Interview with Solomon Nwaka.

abstract：:Radiation-induced lung injury (RILI) is a common complication in cancer patients receiving local thoracic radiation and bone marrow transplantation conditioning. It is divided into early-stage radiation pneumonitis and advanced radiation fibrosis of the lung. This severely hampers the quality of life and survival of c...

journal_title：Future medicinal chemistry

authors： Xia C,Shi W,Zhang Y,Ding L,Gao L,Wang Q,Shao L,Dong L,Gao Y

更新日期：2020-12-01 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：:Richard H Ebright talks to Rachel Coleby, Commissioning Editor: Ebright is at Rutgers University (New Brunswick, NJ, USA), where he performs research on the structure, mechanism, and regulation of bacterial transcription and on antibacterial drug discovery targeting bacterial transcription. He has received research aw...

journal_title：Future medicinal chemistry

authors： Ebright RH

更新日期：2017-10-01 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: Alzheimer's disease (AD) is known to be themajor cause of dementia among the elderly. The structural properties and binding interactions of the AD drug physostigmine (-)-phy, and its analogues (-)-hex and (-)-phe and (+)-phe, were examined, as well as their impact on the conformational changes of two different AD...

journal_title：Future medicinal chemistry

authors： Adeniyi AA,Conradie J

更新日期：2019-08-01 00:00:00

abstract：:Aim: With the increasing emergence of drug-resistant bacteria, the need for new antimicrobial agents has become extremely urgent. This work was to develop sulfonyl thiazoles as potential antibacterial agents. Results & methodology: Novel hybrids of sulfonyl thiazoles were developed from commercial acetanilide and acet...

journal_title：Future medicinal chemistry

authors： Hu YY,Wang J,Li TJ,Yadav Bheemanaboina RR,Ansari MF,Cheng Y,Zhou CH

更新日期：2020-10-01 00:00:00

abstract：AIM:Confirm the use of Plectanthus spp. plants in traditional medicine, particularly as anti-inflammatory and anti-infective agents. MATERIALS & METHODS:Compounds previously isolated from Plectranthus spp. were studied for their anti-inflammatory activity using the SNAP assay and RAW 264.7 cells, by the quantification...

journal_title：Future medicinal chemistry

authors： Andrade JM,Custódio L,Romagnoli A,Reis CP,Rodrigues MJ,Garcia C,Petruccioli E,Goletti D,Faustino C,Fimia GM,Rijo P

更新日期：2018-07-01 00:00:00

abstract：:Micro-organisms express a wide range of transmembrane pumps known as multidrug efflux pumps that improve the micro-organism's ability to survive in severe environments and contribute to resistance against antibiotic and antimicrobial agents. There is significant interest in developing efflux inhibitors as an adjunct t...

journal_title：Future medicinal chemistry

authors： Jamshidi S,Sutton JM,Rahman KM

更新日期：2016-01-01 00:00:00

abstract：:Epigallocatechin gallate (EGCG), one of polyphenols isolated from green tea, exhibits biology-benefiting effects with minimum severe adverse. EGCG is known to be a mitochondrion-targeting medicinal agent, regulating mitochondrial metabolism, including mitochondrial biogenesis, mitochondrial bioenergetics, and mitochon...

journal_title：Future medicinal chemistry

authors： Shi W,Li L,Ding Y,Yang K,Chen Z,Fan X,Jiang S,Guan Y,Liu Z,Xu D,Wu L

更新日期：2018-04-01 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：AIM:Due to the complex nature of Alzheimer's disease, there is a renewed search for pleiotropic agents. RESULTS:Purine+coumarin hybrids have been synthesized and tested for the potential treatment of Alzheimer's disease. Hybrids 6, 4a-b, 14c and 14e inhibit significantly soybean lipoxygenase, whereas derivatives 14b, ...

journal_title：Future medicinal chemistry

authors： Kallitsakis MG,Yañez M,Soriano E,Marco-Contelles J,Hadjipavlou-Litina DJ,Litinas KE

更新日期：2015-01-01 00:00:00

abstract：AIM:Antibiotic resistance has become a major health problem. The σ(70):core interface of bacterial RNA polymerase is a promising drug target. Recently, the coiled-coil and lid-rudder-system of the β' subunit has been identified as an inhibition hot spot. Materials & methods & Results: By using surface plasmon resonance...

journal_title：Future medicinal chemistry

authors： Hüsecken K,Hinsberger S,Elgaher WA,Haupenthal J,Hartmann RW

更新日期：2014-09-01 00:00:00

abstract：:Hepatitis B Virus (HBV) is one of the most prevalent viral infections of human worldwide. The therapies are limited in the clinical context because of negative side effects of interferons and the development of viral resistance to the nucleoside/nucleotide inhibitors. In this review, we summarize the recent advances i...

journal_title：Future medicinal chemistry

authors： Jia H,Rai D,Zhan P,Chen X,Jiang X,Liu X

更新日期：2015-01-01 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：BACKGROUND:Due to the complex nature of Alzheimer's disease, there is a renewed and growing search for multitarget drugs. RESULTS:Donepezil-ferulic acid hybrids (DFAHs) were prepared by the one-pot Ugi-4CR in low-to-moderate yields. DFAHs are potent antioxidant agents, showing oxygen radical absorbance capacity values...

