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Medicinal Chemistry

Volume 15, 8 Issues, 2019
ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)
This journal supports open access

Articles Ahead of Print

Discovery and Optimization of a Series of Sulfonamide Inverse Agonists for the Retinoic Acid Receptor-related Receptor-α


Christelle Doebelin, Yuanjun He, Sean Campbell, Philippe Nuhant, Naresh Kumar, Marcel Koenig, Ruben Garcia-Ordonez, Mi Ra Chang, William R. Roush, Li Lin, Susan Kahn, Michael D. Cameron, Patrick R. Griffin, Laura A. Solt* and Theodore M. Kamenecka*


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Design, Synthesis, and Biological Evaluation of Novel C5-Modified Pyrimidine Ribofuranonucleosides as Potential Antitumor or/and Antiviral Agents


Nikolaos Kollatos, Christos Mitsos, Stella Manta, Niki Tzioumaki, Christos Giannakas, Tania Alexouli, Aggeliki Panagiotopoulou, Dominique Schols, Graciela Andrei and Dimitri Komioti*


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Discovery of N-phenyl-4-(1H-pyrrol-3-yl)pyrimidin-2-amine Derivatives as Potent Mnk2 Inhibitors: Design, Synthesis, SAR Analysis, and Evaluation of in vitro Anti-leukaemic Activity


Ahmed M. Abdelaziz, Sarah Diab, Saiful Islam, Sunita K. C. Basnet, Ben Noll, Peng Li, Laychiluh B. Mekonnen, Jingfeng Lu, Hugo Albrecht, Robert W. Milne, Cobus Gerber, Mingfeng Yu * and Shudong Wang*


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Synthesis, Plasmodium falciparum Inhibitory Activity, Cytotoxicity and Solubility of N2,N4-Disubstituted Quinazoline-2,4-diamines


Nattakarn Pobsuk, Praphasri Suphakun, Supa Hannongbua, Chanin Nantasenamat, Kiattawee Choowongkomon and M. Paul Gleeson*


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Synthesis, Molecular Modelling and Biological Studies of 3-hydroxypyrane- 4-one and 3-hydroxy-pyridine-4-one Derivatives as HIV-1 Integrase Inhibitors


Hajar Sirous, Afshin Fassihi*, Simone Brogi*, Giuseppe Campiani, Frauke Christ, Zeger Debyser, Sandra Gemma, Stefania Butini, Giulia Chemi, Alessandro Grillo, Rezvan Zabihollahi, Mohammad R. Aghasadeghi, Lotfollah Saghaie and Hamid R. Memarian


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Benzoylthioureas: Design, Synthesis and Antimycobacterial Evaluation


Tiago O. Brito, Lethícia O. Abreu, Karen M. Gomes, Maria C. S. Lourenço, Patricia M. L. Pereira, Sueli F. Yamada-Ogatta, Ângelo de Fàtima, Cesar A. Tisher, Fernando Macedo and Marcelle L. F. Bispo*


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Structure Activity Relationship of 4-Amino-2-thiopyrimidine Derivatives as Platelet Aggregation Inhibitors


Barbara Cacciari*, Pamela Crepaldi, Chun Yan Cheng, Elena Bossi , Giampiero Spalluto, Stephanie Federico, Kenneth A. Jacobson and Marco Cattaneo


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The Substantial Improvement of Amphotericin B Selective Toxicity Upon Modification of Mycosamine with Bulky Substituents


Edward Borowski, Natalia Salewska, Joanna Boros-Majewska, Marcin Serocki, Izabela Chabowska, Maria J. Milewska, Dominik Ziętkowski and Sławomir Milewski*


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New Quinazoline-Sulfonylurea Conjugates: Design, Synthesis and Hypoglycemic Activity


Sahar M. Abou-Seri, AlShaimaa M. Taha, Mona A. Mohamed* and Nour M. Abdelkader


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Synthesis and Biological Studies of New Multifunctional Curcumin Platforms for Anticancer Drug Delivery


Andrii Bazylevich , Helena Tuchinsky, Eti Zigman-Hoffman, Ran Weissman , Ofer Shpilberg , Oshrat Hershkovitz-Rokah, Leonid Patsenker and Gary Gellerman*


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Design, Synthesis and In Vitro Evaluation of Novel Anti-HIV 3-Pyrazol-3- yl-Pyridin-2-One Analogs


Sanjay Kumar, Shiv Gupta, Shraddha Gaikwad, Leila Fotooh Abadi, Late Kamlesh Kumar Bhutani, Smita Kulkarni* and Inder Pal Singh*


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Efficacy of Novel Schiff base Derivatives as Antifungal Compounds in Combination with Approved Drugs Against Candida Albicans


Manzoor Ahmad Malik, Shabir Ahmad Lone, Parveez Gull, Ovas Ahmad Dar, Mohmmad Younus Wani, Aijaz Ahmad* and Athar Adil Hashmi*


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The Inhibition of Polysialyltranseferase ST8SiaIV Through Heparin Binding to Polysialyltransferase Domain (PSTD)


Li-Xin Peng, Xue-Hui Liu, Bo Lu, Si-Ming Liao, Feng Zhou, Ji-Min Huang, Dong Chen, Frederic A. Troy II, Guo-Ping Zhou* and Ri-Bo Huang*


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The Multiple Applications and Possible Mechanisms of the Hyperbaric Oxygenation Therapy


Wan Chen, Xingmei Liang , Zhihuan Nong, Yaoxuan Li, Xiaorong Pan, Chunxia Chen * and Luying Huang*


