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European Journal of Medicinal Chemistry

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https://www.readbyqxmd.com/read/29146136/identification-of-highly-potent-btk-and-jak3-dual-inhibitors-with-improved-activity-for-the-treatment-of-b-cell-lymphoma
#1
Yang Ge, Changyuan Wang, Shijie Song, Jiaxin Huang, Zhihao Liu, Yongming Li, Qiang Meng, Jianbin Zhang, Jihong Yao, Kexin Liu, Xiaodong Ma, Xiuli Sun
The BTK and JAK3 receptor tyrosine kinases are two validated and therapeutically amenable targets in the treatment of B-cell lymphomas. Here we report the identification of several classes of pyrimidine derivatives as potent BTK and JAK3 dual inhibitors. Among these molecules, approximately two thirds displayed strong inhibitory capacity at less than 10 nM concentration, and four compounds (7e, 7g, 7m and 7n) could significantly inhibit the phosphorylation of BTK and JAK3 enzymes at concentrations lower than 1 nM...
November 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29137867/functionalized-2-1-benzothiazine-2-2-dioxides-as-new-inhibitors-of-dengue-ns5-rna-dependent-rna-polymerase
#2
Rolando Cannalire, Delia Tarantino, Andrea Astolfi, Maria Letizia Barreca, Stefano Sabatini, Serena Massari, Oriana Tabarrini, Mario Milani, Gilles Querat, Eloise Mastrangelo, Giuseppe Manfroni, Violetta Cecchetti
Over recent years, many RNA viruses have been "re-discovered", including life-threatening flaviviruses, such as Dengue, Zika, and several encephalitis viruses. Since no specific inhibitors are currently available to treat these infections, there is a pressing need for new therapeutics. Among the flaviviral proteins, NS5 RNA-dependent RNA polymerase (RdRp) represents a validated target being essential for viral replication and it has no human analog. To date, few NS5 RdRp inhibitor chemotypes have been reported and no inhibitors are currently in clinical development...
November 11, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133056/therapeutic-potential-of-songorine-a-diterpenoid-alkaloid-of-the-genus-aconitum
#3
REVIEW
Haroon Khan, Seyed Mohammad Nabavi, Antoni Sureda, Nikolay Mehterov, Diana Gulei, Ioana Berindan-Neagoe, Hiroaki Taniguchi, Atanas G Atanasov
Alkaloids are well-studied secondary metabolites, with recent preclinical studies evidencing that many of them exhibit anti-cancer, anti-depressant, anti-nociceptive, anti-inflammatory, anti-pyretic, anti-platelet, anti-oxidant, and anti-bacterial properties. Aconitum is a genus rich of diverse alkaloids. More than 450 alkaloids have been identified in a variety of species. Songorine is a C20 diterpenoid alkaloid and 12-keto analog of napelline, isolated from Aconitum soongaricum and was associated with a heterogeneous panel of biological functions...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133053/synthesis-and-biological-evaluation-of-new-berberine-derivatives-as-cancer-immunotherapy-agents-through-targeting-ido1
#4
Yan-Xiang Wang, Wei-Qiang Pang, Qing-Xuan Zeng, Zhe-Song Deng, Tian-Yun Fan, Jian-Dong Jiang, Hong-Bin Deng, Dan-Qing Song
To discover small-molecule cancer immunotherapy candidates through targeting Indoleamine 2,3-dioxygenase 1 (IDO1), twenty-five new berberine (BBR) derivatives defined with substituents on position 3 or 9 were synthesized and examined for repression of IFN-γ-induced IDO1 promoter activities. Structure-activity relationship (SAR) indicated that large volume groups at the 9-position might be beneficial for potency. Among them, compounds 2f, 2i, 2n, 2o and 8b exhibited increased activities, with inhibition rate of 71-90% compared with BBR...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133052/design-and-synthesis-of-short-amphiphilic-cationic-peptidomimetics-based-on-biphenyl-backbone-as-antibacterial-agents
