MedChemComm

Revisiting amino acids and peptides as anti-glycation agents ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00514H, Review Article H. Chilukuri, M. J. Kulkarni, M. Fernandes The importance of amino acids and peptides in countering glycation and the formation of advanced glycation end-products (AGEs) is reviewed. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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The critical role of novel benzophenone analogs on tumor growth inhibition targeting angiogenesis and apoptosis ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C7MD00593H, Research Article Yasser Hussein Eissa Mohammed, Shaukath Ara Khanum In modern biology, one of the major importance is the progress of anti-cancer drugs with specific targets. The angiopreventive and in vitro tumor inhibition activities of novel synthetic benzophenone analogs... The content of this RSS Feed (c) The Royal Society of Chemistry
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Membrane activity profiling of small molecule B. subtilis growth inhibitors utilizing novel duel-dye fluorescence assay ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C8MD00009C, Research Article Scott McAuley, Alan Huynh, Tomasz Czarny, Eric D. Brown, Justin R Nodwell Small molecule disruption of the bacterial membrane is both a challenge and interest for drug development. While some avoid membrane activity due to toxicity issues, others are interested in leveraging... The content of this RSS Feed (c) The Royal Society of Chemistry
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Approaches to target tractability assessment - a practical perspective ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C7MD00633K, Review Article Kris Brown, Mike M Hann, Ami Lakdawala Shah, Rita Santos, Pam J Thomas, Kieran Todd Abstract. The assessment of the suitability of novel targets to intervention by different modalities, e.g. small molecules or antibodies, is increasingly seen as important in helping to select the most... The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis, characterization and biological evaluation of six highly cytotoxic ruthenium(II) complexes with 4[prime or minute]-substituted-2,2[prime or minute]:6[prime or minute],2[prime or minute][prime or minute]-terpyridine ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00532F, Research Article Qi-Pin Qin, Ting Meng, Ming-Xiong Tan, Yan-Cheng Liu, Shu-Long Wang, Bi-Qun Zou, Hong Liang Various experiments show that Ru1 and Ru6 are telomerase inhibitors targeting c-myc G4 DNA and also cause apoptosis of Hep-G2 cells. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Novel Valdecoxib Derivatives by Ruthenium(II)-Promoted 1,3-Dipolar Cycloaddition of Nitrile Oxides with Alkynes - Synthesis and COX-2 Inhibition Activity. ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C7MD00575J, Research Article Silvia Roscales, Nicole Bechmann, Daniel Holger Weiss, Martin Kockerling, Jens Pietzsch, Torsten Kniess Novel valdecoxib-based cyclooxygenase-2 inhibitors were synthesized in one step via 1,3-dipolar cycloaddition of nitrile oxides with a series of eleven aryl alkynes, six of them described for the first time.... The content of this RSS Feed (c) The Royal Society of Chemistry
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Structure-guided design of a potent peptide inhibitor targeting the interaction between CRK and ABL kinase ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00619E, Research Article Qingliang Shen, Veer S. Bhatt, Inna Krieger, James C. Sacchettini, Jae-Hyun Cho CT-10 regulator of kinase (CRK) proteins play important roles in human cancer metastasis and invasion. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Studies towards elucidating the potential of 5,10,15,20-tetrakis(p-carboxymethyleneoxyphenyl)porphyrin as a theranostic agent for applications in PET and PDT ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C7MD00433H, Research Article Mohini Guleria, Chandan Kumar, Tapas Das, Jeyachitra Amirdhanayagam, Rohit Sharma, Haladhar Deb Sarma, Ashutosh Dash Porphyrins, owing to their inherent tendency to accumulate in tumorous lesions, are considered suitable for developing agents for theranostic applications involving tumor diagnosis and targeted tumor therapy. The aim of... The content of this RSS Feed (c) The Royal Society of Chemistry
