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Future Medicinal Chemistry

Peter V Dubovskii, Anastasia A Ignatova, Pavel E Volynsky, Igor A Ivanov, Maxim N Zhmak, Alexey V Feofanov, Roman G Efremov
AIM: Spider venom is a rich source of antibacterial peptides, whose hemolytic activity is often excessive. METHODOLOGY: How to get rid of it? Using latarcins from Lachesana tarabaevi and oxyopinin Oxt 4a from Oxyopes takobius spider venoms we performed coarse-grained molecular dynamics simulations of these peptides in the presence of lipid bilayers, mimicking erythrocyte membranes. This identified hemolytically active fragments within Oxt 4a and latarcins. Then, we synthesized five 20-residue peptides, containing different parts of the Oxt 4a and latarcin-1 sequence, carrying mutations within the identified regions...
September 14, 2018: Future Medicinal Chemistry
Anja Kolarič, Nikola Minovski
No abstract text is available yet for this article.
September 14, 2018: Future Medicinal Chemistry
Nikhil Shri Sahajpal, Alka Chaubey, Rajesh Kumar Goel, Subheet Kumar Jain
No abstract text is available yet for this article.
September 14, 2018: Future Medicinal Chemistry
Livia Neves Borgheti-Cardoso, Xavier Fernàndez-Busquets
No abstract text is available yet for this article.
September 14, 2018: Future Medicinal Chemistry
Adnan A Bekhit, Manal N Saudi, Ahmed Mm Hassan, Salwa M Fahmy, Tamer M Ibrahim, Doaa Ghareeb, Aya M El-Seidy, Sayed M Al-Qallaf, Huda J Habib, Alaa El-Din A Bekhit
AIM: Novel open chain and cyclized derivatives containing pyrazole scaffold were designed, synthesized and evaluated as antileishmanial compounds. Methodology & results: In silico reverse docking experiment suggested Leishmania major pteridine reductase (Lm-PTR1) as a putative target for the synthesized compounds. In vitro antileishmanial screening against L. major promastigotes and amastigotes using miltefosine and amphotericin B as references showed that the majority of the compounds displayed activity higher than miltefosine...
September 14, 2018: Future Medicinal Chemistry
Wei Hou, Siyi Hu, Zhenzhong Su, Qi Wang, Guangping Meng, Tingting Guo, Jie Zhang, Peng Gao
AIM: Acute lung injury is a common clinical syndrome associated with significant morbidity. Myricetin has been demonstrated to inhibit inflammation in a variety of diseases. In this study, we aimed to investigate the protective effects of myricetin on inflammation in lipopolysaccharide-stimulated RAW 264.7 cells and lipopolysaccharide-induced lung injury model. Results/methodology: In this study, we detected the anti-inflammatory effects of myricetin by ELISA, RT-PCR and Western blot, respectively...
August 10, 2018: Future Medicinal Chemistry
Matthew A Sellwood, Mohamed Ahmed, Marwin Hs Segler, Nathan Brown
No abstract text is available yet for this article.
September 1, 2018: Future Medicinal Chemistry
Jaclyn J Renfrow, Michael H Soike, Waldemar Debinski, Shakti H Ramkissoon, Ryan T Mott, Mark B Frenkel, Jann N Sarkaria, Glenn J Lesser, Roy E Strowd
Hypoxia is an important contributor to aggressive behavior and resistance mechanisms in glioblastoma. Upregulation of hypoxia inducible transcription factors (HIFs) is the primary adaptive cellular response to a hypoxic environment. While HIF1α has been widely studied in cancer, HIF2α offers a potentially more specific and appealing target in glioblastoma given expression in glioma stem cells and not normal neural progenitors, activation in states of chronic hypoxia and expression that correlates with glioma patient survival...
September 1, 2018: Future Medicinal Chemistry
Krzysztof Z Łączkowski, Angelika Baranowska-Łączkowska
No abstract text is available yet for this article.