#5
Rajesh Kuppusamy, Muhammad Yasir, Thomas Berry, Charles G Cranfield, Shashidhar Nizalapur, Eugene Yee, Onder Kimyon, Aditi Taunk, Kitty K K Ho, Bruce Cornell, Mike Manefield, Mark Willcox, David StC Black, Naresh Kumar
Antimicrobial peptides (AMPs) and their synthetic mimics have received recent interest as new alternatives to traditional antibiotics in attempts to overcome the rise of antibiotic resistance in many microbes. AMPs are part of the natural defenses of most living organisms and they also have a unique mechanism of action against bacteria. Herein, a new series of short amphiphilic cationic peptidomimetics were synthesized by incorporating the 3'-amino-[1,1'-biphenyl]-3-carboxylic acid backbone to mimic the essential properties of natural AMPs...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133046/design-synthesis-and-biological-evaluation-of-novel-benzimidazole-amidines-as-potent-multi-target-inhibitors-for-the-treatment-of-non-small-cell-lung-cancer
#6
Andrea Bistrović, Luka Krstulović, Anja Harej, Petra Grbčić, Mirela Sedić, Sanja Koštrun, Sandra Kraljević Pavelić, Miroslav Bajić, Silvana Raić-Malić
A series of novel amidino 2-substituted benzimidazoles linked to 1,4-disubstituted 1,2,3-triazoles were synthesized by implementation of microwave and ultrasound irradiation in click reaction and subsequent condensation of thus obtained 4-(1,2,3-triazol-1-yl)benzaldehyde with o-phenylenediamines. In vitro antiproliferative screening of compounds performed on human cancer cell lines revealed that p-chlorophenyl-substituted 1,2,3-triazolyl N-isopropylamidine 10c and benzyl-substituted 1,2,3-triazolyl imidazoline 11f benzimidazoles had selective and potent cytostatic activities in the low nM range against non-small cell lung cancer cell line A549, which could be attributed to induction of apoptosis and primary necrosis...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133044/molecular-docking-design-synthesis-and-antifungal-activity-study-of-novel-triazole-derivatives
#7
Junqi Wu, Tingjunhong Ni, Xiaoyun Chai, Ting Wang, Hongrui Wang, Jindong Chen, Yongsheng Jin, Dazhi Zhang, Shichong Yu, Yuanying Jiang
The incidence of life-threatening fungal infections has dramatically increased for decades. In order to develop novel antifungal agents, two series of (2R,3R)-1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(N-substitutied)-2-butanols (3a-o, 5a-f, 8a-u), which were analogues of voriconazole, were designed, synthesized and characterized by (1)H NMR, (13)C NMR and HRMS. The MIC80 values showed that the target compounds 3a-o indicated better activities than fluconazole on three important fungal pathogens except for 3i...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133041/design-synthesis-and-biological-evaluation-of-novel-aryldiketo-acids-with-enhanced-antibacterial-activity-against-multidrug-resistant-bacterial-strains
#8
Ilija N Cvijetić, Tatjana Ž Verbić, Pedro Ernesto de Resende, Paul Stapleton, Simon Gibbons, Ivan O Juranić, Branko J Drakulić, Mire Zloh
Antimicrobial resistance (AMR) is a major health problem worldwide, because of ability of bacteria, fungi and viruses to evade known therapeutic agents used in treatment of infections. Aryldiketo acids (ADK) have shown antimicrobial activity against several resistant strains including Gram-positive Staphylococcus aureus bacteria. Our previous studies revealed that ADK analogues having bulky alkyl group in ortho position on a phenyl ring have up to ten times better activity than norfloxacin against the same strains...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133040/synthesis-and-biological-evaluation-of-novel-alkylated-polyamine-analogues-as-potential-anticancer-agents
#9
Meng Li, Yuxia Wang, Chaochao Ge, Liping Chang, Chaojie Wang, Zhiyong Tian, Senzhen Wang, Fujun Dai, Luyao Zhao, Songqiang Xie