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Recent updates in the discovery and development of novel antimalarial drug candidates ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00637C, Review Article John Okombo, Kelly Chibale Concerns of emerging resistance and the search for molecules with potential for single exposure radical cure and prophylaxis have spurred research into compounds with target profiles for clinical development into antimalarial drugs. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Membrane-active antimicrobial poly(amino-modified alkyl) [small beta]-cyclodextrins synthesized via click reactions ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00592J, Research Article Hatsuo Yamamura, Miho Nonaka, Shingo Okuno, Ryogo Mitsuhashi, Hisato Kato, Takashi Katsu, Kazufumi Masuda, Koichi Tanimoto, Haruyoshi Tomita, Atsushi Miyagawa The modified cyclodextrins exhibited antimicrobial activity against drug-resistant bacteria and less hemolytic activity. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Exploring eukaryotic versus prokaryotic ribosomal RNA recognition with aminoglycoside derivatives ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD00001H, Research Article Narayana Murthy Sabbavarapu, Tomasz Pienko, Bat-Hen Zalman, Joanna Trylska, Timor Baasov New aminoglycosides containing 6[prime or minute]-carboxylic acid or 6[prime or minute]-amide were designed, synthesized and their ability to readthrough nonsense mutations was examined. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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5,6-Benzoflavones as cholesterol esterase inhibitors: synthesis, biological evaluation and docking studies ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00565B, Research Article Jatinder V. Singh, Anumeet Kaur, Kavita Bhagat, Manish K. Gupta, Manwinder Singh, Harbinder Singh, Preet Mohinder S. Bedi A library of forty 5,6-benzoflavone derivatives was synthesized and evaluated for their inhibitory potential against cholesterol esterase (CEase) enzyme. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Automated synthesis of [68Ga]oxine, improved preparation of 68Ga-labeled erythrocytes for blood-pool imaging, and preclinical evaluation in rodents ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00607A, Research Article Stephen Thompson, Melissa E. Rodnick, Jenelle Stauff, Janna Arteaga, Timothy J. Desmond, Peter J. H. Scott, Benjamin L. Viglianti Radiolabeled erythrocytes have multiple applications in nuclear medicine, including blood pool imaging. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Design, synthesis and biological evaluation of novel 5-hydroxy-2-methyl-4H-pyran-4-one derivatives as antiglioma agents ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00551B, Research Article Yi-Bin Li, Wen Hou, Hui Lin, Ping-Hua Sun, Jing Lin, Wei-Min Chen Two series of 5-hydroxy-2-methyl-4H-pyran-4-one derivatives were synthesized and their antiglioma activities were evaluated. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Design, synthesis and evaluation of (R)-3-(7-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-5-azaspiro[2.4]heptan-5-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00568G, Research Article Chieyeon Chough, Sunmin Lee, Misuk Joung, Jaemin Lee, Jong Hoon Kim, B. Moon Kim We discovered a new JAK1-selective inhibitor with a selectivity index of 48 and identified its efficacy in CIA and AIA models. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Oral drug suitability parameters ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00586E, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. M. C. Wenlock Assessing the oral drug suitability of compounds as early as possible is an important objective in drug discovery. Two new oral drug suitability parameters are proposed to facilitate the ranking of compounds with respect to dose and in vivo exposure. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Correction: Synthesis, characterization and biological application of 5-quinoline 1,3,5-trisubstituted pyrazole based platinum(II) complexes ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD90005A, Correction Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Miral V. Lunagariya, Khyati P. Thakor, Reena R. Varma, Bhargav N. Waghela, Chandramani Pathak, Mohan N. Patel To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Structure-guided approach identifies a novel class of HIV-1 Ribonuclease H inhibitors: Binding mode insights through magnesium complexation and site-directed mutagenesis studies ()