September 1, 2018: Future Medicinal Chemistry
Maryam A Z El-Attar, Rasha Y Elbayaa, Omaima G Shaaban, Nargues S Habib, Abeer E Abdel Wahab, Ibrahim A Abdelwahab, Soad A M El-Hawash
AIM: The development of a new class of antimicrobial agents is the optimal lifeline to scrap the escalating jeopardy of drug resistance. EXPERIMENTAL: This study aims to design and synthesize a series of pyrazolo-1,2,4-triazolo[4,3-a]quinoxalines, to develop agents having antimicrobial activity through potential inhibition of dihyropteroate synthase enzyme. The target compounds have been evaluated for their in-vitro antimicrobial activity. RESULTS & DISCUSSION: Compounds 5b, 5c were equipotent (minimal inhibitory concentration = 12...
September 1, 2018: Future Medicinal Chemistry
Maria A Soldatkina, Vitalii V Klochko, Svitlana D Zagorodnya, Sunelle Rademan, Michelle H Visagie, Maphuti T Lebelo, Mokgadi V Gwangwa, Anna M Joubert, Namrita Lall, Oleg N Reva
AIM: To determine the computer-predicted anticancer activity of antibiotic batumin. MATERIALS & METHODS: Cytotoxicity assays, cell morphology microscopy and cell cycle progression were studied in cancer and nontumorigenic cell lines. An in vivo experiment on Lewis lung carcinoma (3LL)-transplanted mice was conducted to evaluate potential antimetastatic. RESULTS & CONCLUSION: Cytotoxicity against melanoma and lung carcinoma cells (IC50 ≈ 5 μg/ml) was detected...
September 1, 2018: Future Medicinal Chemistry
Martin Andrs, Monika Pospisilova, Martina Seifrtova, Radim Havelek, Ales Tichy, Katerina Vejrychova, Michaela Polednikova, Lukas Gorecki, Daniel Jun, Jan Korabecny, Martina Rezacova
AIM: DNA damage response plays an eminent role in patients' response to conventional chemotherapy and radiotherapy. Its inhibition is of great interest as it can overcome cancer cell resistance and reduce the effective doses of DNA damaging agents. Results & methodology: We have focused our research on phosphatidylinositol 3-kinase-related kinases and prepared 35 novel compounds through a scaffold hopping approach. The newly synthesized inhibitors were tested on a panel of nine cancer and one healthy cell lines alone and in combination with appropriate doses of doxorubicin...
September 1, 2018: Future Medicinal Chemistry
Etyene Jg Silva, Adriana Bezerra-Souza, Luiz Fd Passero, Márcia D Laurenti, Gláucio M Ferreira, Drielli Gv Fujii, Gustavo Hg Trossini, Cristiano Raminelli
AIM: Considering the epidemiology of leishmaniasis, the emergence of resistant parasites to the approved drugs, and severe clinical manifestations, the development of novel leishmanicidal molecules has become of considerable importance. RESULTS: In this work, three commercially available and 19 synthesized quinoline derivatives were evaluated against promastigote and amastigote forms of Leishmania (Leishmania) amazonensis. In addition, structural parameters and molecular electrostatic potentials were obtained by theoretical calculations, allowing statistical (principal component analyses and hierarchical cluster analyses) and comparative (molecular electrostatic potentials vs leishmanicidal activities) studies, respectively...
September 1, 2018: Future Medicinal Chemistry
Wen-Jun Xue, Ming-Tao Li, Lin Chen, Li-Ping Sun, Yu-Yan Li
FGFs and their receptors (FGFRs) are critical for many biologic processes, including angiogenesis, wound healing and tissue regeneration. Aberrations in FGFR signaling are common in cancer, making FGFRs a promising target in antitumor studies. To date, many FGFR inhibitors are being detected in clinical studies, and resistance to some inhibitors has emerged. Understanding the mechanisms of resistance is a fundamental step for further implementation of targeted therapies. In this review, we will describe the basic knowledge regarding FGF/FGFR signaling and categorize the clinical FGFR inhibitors...