A new class of polyamine analogues modified by alkylation at the terminal of the polyamine chain has been synthesized and their structures were determined by (1)H NMR, (13)C NMR, ESI-MS and elemental analysis. As the representative compound, 3f displayed a broad spectrum of anti-cancer effects by MTT assays. Tumor xenograft model and pulmonary metastasis model showed that compound 3f significantly suppressed tumor growth and metastasis in vivo, which was more stronger than the reference drug amonafide. Molecular mechanisms indicated that compound 3f exhibited antiproliferative activities and induced the generation of reactive oxygen species (ROS), which resulted in the occurrence of autophagy...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133038/new-metalo-therapeutics-of-nsaids-against-human-breast-cancer-cells
#10
Christina N Banti, Constantina Papatriantafyllopoulou, Anastasios J Tasiopoulos, Sotiris K Hadjikakou
The non steroidal anti-inflammatory drugs (NSAID's)-silver(I) metallodrugs of aspirin (aspH), salicylic acid (salH2), naproxen (napH) acid or p-hydrobenzoic acid (pHbzaH) and the mitochondriotropic triphenylarsine (tpAs) with the formulae [Ag(asp)(tpAs)3] (1), [Ag(salH)(tpAs)3] (2), [Ag(nap)(tpAs)3] (3) and {[Ag(pHbza)(tpAs)3]∙(dmf)} (4) and [Ag(tpAs)3(NO3)] (5) have been synthesized and characterized by m.p., FT-IR, UV-vis and (1)H NMR, spectroscopic techniques and X-ray crystallography. The in vitro cytotoxic activity of 1-5 against human breast adenocarcinoma cancer cells: MCF-7 (positive to estrogen receptors (ERs)) and MDA-MB-231 (negative to estrogen receptors (ERs)) was evaluated...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133036/1-2-4-thiadiazolidin-3-5-diones-as-novel-hydrogen-sulfide-donors
#11
Beatrice Severino, Angela Corvino, Ferdinando Fiorino, Paolo Luciano, Francesco Frecentese, Elisa Magli, Irene Saccone, Paola Di Vaio, Valentina Citi, Vincenzo Calderone, Luigi Servillo, Rosario Casale, Giuseppe Cirino, Valentina Vellecco, Mariarosaria Bucci, Elisa Perissutti, Vincenzo Santagada, Giuseppe Caliendo
Hydrogen sulfide (H2S) is an endogenous modulator that plays significant physio-pathological roles in several biological systems. In this research field there is a large interest in developing selective CBS and CSE inhibitors and H2S releasing moieties, that could be either used as therapeutic agents or linked to known drugs. One of the major problem is the limited availability of chemicals that ensure a controlled release of H2S in vitro as well in vivo. Aiming to obtain novel H2S donors, whose release properties could be appropriately modulated, we have synthesized a series of 1,2,4-thiadiazolidine-3,5-diones (THIA 1-10) as innovative donors that could release H2S in controlled manner...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29150335/camptothecin-psammaplin-a-hybrids-as-topoisomerase-i-and-hdac-dual-action-inhibitors
#12
Raffaella Cincinelli, Loana Musso, Roberto Artali, Mario Guglielmi, Erminia Bianchino, Francesco Cardile, Fabiana Colelli, Claudio Pisano, Sabrina Dallavalle
Recent studies have demonstrated enhanced anticancer effects of combination therapy consisting of camptothecin derivatives and HDAC inhibitors. To exploit this synergy in a single active compound, we designed new dual-acting multivalent molecules simultaneously targeting topoisomerase I and HDAC. In particular, a selected compound containing a camptothecin and the psammaplin A scaffold showed a broad spectrum of antiproliferative activity, with IC50 values in the nanomolar range. Preliminary in vivo results indicated a strong antitumor activity on human mesothelioma primary cell line MM473 orthotopically xenografted in CD-1 nude mice and very high tolerability...