Med. Chem. Commun., 2018, Accepted Manuscript DOI: 10.1039/C7MD00600D, Research Article Vasanthanathan Poongavanam, Angela Corona, Casper Svendsen, Luigi Scipione, Nicole Grandi, Fabiana Pandolfi, Roberto Di Santo, Roberta Costi, Francesca Esposito, Enzo Tramontano, Jacob Kongsted HIV persistent infection requires a life-long treatment and among the 2.1 million new HIV infections that occur every year there is an increased rate of transmitted drug-resistant mutations. This fact... The content of this RSS Feed (c) The Royal Society of Chemistry
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A novel allosteric inhibitor that prevents IKK[small beta] activation ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00599G, Research Article Hongbo Liu, Hao Liang, Hu Meng, Xiaobing Deng, Xiaoling Zhang, Luhua Lai A novel compound binding with inactive IKK[small beta] and allosterically blocking its activation. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Targeting rare diseases ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C8MD90001A, In the Pipeline Is working on genetic mutations that affect only a few in every thousand people a risky strategy? To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Identification of karanjin isolated from the Indian beech tree as a potent CYP1 enzyme inhibitor with cellular efficacy via screening of a natural product repository ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00388A, Research Article Prashant Joshi, Vinay R. Sonawane, Ibidapo S. Williams, Glen J. P. McCann, Linda Gatchie, Rajni Sharma, Naresh Satti, Bhabatosh Chaudhuri, Sandip B. Bharate Karanjin has been identified as CYP1 inhibitor. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Resistance-breaking profiling and gene expression analysis on an organometallic ReI-phenanthridine complex reveal parallel activation of two apoptotic pathways ()
Med. Chem. Commun., 2018, 9,173-180 DOI: 10.1039/C7MD00545H, Research Article Marcel Konig, Daniel Siegmund, Lukasz J. Raszeja, Aram Prokop, Nils Metzler-Nolte Emerging resistances of tumors against multiple anti-cancer agents require compounds with a novel mode of action such as the Re metallodrug candidate studied herein, which activates two apoptotic pathways simultaneously. The content of this RSS Feed (c) The Royal Society of Chemistry
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In depth analysis of kinase cross screening data to identify chemical starting points for inhibition of the Nek family of kinases ()
Med. Chem. Commun., 2018, 9,44-66 DOI: 10.1039/C7MD00510E, Review Article C. I. Wells, N. R. Kapadia, R. M. Counago, D. H. Drewry Potent, selective, and cell active small molecule kinase inhibitors are useful tools to help unravel the complexities of kinase signaling. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and in vitro evaluation of substituted 3-cinnamoyl-4-hydroxy-pyran-2-one (CHP) in pursuit of new potential antituberculosis agents ()
Med. Chem. Commun., 2018, 9,165-172 DOI: 10.1039/C7MD00366H, Research Article Zubair Shanib Bhat, Hafiz Ul Lah, Muzafar Ahmad Rather, Mubashir Maqbool, Tabassum Ara, Zahoor Ahmad, Syed Khalid Yousuf Tuberculosis is an ever-evolving infectious disease that urgently needs new drugs. The content of this RSS Feed (c) The Royal Society of Chemistry
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Strigolactones: a plant phytohormone as novel anti-inflammatory agents ()
Med. Chem. Commun., 2018, 9,181-188 DOI: 10.1039/C7MD00461C, Research Article Jun-Xia Zheng, Yu-Shui Han, Jin-Cai Wang, Hui Yang, Hao Kong, Kang-Jia Liu, Si-Yu Chen, Yi-Rui Chen, Yi-Qun Chang, Wei-Min Chen, Jia-Liang Guo, Ping-Hua Sun Strigolactones (SLs), a representative SL, GR24 and its reductive products of D-ring were synthesized and their anti-inflammatory activities were fully evaluated on both in vitro and in vivo models. The content of this RSS Feed (c) The Royal Society of Chemistry
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Novel cell-penetrating-amyloid peptide conjugates preferentially kill cancer cells ()