September 1, 2018: Future Medicinal Chemistry
Kush Patel, Zainab So Ahmed, Xuemei Huang, Qianqian Yang, Elmira Ekinci, Christine M Neslund-Dudas, Bharati Mitra, Fawzy Aem Elnady, Young-Hoon Ahn, Huanjie Yang, Jinbao Liu, Qing Ping Dou
The ubiquitin proteasome system has been validated as a target of cancer therapies evident by the US FDA approval of anticancer 20S proteasome inhibitors. Deubiquitinating enzymes (DUBs), an essential component of the ubiquitin proteasome system, regulate cellular processes through the removal of ubiquitin from ubiquitinated-tagged proteins. The deubiquitination process has been linked with cancer and other pathologies. As such, the study of proteasomal DUBs and their inhibitors has garnered interest as a novel strategy to improve current cancer therapies, especially for cancers resistant to 20S proteasome inhibitors...
September 1, 2018: Future Medicinal Chemistry
Yi Jer Tan, Yeuan Ting Lee, Keng Yoon Yeong, Sven H Petersen, Koji Kono, Soo Choon Tan, Chern Ein Oon
AIM: This study aims to investigate the mode of action of a novel sirtuin inhibitor (BZD9L1) and its associated molecular pathways in colorectal cancer (CRC) cells. MATERIALS & METHODS: BZD9L1 was tested against metastatic CRC cell lines to evaluate cytotoxicity, cell cycle and apoptosis, senescence, apoptosis related genes and protein expressions, as well as effect against major cancer signaling pathways. RESULTS & CONCLUSION: BZD9L1 reduced the viability, cell migration and colony forming ability of both HCT 116 and HT-29 metastatic CRC cell lines through apoptosis...
September 1, 2018: Future Medicinal Chemistry
Alejandro Speck-Planche
No abstract text is available yet for this article.
September 1, 2018: Future Medicinal Chemistry
Silvia Franchini, Leda Ivanova Bencheva, Umberto Maria Battisti, Annalisa Tait, Claudia Sorbi, Paola Fossa, Elena Cichero, Simone Ronsisvalle, Giuseppina Aricò, Nunzio Denora, Rosa Maria Iacobazzi, Antonio Cilia, Lorenza Pirona, Livio Brasili
AIM: Targeting 5-HT1A receptor (5-HT1A R) as a strategy for CNS disorders and pain control. METHODOLOGY: A series of 1,3-dioxolane-based 2-heteroaryl-phenoxyethylamines was synthesized by a convergent approach and evaluated at α1 -adrenoceptors and 5-HT1A R by binding and functional experiments. Absorption, distribution, metabolism, excretion and toxicity prediction studies were performed to explore the drug-likeness of the compounds. RESULTS & CONCLUSION: The most promising compound, the pyridin-4-yl derivative, emerged as a potent and selective 5-HT1A R agonist (pKi = 9...
September 1, 2018: Future Medicinal Chemistry
Theodora Chatzisideri, George Leonidis, Vasiliki Sarli
There is a growing interest for the discovery of new cancer-targeted delivery systems for drug delivery and diagnosis. A synopsis of the bibliographic data will be presented on bombesin, neurotensin, octreotide, Arg-Gly-Asp, luteinizing hormone-releasing hormone and other peptides. Many of them have reached the clinics for therapeutic or diagnostic purposes, and have been utilized as carriers of known cytotoxic agents such as doxorubicin, paclitaxel, cisplatin, methotrexate or dyes and radioisotopes. In our article, recent advances in the development of peptides as carriers of cytotoxic drugs or radiometals will be analyzed...
September 1, 2018: Future Medicinal Chemistry
Shuaishi Gao, Luhua Lai
No abstract text is available yet for this article.
September 1, 2018: Future Medicinal Chemistry
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