： Janecka A,Gentilucci L

更新日期：2014-01-01 00:00:00

abstract：:Diabetes mellitus is an increasing public health problem in the world. Type 2 diabetes is the most common type of diabetes whose complications contribute to its high death rate. It seriously impacts healthcare systems and patients' quality of life. Therefore, effective measures and new treatment strategies are needed ...

journal_title：Future medicinal chemistry

authors： Turdu G,Gao H,Jiang Y,Kabas M

更新日期：2018-05-01 00:00:00

abstract：:The use of electron density-based molecular descriptors in drug research, particularly in quantitative structure--activity relationships/quantitative structure--property relationships studies, is reviewed. The exposition starts by a discussion of molecular similarity and transferability in terms of the underlying elec...

journal_title：Future medicinal chemistry

authors： Matta CF,Arabi AA

更新日期：2011-06-01 00:00:00

abstract：AIM:Cancer is among the leading causes of death worldwide. Medical interest has focused on macrocyclic polyamines because of their properties as antitumor agents. Results/Methodology: We have designed and synthesized a series of 1,2-diaminocyclohexane derivatives with notable in vitro antiproliferative activities again...

journal_title：Future medicinal chemistry

authors： Morales F,Ramírez A,Morata-Tarifa C,Navarro SA,Marchal JA,Campos JM,Conejo-García A

更新日期：2017-03-01 00:00:00

abstract：:Bromodomain and extra-terminal domain (BET) protein family plays an important role in regulating gene transcription preferentially at super-enhancer regions and has been involved with several types of cancers as a candidate. Up to now, there are 16 pan-BET inhibitors in clinical trials, however, most of them have unde...

journal_title：Future medicinal chemistry

authors： Yang Y,Wu Z,Chen P,Zheng P,Zhang H,Zhou J

更新日期：2020-09-01 00:00:00

abstract：:The compound class of 3-carboranyl thymidine analogues (3CTAs) are boron delivery agents for boron neutron capture therapy (BNCT), a binary treatment modality for cancer. Presumably, these compounds accumulate selectively in tumor cells via intracellular trapping, which is mediated by hTK1. Favorable in vivo biodistri...

journal_title：Future medicinal chemistry

authors： Khalil A,Ishita K,Ali T,Tjarks W

更新日期：2013-04-01 00:00:00

abstract：:Endogenous nucleotides have widespread actions in the cardiovascular system, but it is only recently that the P2X and P2Y receptor subtypes, at which they act, have been identified and subtype-selective agonists and antagonists developed. These advances have greatly increased our understanding of the physiological and...

journal_title：Future medicinal chemistry

authors： Kennedy C,Chootip K,Mitchell C,Syed NI,Tengah A

更新日期：2013-03-01 00:00:00

abstract：:This perspective explores the origins of both fluorine and medicinal chemistry a century ago and traces the early history of the intersection of these areas and the subsequent roles that fluorine has played in advancing medicinal innovations and diagnoses during the past 60 years. The overview highlights remarkable br...

journal_title：Future medicinal chemistry

authors： Filler R,Saha R

更新日期：2009-08-01 00:00:00

abstract：:Existing therapies for allergic asthma are far from perfect: the global prevalence of disease increases despite them and they are poorly effective in dealing with the exacerbations that account for hospitalization and asthma deaths. Commercially, there are pressures on these existing medicines too--a growing threat fr...

journal_title：Future medicinal chemistry

authors： Robinson C,Zhang J,Newton GK,Perrior TR

更新日期：2013-02-01 00:00:00

abstract：:There is an ever pressing need to develop new drugs for the treatment of cancer. Gallium nitrate, a group IIIa metal salt, inhibits the proliferation of tumor cells in vitro and in vivo and has shown activity against non-Hodgkin's lymphoma and bladder cancer in clinical trials. Gallium can function as an iron mimetic ...

journal_title：Future medicinal chemistry

authors： Chitambar CR

更新日期：2012-06-01 00:00:00

abstract：:More research effort needs to be invested in antimicrobial drug development to address the increasing threat of multidrug-resistant organisms. The enzyme DHPS has been a validated drug target for over 70 years as the target for the highly successful sulfa drugs. The use of sulfa drugs has been compromised by the wides...

journal_title：Future medicinal chemistry

authors： Hammoudeh DI,Zhao Y,White SW,Lee RE

更新日期：2013-07-01 00:00:00

abstract：:Aim: WHO Malaria report 2017 estimated 216 million cases of malaria and 445,000 deaths worldwide, with 91% of deaths affecting the African region. Results/methodology: Microwave promoted the synthesis of cycloalkyl amine substituted isoindoline-1,3-dione-4-aminoquinolines was urbanized for evaluating their antiplasmod...

journal_title：Future medicinal chemistry

authors： Rani A,Kumar S,Legac J,Adeniyi AA,Awolade P,Singh P,Rosenthal PJ,Kumar V

更新日期：2020-02-01 00:00:00

abstract：:Camellia oleifera Abel is a member of Camellia, and its seeds are used to extract Camellia oil, which is generally used as cooking oil in the south of China. Camellia oil consists of unsaturated fatty acids, tea polyphenol, squalene, saponin, carrot element and vitamins, etc. The seed remains after oil extraction of C...

journal_title：Future medicinal chemistry

authors： Xiao X,He L,Chen Y,Wu L,Wang L,Liu Z

更新日期：2017-11-01 00:00:00

abstract：:Matrix metalloproteinases are zinc-dependent enzymes whose main function is to cleave the components of the extracellular matrix. Their overexpression is evident in all cancers but to date there is no satisfactory way to inhibit their actions. Here, we look at their types, their structures, their functions and the dev...

journal_title：Future medicinal chemistry

authors： King SE

更新日期：2016-01-01 00:00:00

abstract：:The development of novel pharmaceutical treatments for disorders of the cerebral vasculature is a serious unmet medical need. These vascular disorders are typified by a disruption in the delicate Rho signaling equilibrium within the blood vessel wall. In particular, Rho kinase overactivation in the smooth muscle and e...

journal_title：Future medicinal chemistry

authors： Bond LM,Sellers JR,McKerracher L

更新日期：2015-01-01 00:00:00

abstract：:It is increasingly clear that academic high-throughput screening (HTS) and virtual HTS triage suffers from a lack of scientists trained in the art and science of early drug discovery chemistry. Many recent publications report the discovery of compounds by screening that are most likely artifacts or promiscuous bioacti...

journal_title：Future medicinal chemistry

authors： Dahlin JL,Walters MA

更新日期：2014-07-01 00:00:00

abstract：:During the current decade, data on the post-translational hydroxylation of specific amino acid residues of some ribosomal proteins and translation factors in both eukaryotes and eubacteria have accumulated. The reaction is catalyzed by dedicated oxygenases (so-called ribosomal oxygenases), whose action is impaired und...

journal_title：Future medicinal chemistry

authors： Graifer D,Malygin A,Karpova G

更新日期：2019-02-25 00:00:00

abstract：:Computer-aided drug design (CADD) methodologies have made great advances and contributed significantly to the discovery and/or optimization of many clinically used drugs in recent years. CADD tools have likewise been applied to the discovery of inhibitors of HIV-1 integrase, a difficult and worthwhile target for the d...

journal_title：Future medicinal chemistry

authors： Liao C,Nicklaus MC

更新日期：2010-07-01 00:00:00