Med. Chem. Commun., 2018, 9,121-130 DOI: 10.1039/C7MD00321H, Research Article John R. Veloria, Luxi Chen, Lin Li, Gail A. M. Breen, Jiyong Lee, Warren J. Goux The goal of this study was to develop a peptide which could use the toxic effects of amyloid, a substance which is the hallmark of over 25 known human diseases, to selectively kill cancer cells. The content of this RSS Feed (c) The Royal Society of Chemistry
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Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics ()
Med. Chem. Commun., 2018, 9,160-164 DOI: 10.1039/C7MD00527J, Research Article G. M. L. Consoli, G. Granata, R. Picciotto, A. R. Blanco, C. Geraci, A. Marino, A. Nostro Synthesis of a new polycationic calix[4]arene derivative: intrinsic antibacterial activity and additive effect when combined with antibiotics against ATCC and resistant bacteria. The content of this RSS Feed (c) The Royal Society of Chemistry
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Design, synthesis and biological evaluation of tacrine-1,2,3-triazole derivatives as potent cholinesterase inhibitors ()
Med. Chem. Commun., 2018, 9,149-159 DOI: 10.1039/C7MD00457E, Research Article Gaochan Wu, Yun Gao, Dongwei Kang, Boshi Huang, Zhipeng Huo, Huiqing Liu, Vasanthanathan Poongavanam, Peng Zhan, Xinyong Liu We report herein the design and synthesis of a series of 11 novel tacrine-1,2,3-triazole derivatives via a Cu(I)-catalyzed alkyne-azide 1,3-dipolar cycloaddition (CuAAC) reaction. The content of this RSS Feed (c) The Royal Society of Chemistry
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Rise of the biologics ()
Med. Chem. Commun., 2018, 9,10-11 DOI: 10.1039/C7MD90046E, In the Pipeline Antibodies, RNA and gene therapy don't necessarily compete with small molecule drugs - and they all rely on chemistry. The content of this RSS Feed (c) The Royal Society of Chemistry
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Identification of non-substrate-like glycosyltransferase inhibitors from library screening: pitfalls & hits ()
Med. Chem. Commun., 2018, 9,131-137 DOI: 10.1039/C7MD00550D, Research Article Masaki Ema, Yong Xu, Sebastian Gehrke, Gerd K. Wagner 5-Methyl pyrazol-3-ones are genuine, non-substrate-like inhibitors of the bacterial glycosyltransferase LgtC, but aminosteroids are not. The content of this RSS Feed (c) The Royal Society of Chemistry
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MyD88 in antigen-presenting cells is not required for CD4+ T-cell responses during peptide nanofiber vaccination ()
Med. Chem. Commun., 2018, 9,138-148 DOI: 10.1039/C7MD00367F, Research Article Youhui Si, Yi Wen, Jianjun Chen, Rebecca R. Pompano, Huifang Han, Joel H. Collier, Anita S. Chong Self-assembled peptide nanofiber vaccines trigger redundant MyD88-dependent and MyD88-independent signaling pathways in APCs and T cells. The content of this RSS Feed (c) The Royal Society of Chemistry
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A [small beta]-carboline derivative-based nickel(II) complex as a potential antitumor agent: synthesis, characterization, and cytotoxicity ()
Med. Chem. Commun., 2018, 9,100-107 DOI: 10.1039/C7MD00428A, Research Article Jing-Mei Yang, Yan-Hong Zhu, Sheng Chen, Xing Lu, Yi-Ming Wu, Feng-E Ma, Liang-Ping Li, Yang Yang, Zhen-Hao Shi, Kun-Yuan Huang, Xue Hong, Ping Jiang, Yan Peng A novel nickel(II) complex was synthesized and characterized. It significantly induced cell cycle arrest at S phase, and caused the down-regulation of p-AKT, cyclin E, cyclin A and CDK2 and the up-regulation of p27. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and biological evaluation of rapamycin-derived, next generation small molecules ()
Med. Chem. Commun., 2018, 9,27-43 DOI: 10.1039/C7MD00474E, Review Article Shiva Krishna Reddy Guduru, Prabhat Arya This review describes mammalian target of rapamycin (mTOR) structure with key role in biological system and selected case studies related to the synthesis of rapamycin-derived and hybrid molecules to explore their biological properties. The content of this RSS Feed (c) The Royal Society of Chemistry
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Antitumor effect of sikokianin C, a selective cystathionine [small beta]-synthase inhibitor, against human colon cancer in vitro and in vivo ()
