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Future Medicinal Chemistry

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https://www.readbyqxmd.com/read/29779411/wnt-pathway-a-hallmark-of-drug-discovery-challenge
#1
Ivan Babic, Venkata M Yenugonda, Santosh Kesari, Elmar Nurmemmedov
No abstract text is available yet for this article.
May 21, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29779400/design-synthesis-and-biological-evaluation-of-chromenopyrimidines-as-potential-cytotoxic-agents
#2
Nehal M El-Bakhshawangy, Hala B El-Nassan, Asmaa E Kassab, Azza T Taher
AIM: The design and synthesis of chromenopyrimidines as microtubule destabilizing agents. MATERIALS & METHODS: Novel chromenopyrimidines and chromenotriazolopyrimidines were prepared and evaluated for their cytotoxicity against MCF-7 cell line. The most potent compound was tested for its possible effect on tubulin inhibition, cell cycle distribution, apoptosis initiation and caspase-3 activation. RESULTS: All the prepared compounds showed potent cytotoxic activity...
May 21, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29766737/identification-of-small-molecule-egfr-allosteric-inhibitors-by-high-throughput-docking
#3
Fabiana Caporuscio, Annachiara Tinivella, Valentina Restelli, Marta S Semrau, Luca Pinzi, Paola Storici, Massimo Broggini, Giulio Rastelli
AIM: The EGFR inhibitors represent the first-line treatment of non-small-cell lung cancer. However, the emergence of resistance urgently requires the development of new inhibitors targeting drug-resistant mutants. METHODOLOGY: A recently released structure of an EGFR kinase domain in complex with an allosteric inhibitor and a mutant protein model derived from it were used to set up a low-cost high-throughput docking protocol for the fast identification of EGFR allosteric inhibitors...
May 16, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29749767/design-synthesis-and-biological-evaluation-of-some-novel-quinazolinone-derivatives-as-potent-apoptotic-inducers
#4
Raghad M Nowar, Essam Eldin A Osman, Sahar M Abou-Seri, Samir M El Moghazy, Dalal A Abou El Ella
AIM: Novel quinazolinone and triazinoquinazolinone derivatives were designed and synthesized as apoptotic inducers. METHODOLOGY/RESULTS: Most of the synthesized compounds showed excellent antiproliferative activity against MCF-7 and HCT-116 cell lines, respectively. Compounds 7a, 8a, 8d, 14a and 14d were superior to doxorubicin as activators of caspases 3, 8 and 9 in HCT-116 cell line. The most potent caspase inducers, 8d and 14a showed cell cycle arrest mainly in G1 and S phase, respectively and increased the levels of p53, Bax and the Bax/Bcl-2 ratio compared with doxorubicin in HCT-116 cells with excellent selectivity against CCD-18Co human colon normal cell line...
May 11, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29749760/plant-dipeptidyl-peptidase-iv-inhibitors-as-antidiabetic-agents-a-brief-review
#5
Gulmira Turdu, Hongwei Gao, Yingying Jiang, Madina Kabas
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 to solve this increasingly serious global problem. In recent years, inhibition of dipeptidyl peptidase IV (DPP-IV) has emerged as a new treatment option for Type 2 diabetes. This article reviews various plant DPP-IV inhibitors that showed inhibition toward enzyme as a major target for the management of Type 2 diabetes...
May 11, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29749759/anticancer-properties-of-the-abietane-diterpene-6-7-dehydroroyleanone-obtained-by-optimized-extraction
#6
Catarina Garcia, Catarina Oliveira Silva, Carlos M Monteiro, Marisa Nicolai, Ana Viana, Joana M Andrade, Isabel Barasoain, Tijana Stankovic, José Quintana, Inmaculada Hernández, Ignacio González, Francisco Estévez, Ana M Díaz-Lanza, Catarina P Reis, Carlos Am Afonso, Milica Pesic, Patrícia Rijo
AIM: 6,7-dehydroroyleanone (DHR) is a cytotoxic abietane present in the essential oil of Plectranthus madagascariensis. METHODS/RESULTS: Different extraction parameters were tested, and its extraction optimization was accomplished with a Clevenger apparatus-based hydrodistillation. After isolation, its effect on microtubules, P-glycoprotein and caspases was assessed on several cell lines and the compound was coupled with hybrid nanoparticles. The results show that DHR does not interfere with microtubule formation, but evades the resistance mechanisms of P-glycoprotein...
May 11, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29749749/recent-progress-of-sodium-glucose-transporter-2-inhibitors-as-potential-antidiabetic-agents
#7
Yajing Zhang, Huazhuo Ban, Runan Yu, Zhijian Wang, Dayong Zhang
SGLT2 inhibitors were promising and novel antidiabetic drugs which suppressed glucose reabsorption and increased urinary glucose exertion. This review paper are aimed to summarize the recent progress of SGLT2 inhibitors during the last 5 years. This paper first summarizes the information of SGLT2 inhibitors, including mechanism, evolution and then focuses on the recent efforts on structure-activity relationships and structural optimization of SGLT2 inhibitors. Finally, the corresponding clinical therapeutic efficacy and adverse drug reaction in patients with Type 2 diabetes are discussed in detail...