November 8, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29146133/synthesis-and-bio-evaluation-of-indole-chalcone-based-benzopyrans-as-promising-antiligase-and-antiproliferative-agents
#13
Sampa Gupta, Pooja Maurya, Akanksha Upadhyay, Pragati Kushwaha, Shagun Krishna, Mohammad Imran Siddiqi, Koneni V Sashidhara, Dibyendu Banerjee
DNA replication and repair are complex processes accomplished by the concerted action of a network of enzymes and proteins. DNA ligases play a crucial role in these processes by catalyzing the nick joining between DNA strands. As compared to normal cells, elevated levels of human DNA ligase I (hLigI) is reported in some cancers. We studied the inhibition of hLigI mediated DNA nick sealing activity followed by the antiproliferative activity of novel indole-chalcone based benzopyran compounds on cancer cells...
November 7, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29129512/thieno-2-3-b-pyridine-derivatives-are-potent-anti-platelet-drugs-inhibiting-platelet-activation-aggregation-and-showing-synergy-with-aspirin
#14
Naif K Binsaleh, Catherine A Wigley, Kathryn A Whitehead, Michelle van Rensburg, Johannes Reynisson, Lisa I Pilkington, David Barker, Sarah Jones, Nina C Dempsey-Hibbert
Drugs which inhibit platelet function are commonly used to prevent blood clot formation in patients with Acute Coronary Syndromes (ACS) or those at risk of stroke. The thieno[3,2-c]pyridine class of therapeutic agents, of which clopidogrel is the most commonly used, target the P2Y12 receptor, and are often used in combination with acetylsalicylic acid (ASA). Six thieno[2,3-b]pyridine were assessed for in vitro anti-platelet activity; all derivatives showed effects on both platelet activation and aggregation, and showed synergy with ASA...
November 7, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133061/design-synthesis-and-cytotoxic-activity-of-n-modified-oleanolic-saponins-bearing-a-glucosamine
#15
You-Yu Lin, She-Hung Chan, Yu-Pu Juang, Hsin-Min Hsiao, Jih-Hwa Guh, Pi-Hui Liang
A series of N-acyl, N-alkoxycarbonyl, and N-alkylcarbamoyl derivatives of 2'-deoxy-glucosyl bearing oleanolic saponins were synthesized and evaluated against HL-60, PC-3, and HT29 tumor cancer cells. The SAR studies revealed that the activity increased in order of conjugation of 2' -amino group with carbamate > amide > urea derivatives. Lengthening the alkyl chain increased the cytotoxicity, the peak activity was found to around heptyl to nonyl substitutions. 2'-N-heptoxycarbonyl derivative 56 was found to be the most cytotoxic (IC50 = 0...
November 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133049/design-and-synthesis-of-novel-c14-urea-tetrandrine-derivatives-with-potent-anti-cancer-activity
#16
Junjie Lan, Lan Huang, Huayong Lou, Chao Chen, Tangjingjun Liu, Shengcao Hu, Yao Yao, Junrong Song, Jun Luo, Yazhou Liu, Bin Xia, Lei Xia, Xueyi Zeng, Yaacov Ben-David, Weidong Pan
Tetrandrine is a dibenzyltetrahydroisoquinoline alkaloid, isolated from traditional Chinese medicinal plant Stephania tetrandra, with anti-tumor activity. Our previous study identified several derivatives of tetrandrine showing better activities than parental compound against human hepatocellular carcinoma cells. To increase diversity and cytotoxic activities of the original compound, a series of novel 14-urea-tetrandrine derivatives were synthesized through structural modification of tetrandrine. These derivaties demonstrated a moderate to strong anti-proliferative activities against human cell lines HEL and K562 (Leukemia), prostate (PC3), breast (MDA-MB-231) and melanoma (WM9)...