Med. Chem. Commun., 2018, 9,113-120 DOI: 10.1039/C7MD00484B, Research Article Weining Niu, Fei Chen, Jun Wang, Jing Qian, Shasha Yan A natural biflavonoid compound, sikokianin C, which is a selective, competitive inhibitor of cystathionine [small beta]-synthase, inhibits the proliferation and growth of colon cancer cells in vitro and in vivo. The content of this RSS Feed (c) The Royal Society of Chemistry
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Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A3 adenosine receptor ()
Med. Chem. Commun., 2018, 9,81-86 DOI: 10.1039/C7MD00375G, Research Article Barbara Cosimelli, Giovanni Greco, Sonia Laneri, Ettore Novellino, Antonia Sacchi, Simona Collina, Daniela Rossi, Sandro Cosconati, Elisabetta Barresi, Sabrina Taliani, Maria Letizia Trincavelli, Claudia Martini Chiral pyrimidines were identified as potent and selective hA3 AR antagonists. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and pharmaceutical characterization of site specific mycophenolic acid-modified Xenopus glucagon-like peptide-1 analogs ()
Med. Chem. Commun., 2018, 9,67-80 DOI: 10.1039/C7MD00471K, Research Article Jing Han, Junjie Fu, Lidan Sun, Yue Han, Qiuyi Mao, Fang Liao, Xinshi Zheng, Ke Zhu A novel means for half-life extension of peptide drugs. 3d has potential to be developed as a therapeutic agent for T2DM. The content of this RSS Feed (c) The Royal Society of Chemistry
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Narrow-spectrum antibacterial agents ()
Med. Chem. Commun., 2018, 9,12-21 DOI: 10.1039/C7MD00528H, Review Article Roberta J. Melander, Daniel V. Zurawski, Christian Melander Narrow-spectrum antibiotics have the potential to limit selection for and spread of resistance, and to elicit a lesser detrimental effect upon the host microbiome. The content of this RSS Feed (c) The Royal Society of Chemistry
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Phenylethynyl-substituted heterocycles inhibit cyclin D1 and induce the expression of cyclin-dependent kinase inhibitor p21Wif1/Cip1 in colorectal cancer cells ()
Med. Chem. Commun., 2018, 9,87-99 DOI: 10.1039/C7MD00393E, Research Article Vitaliy M. Sviripa, Liliia M. Kril, Wen Zhang, Yanqi Xie, Przemyslaw Wyrebek, Larissa Ponomareva, Xifu Liu, Yaxia Yuan, Chang-Guo Zhan, David S. Watt, Chunming Liu Fluorinated phenylethynyl-substituted heterocycles inhibit cyclin D1, induce cyclin-dependent kinase inhibitor-1 and block the proliferation of colorectal cancer cells. The content of this RSS Feed (c) The Royal Society of Chemistry
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Highly efficient antibody purification with controlled orientation of protein A on magnetic nanoparticles ()
Med. Chem. Commun., 2018, 9,108-112 DOI: 10.1039/C7MD00468K, Research Article Sunghyun Kim, Daekyung Sung, Jeong Ho Chang In this study, we prepared protein A grafted magnetic nanoparticles for industrial large-scale purification of antibodies with enhancement of binding capacity and immobilization by controlled orientation with chlorophenylsilane (CPTMS) on the surface. The content of this RSS Feed (c) The Royal Society of Chemistry
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Artificial macrocycles as IL-17A/IL-17RA antagonists ()
Med. Chem. Commun., 2018, 9,22-26 DOI: 10.1039/C7MD00464H, Review Article Wenjia Wang, Matthew R. Groves, Alexander Domling Interleukin 17(A) is a pro-inflammatory cytokine involved in several auto-immune and inflammatory diseases. The content of this RSS Feed (c) The Royal Society of Chemistry
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Discovery of 7-hydroxyaporphines as conformationally restricted ligands for beta-1 and beta-2 adrenergic receptors ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00656J, Research Article Angela F. Ku, Gregory D. Cuny Potent beta-1 and beta-2 adrenergic receptor antagonism via a conformationally restricted aporphine scaffold with defined stereochemistry has been developed. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Design, synthesis and evaluation of indole derivatives as multifunctional agents against Alzheimer's disease ()
Med. Chem. Commun., 2018, Advance Article DOI: 10.1039/C7MD00569E, Research Article Ireen Denya, Sarel F. Malan, Adaze B. Enogieru, Sylvester I. Omoruyi, Okobi E. Ekpo, Erika Kapp, Frank T. Zindo, Jacques Joubert Novel indole derivatives as multi-target directed ligands with neuroprotective abilities. X = NH or O. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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