journal_title：Future medicinal chemistry

authors： Benchekroun M,Ismaili L,Pudlo M,Luzet V,Gharbi T,Refouvelet B,Marco-Contelles J

更新日期：2015-01-01 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：: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 pharmacokinetic treatment strategy targets the drug molecule itself, aiming to reduce drug concentration at the site of action, thereby minimizing any pharmacodynamic effect. This approach might be useful in the treatment of acute drug toxicity/overdose and in the long-term treatment of addiction. Phase IIa contro...

journal_title：Future medicinal chemistry

authors： Gorelick DA

更新日期：2012-02-01 00:00:00

abstract：:CDK12 and CDK13 are Ser/Thr protein kinases that regulate transcription and co-transcriptional processes. Genetic silencing of CDK12 is associated with genomic instability in a variety of cancers, including difficult-to-treat breast, ovarian, colorectal, brain and pancreatic cancers, and is synthetic lethal with PARP,...

journal_title：Future medicinal chemistry

authors： Tadesse S,Duckett DR,Monastyrskyi A

更新日期：2021-01-01 00:00:00

abstract：:The protein kinase superfamily is one of the most important families of enzymes in molecular biology. Protein kinases typically catalyze the transfer of the γ-phosphate from ATP to a protein substrate (a highly ubiquitous cellular reaction), thereby controlling key areas of cell regulation. Deregulation of protein kin...

journal_title：Future medicinal chemistry

authors： Elphick LM,Lee SE,Anderson AA,Child ES,Bonnac L,Gouverneur V,Mann DJ

更新日期：2009-10-01 00:00:00

abstract：:This review provides an overview of chemokines and their receptors, with an emphasis on general features and nomenclature along with a short summary of their properties and functions. It is intended as an introduction to the subject and a reference point for those wishing to learn key facts about chemokines and their ...

journal_title：Future medicinal chemistry

authors： Vinader V,Afarinkia K

更新日期：2012-05-01 00:00:00

abstract：:Many natural products that consist of quinoline core are found to be bioactive and the versatility of quinoline and its derivatives have attracted great attention in the field of drug development. As a result, in recent years, many green and sustainable synthetic approaches for the synthesis of structurally diverse qu...

journal_title：Future medicinal chemistry

authors： Chung PY,Bian ZX,Pun HY,Chan D,Chan AS,Chui CH,Tang JC,Lam KH

更新日期：2015-01-01 00:00:00

abstract：:Nutrient-sensing receptors, including fatty acid receptors (FFA1-FFA4), Ca2+-sensing receptors and Zn2+-sensing receptors, are involved in several biological processes. These receptors are abundantly expressed in the GI tract, where they have been shown to play crucial roles in regulating GI function. This review prov...

journal_title：Future medicinal chemistry

authors： Pongkorpsakol P,Moonwiriyakit A,Muanprasat C

更新日期：2017-03-01 00:00:00

abstract：:With the goal of refining our discovery DMPK workflow, we conducted a retrospective analysis on internal Celgene compounds by calculating the physicochemical properties and gathering data from several assays including solubility, rat and human liver S9 stability, Caco-2 permeability, and rat intravenous (iv.) and oral...

journal_title：Future medicinal chemistry

authors： Kulkarni A,Riggs J,Phan C,Bai A,Calabrese A,Shi T,Moghaddam MF

更新日期：2014-02-01 00:00:00

abstract：:Nucleoside analogs are extremely useful for the development of therapeutic agents to control viral diseases and cancer. Among the numerous modifications on the nucleoside skeleton, replacement of the oxygen of the furanose ring by a CH2 group resulted in increased flexibility and higher resistance to phosphorylases an...

journal_title：Future medicinal chemistry

authors： Bessières M,Chevrier F,Roy V,Agrofoglio LA

更新日期：2015-01-01 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：:The DNA repair protein, O6-methylguanine DNA methyltransferase (MGMT), can confer resistance to guanine O6-alkylating agents. Therefore, inhibition of resistant MGMT protein is a practical approach to increase the anticancer effects of such alkylating agents. Numerous small molecule inhibitors were synthesized and exh...

journal_title：Future medicinal chemistry

authors： Sun G,Zhao L,Zhong R,Peng Y

更新日期：2018-08-01 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:The similarity in the biological function of the bioisosteric pair, carboxyl and sulfonamide functional groups, is studied using the quantitative tool, average electron density of the bioisosteric moiety in drug molecules and the qualitative tool, electrostatic potential. Results/methodology: Five different capping...

journal_title：Future medicinal chemistry

authors： Arabi AA

更新日期：2017-12-01 00:00:00

abstract：:Background: Andrographolide and its benzylidene derivatives, SRJ09 and SRJ23, potentially bind oncogenic K-Ras to exert anticancer activity. Their molecular interactions with K-Ras oncoproteins that lead to effective biological activity are of major interest. Methods & results:In silico docking and molecular dynamics ...

journal_title：Future medicinal chemistry

authors： Quah SY,Tan MS,Ho KL,Manan NA,Gorfe AA,Deb PK,Sagineedu SR,Stanslas J

更新日期：2020-09-01 00:00:00