November 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133051/design-synthesis-and-preliminary-biological-evaluation-of-5-8-dihydropteridine-6-7-diones-that-induce-apoptosis-and-suppress-cell-migration
#17
Peng-Fei Geng, Cong-Cong Wang, Zhong-Hua Li, Xiao-Ning Hu, Tao-Qian Zhao, Dong-Jun Fu, Bing Zhao, Bin Yu, Hong-Min Liu
Pteridines are an important class of fused heterocycles found in natural products and drug molecules, and have shown diverse biological activities. A focused library of 5,8-dihydropteridine-6,7-dione derivatives were designed and evaluated for their antiproliferative activity against MGC-803, SGC-7901, A549 and PC-3 cancer cell lines. The SARs studies highlighted the importance of the piperazine substituted 5,8-dihydropteridine-6,7-dione frameworks for the activity and revealed essential structural elements...
November 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29146134/novel-2-2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl-1-1-3-5-triazin-2-ylamino-guanidine-derivatives-inhibition-of-human-carbonic-anhydrase-cytosolic-isozymes-i-and-ii-and-the-transmembrane-tumor-associated-isozymes-ix-and-xii-anticancer-activity-and-molecular
#18
Beata Żołnowska, Jarosław Sławiński, Krzysztof Szafrański, Andrea Angeli, Claudiu T Supuran, Anna Kawiak, Miłosz Wieczór, Joanna Zielińska, Tomasz Bączek, Sylwia Bartoszewska
A series of novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(6-substituted-4-chloro-1,3,5-triazin-2-ylamino)guanidine derivatives 9-20 have been synthesized by substitution of chlorine atom at the 1,3,5-triazine ring in compounds 5-8 with 3- or 4-aminobenzenesulfonamide and 4-(aminomethyl)benzenesulfonamide hydrochloride. All the synthesized compounds were evaluated for their inhibitory activity toward hCA I, II, IX and XII as well as anticancer activity against HeLa, HCT-116 and MCF-7 human tumor cell lines...
November 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133050/newly-designed-organotin-iv-carboxylates-with-peptide-linkage-synthesis-structural-elucidation-physicochemical-characterizations-and-pharmacological-investigations
#19
Muhammad Sirajuddin, Vickie McKee, Muhammad Tariq, Saqib Ali
Fourteen new organotin(IV) carboxylate complexes with peptide linkage of (2-(4-methoxy-2-nitrophenylcarbamoyl)benzoic acid) were successfully synthesized and characterized by elemental analyses, FT-IR, NMR ((1)H, (13)C and (119)Sn) and single crystal X-ray techniques. FT-IR results of the sodium salt of 2-(4-methoxy-2-nitrophenylcarbamoyl)benzoic acid and complexes showed that the coordination took place via oxygen atoms of the carboxylate group. (1)J((119)Sn-(13)C), (2)J((119)Sn-(1)H) and θ values calculated from (1)H and (13)C NMR data using Lockhart's equation reveal a trigonal bipyramidal geometry for triorganotin(IV) derivatives and an octahedral geometry for diorganotin(IV) derivatives...
November 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29133037/the-novel-4-phenyl-2-phenoxyacetamide-thiazoles-modulates-the-tumor-hypoxia-leading-to-the-crackdown-of-neoangiogenesis-and-evoking-the-cell-death
#20
Yasser Hussein Eissa Mohammed, Vikas H Malojirao, Prabhu Thirusangu, Mohammed Al-Ghorbani, B T Prabhakar, Shaukath Ara Khanum
Tumor microenvironment is a complex multistep event which involves several hallmarks that transform the normal cell into cancerous cell. Designing the novel antagonistic molecule to reverse the tumor microenvironment with specific target is essential in modern biological studies. The novel 4-phenyl-2-phenoxyacetamide thiazole analogues 8a-ab were synthesized in multistep process, then screened and assessed for cytotoxic and anti-proliferative effects in vitro against multiple cancer cells of different origin such as MCF-7, A549, EAC and DLA cells which revealed that compound 8f with fluoro and methyl substitute has potential cytotoxic efficacy with an average IC50 value of ˜ 13 μM...
November 4, 2017: European Journal of Medicinal Chemistry
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