May 11, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29749746/dithiolethiones-a-privileged-pharmacophore-for-anticancer-therapy-and-chemoprevention
#8
Mohd Imran Ansari, Mohd M Khan, Mohammad Saquib, Shahnaaz Khatoon, Mohd Kamil Hussain
Dithiolethiones are five-membered sulfur-containing cyclic scaffolds that exhibit antioxidative, anti-inflammatory, antithrombic and chemotherapeutic activities. Dithiolethiones display the chemopreventive and cytoprotective effects by activating the antioxidant response element and mounting the transcription of cytoprotective phase II enzymatic machinery. In addition, several classes of dithiolethiones efficiently modulate the activities of proteins that play crucial roles in normal and cancer cells, including glutathione S-transferase, cyclooxygenases and master regulator NF-κB...
May 11, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29749745/potential-cytotoxic-and-selective-effect-of-new-benzo-b-xanthenes-against-oral-squamous-cell-carcinoma
#9
Bruna C Zorzanelli, Lucas N de Queiroz, Raíssa Ma Santos, Luiza M Menezes, Fernanda C Gomes, Vitor F Ferreira, Fernando de C da Silva, Bruno K Robbs
AIM: The current work shows a new synthetic methodology to obtain 21 naphthoquinones that have been evaluated against oral cavity cancer. The compounds were obtained by a three-component reaction involving lawsone, dimedone and aromatic aldehydes catalyzed by lithium chloride under microwave irradiation to produce families of 1,4- and 1,2-naphthoquinones. RESULTS: A clonogenic assay was performed on SCC9 cell line cultures with all compounds, revealing five very active compounds...
May 11, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29745776/design-synthesis-structure-activity-relationships-of-a-new-class-of-antihuman-enterovirus-d68-a71-agents
#10
Bidyadhar Sethy, Chung-Fan Hsieh, Chieh Yeh, Jim-Tong Horng, Pei-Wen Hsieh
AIM: No antiviral medications are currently approved to treat enterovirus (EV)-associated disease or prevent EV infection. METHODS: In this study, a series of probenecid derivatives were designed via a rational strategy and synthesized to obtain more potent anti-EV agents. RESULTS: Compounds 8 and 24 exhibited the most potent activity against EV D68 and A71, with half maximal effective concentration (EC50 ) values of 2.49/2.09 and 2.59/2.41 μM, respectively, and revealed a broad inhibition spectrum toward other EV strains, with high selectivity indices...
May 10, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29719974/global-medicinal-chemistry-and-gcpr-conference
#11
Laurent Schio
Laurent Schio speaks to Benjamin Walden, Commissioning Editor. Laurent Schio is leading the group of Integrated Drug Discovery of Sanofi, France. He joined Sanofi more than 25 years ago and is an organic chemist by training. He has made most of his career in medicinal chemistry supporting and leading projects, especially in the anti-infective and then in the oncology fields. He has developed a strong expertise in kinases and lately has contributed to the discovery of several clinical candidates for cancer treatment...
May 3, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29719970/metal-chelating-agents-against-viruses-and-parasites
#12
Erofili Giannakopoulou, Vasiliki Pardali, Grigoris Zoidis
No abstract text is available yet for this article.
May 3, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29717883/drugging-homologous-recombination-back-to-the-future
#13
Hannah Sanford-Crane, Tanja Pejovic, Xiangshu Xiao
No abstract text is available yet for this article.
May 2, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29708431/synthesis-and-evaluation-of-thiazolidinone-pyrazole-conjugates-as-anticancer-and-antimicrobial-agents
#14
Mahima Bhat, Boja Poojary, Bhuvanesh Sukhlal Kalal, Purawarga Matada Gurubasavaraja Swamy, Senthamaraikannan Kabilan, Vasantha Kumar, Nooji Shruthi, Selvam Athavan Alias Anand, Vinitha Ramanath Pai
AIM: To synthesize a series of new thiazolidinone-pyrazole hybrids (5a-o) and assess their anticancer (in vitro and in vivo) and antimicrobial activities. RESULTS: The compounds 5h (against Ehrlich ascites carcinoma cells), 5e and 5i (against the human breast cancer [MDA-MB231] cell line) exhibited potent anticancer activity. All the compounds except 5g and 5e found to be less toxic for the human dermal fibroblast cells. The effective interactions of the compounds in silico with MDM2 exemplified their inhibitory potency...