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Inhibition of α-amylase Activity by Zn2+: Insights from Spectroscopy and Molecular Dynamics Simulations


Si-Ming Liao, Nai-Kun Shen, Ge Liang, Bo Lu, Zhi-Long Lu, Li-Xin Peng, Feng Zhou, Li-Qin Du, Yu-Tuo Wei, Guo-Ping Zhou* and Ri-Bo Huang*


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Design and Synthesis of Novel Sulfonamide-Derived Triazoles and Bioactivity Exploration


Shi-Chao He, Hui-Zhen Zhang*, Hai-Juan Zhang, Qing Sun and Cheng-He Zhou


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Novel Conjugated Unsaturated Ketones with Submicromolar Potencies Towards some Leukemic and Colon Cancer Cells


Swagatika Das, H. Inci Gul, Umashankar Das*, Jan Balzarini, Stephen G. Dimmock and Jonathan R. Dimmock *


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Phenolic Imidazole Derivatives with Dual Antioxidant/Antifungal Activity: Synthesis and Structure-Activity Relationship


Ana P. Bettencourt, Marian Castro, Joao P. Silva, Francisco Fernandes, Olga P. Coutinho, Maria J. Sousa, M. Fernanda Proenca* and Filipe M. Areias*


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Pyrrolopyrazoles: Synthesis, Evaluation and Pharmacological Screening as Antidepressant Agents


Samar Said Fatahala*, Shahira Nofal, Eman Mahmoud and Rania Helmy Abd El-hameed


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Synthesis and Evaluation of Antifungal and Antitrypanosomastid Activities of Symmetrical 1,4-Disubstituted-1,2,3-Bistriazoles Obtained by CuAAC Conditions


Mauricio M. Victor*, Ravir R. Farias, Danielle L. da Silva, Paulo Henrique Fonseca do Carmo, Maria A. de Resende-Stoianoff, Claudio Viegas, Patricia F. Espurie and Marcos J. Marquese


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Synthesis, Anti-Varicella-Zoster Virus and Anti-Cytomegalovirus Activity of 4,5-Disubstituted 1,2,3-(1H)-Triazoles


Wei-yuan Yuan, Xue Chen, Ning-ning Liu, Yi-ning Wen, Bei Yang, Graciela Andrei, Robert Snoeck, Yu-hong Xiang, Yong-wei Wu, Zhen Jiang, Dominique Schols, Zhuo-yong Zhang and Qin-pei Wu*


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Synthesis and Biological Evaluation of Acridine/Acridone Analogs as Potential Anticancer Agents


Monika Gensicka-Kowalewska, Mirosława Cichorek, Anna Ronowska, Milena Deptuła, Ilona Klejbor and Krystyna Dzierzbicka*


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Evaluation of Antiplasmodial Potential of C-2 and C-8 Modified Quinolines: in vitro and in silico Study


Rakesh Kumar, Ritika Sharma, Inder Kumar, Pooja Upadhyay, Ankit Kumar Dhiman, Rohit Kumar, Rakesh Kumar, Rituraj Purohit*, Dinkar Sahal* and Upendra Sharma*


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Design, Synthesis, Antimicrobial and Anti-biofilm Evaluation, and Molecular Docking of Newly Substituted Fluoroquinazolinones


Mohamed F. Zayed, Sabrin R.M. Ibrahim*, EL-Sayed E. Habib, Memy H. Hassan, Sahar Ahmed and Heba S. Rateb


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Synthesis and Biological Evaluation of Polyfluoroalkylated Antipyrines and their Isomeric O-Methylpyrazoles


Natalya Agafonova, Evgeny Shchegolkov*, Yanina Burgart, Victor Saloutin, Alexandra Trefilova, Galina Triandafilova, Sergey Solodnikov, Vera Maslova, Sophia Borisevich, Olga Krasnykh and Sergey Khursan


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Antiprotozoal Activities of Tetrazole-quinolines with Aminopiperidine Linker


Patrick Hochegger, Johanna Faist, Werner Seebacher, Robert Saf, Pascal Mäser, Marcel Kaiser and Robert Weis*


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Rational Design of Colchicine Derivatives as anti-HIV Agents via QSAR and Molecular Docking


Apilak Worachartcheewan*, Napat Songtawee, Suphakit Siriwong, Supaluk Prachayasittikul*, Chanin Nantasenamat and Virapong Prachayasittikul


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Ligand-Based Drug Design: Synthesis and Biological Evaluation of Substituted Benzoin Derivatives as Potential Antitumor Agents


Dima A. Sabbah*, Ameerah Hasan Ibrahim, Wamidh H. Talib, Khalid M. Alqaisi, Kamal Sweidan, Sanaa K. Bardaweel, Ghassan Abu Sheikha, Haizhen A. Zhong, Eveen Al-Shalabi, Reema Abu Khalaf and Mohammad S. Mubarak


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New N,C-Diaryl-1,2,4-triazol-3-ones: Synthesis and Evaluation as Anticancer Agents


Dolores Santa Maria*, Rosa M. Claramunt, Jose Elguero, Miguel Carda, Eva Falomir and Celia Martin-Beltran


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Anticancer Activity and Topoisomerase II Inhibition of Naphthalimides with ω-Hydroxylalkylamine Side-Chains of Different Lengths


Mateusz D. Tomczyk, Anna Byczek Wyrostek, Klaudia Strama, Martyna Wawszków, Przemysław Kasprzycki and Krzysztof Z. Walczak*


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