April 30, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29683339/discovery-of-benzylthio-analogs-of-fluconazole-as-potent-antifungal-agents
#15
Kamran Motahari, Hamid Badali, Seyedeh Mahdieh Hashemi, Hamed Fakhim, Hassan Mirzaei, Afsane Vaezi, Mohammad Shokrzadeh, Saeed Emami
AIM: A new series of triazole alcohol antifungals 8a-j were designed by introducing benzylthio functionality on one triazole ring of fluconazole. RESULTS: The antifungal activity evaluation of target compounds against 16 Candida isolates indicated that all compounds with MIC values of 0.063-1 μg/ml had better profile of activity in respect to fluconazole (MICs = 0.5-4 μg/ml) against fluconazole-susceptible isolates. In particular, the representative compounds 8b and 8e were also active against fluconazole-resistant isolates of Candida albicans and Candida parapsilosis (MICs = 0...
April 23, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29676588/lysine-acetyltransferase-inhibitors-structure-activity-relationships-and-potential-therapeutic-implications
#16
Francesco Fiorentino, Antonello Mai, Dante Rotili
Lysine acetylation is a post-translational modification of both histone and nonhistone proteins that is catalyzed by lysine acetyltransferases and plays a key role in numerous biological contexts. The dysregulation of this enzyme activity is implicated in many human pathologies such as cancer, neurological and inflammatory disorders. Many lysine acetyltransferase inhibitors (KATi) have been developed so far, but there is still the need for new, more potent, metabolically stable and selective KATi as chemical tools for studying KAT biology and/or as potential therapeutic agents...
April 20, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29676183/synthesis-%C3%AE-glucosidase-inhibitory-glucose-consumption-promoting-activities-of-flavonoid-coumarin-hybrids
#17
Hua Sun, Xiaotong Song, Yunchang Tao, Ming Li, Ke Yang, Hang Zheng, Zongxin Jin, Robert H Dodd, Guojun Pan, Kui Lu, Peng Yu
AIM: The research of novel and potent antidiabetic agents is urgently needed for the control of the exploding diabetic population. We previously reported the synthesis and antidiabetic activity of natural 8-(6"-umbelliferyl)-apigenin (1), but its antidiabetic targets are not known. Therefore, four series of derivatives were synthesized and evaluated for their antidiabetic activities. Results & methodology: Compounds (5a) and (14a) were identified as new α-glucosidase and α-amylase dual inhibitors...
April 20, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29676175/epigenetic-agents-in-combined-anticancer-therapy
#18
Zdeněk Kejík, Milan Jakubek, Robert Kaplánek, Jarmila Králová, Ivan Mikula, Pavel Martásek, Vladimír Král
In the last decade, epigenetic drugs (such as inhibitors of DNA methyltransferases and histone deacetylases) have been intensively used for cancer treatment. Their applications have shown high anticancer effectivity and tolerable side effects. However, they are unfortunately not effective in the treatment of some types and phenotypes of cancers. Nevertheless, several studies have demonstrated that problems of drug efficacy can be overcome through the combined application of therapeutic modulates. Therefore, combined applications of epigenetic agents with chemotherapy, radiation therapy, immunotherapy, oncolytic virotherapy and hyperthermia have been presented...
April 20, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29676173/biomolecular-basis-of-matrix-metallo-proteinase-9-activity
#19
Rayala Swetha, Chandrim Gayen, Devendra Kumar, Tryambak Deo Singh, Gyan Modi, Sushil Kumar Singh
Matrix metalloproteinases (MMPs) are structurally related endopeptidases. They are also known as metzincins due to their interaction with zinc ion of the conserved methionine (Met) at the active site. MMPs play an important role in physiological and signaling processes of wound healing, bone resorption and angiogenesis. The structure of MMPs consists of signal peptide, propeptide, catalytic domain, hinge region and hemopexin-like domain. MMP-9 shares high structural and functional similarities with MMP-2, therefore designing selective MMP-9 inhibitors (MMPIs) is challenging...
April 20, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29676170/discovery-of-novel-dual-acetylcholinesterase-inhibitors-with-antifibrillogenic-activity-related-to-alzheimer-s-disease
#20
Jonathan R de Almeida, Micheli Figueiro, Wanda Pereira Almeida, Carlos Henrique Tomich de Paula da Silva
AIM: Alzheimer's disease is a progressive and neurodegenerative disorder of the CNS, affecting elderly people. The current pharmacological approach is based on the improvement of cholinergic neurotransmission by inhibiting acetylcholinesterase (AChE) with AChE inhibitors. The disease is also characterized by the accelerated accumulation of β-amyloid plaques around neurons. Furthermore, in vitro studies revealed that AChE can induce β-amyloid peptide (Aβ) aggregation. METHODOLOGY: Computer-aided molecular design by virtual screening was here employed to discover novel potential AChE inhibitors, with antifibrillogenic properties, in other words, inhibiting Aβ aggregation...
April 20, 2018: Future Medicinal Chemistry
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