© WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Editorial Board Chairs: Antonello Mai, Rainer Metternich. Assoc. Editors: David Peralta, Scott Williams (Sr)
Impact Factor: 2.98
ISI Journal Citation Reports © Ranking: 2015: 18/59 (Chemistry Medicinal); 77/255 (Pharmacology & Pharmacy)
Online ISSN: 1860-7187
November 23, 2016
13th WCMBC in Steamboat Springs: January 2017
ChemMedChem will be sponsoring the next Winter Conference on Medicinal & Bioorganic Chemistry this coming January 22nd–26th in Steamboat Springs, Colorado. The organizers have lined up another impressive list of presenters for this year's event. And as if excellent cutting-edge science weren't enough, this meeting comes with a healthy dose of play time too: unforgettable skiing in the bright sun and deep snow of northern Colorado. Make sure to register soon!
Recently Published Articles
- Form Matters: Stable Helical Foldamers Preferentially Target Human Monocytes and Granulocytes
Benedetta Del Secco, Dr. Giulia Malachin, Lorenzo Milli, Nicola Zanna, Prof. Emanuele Papini, Prof. Andrea Cornia, Dr. Regina Tavano and Prof. Claudia Tomasini
Version of Record online: 19 JAN 2017 | DOI: 10.1002/cmdc.201600597
Where form is function: Hybrid peptide oligomers with helical frameworks can associate preferentially with inflammatory cells, regardless of their charge or chemical nature. Such foldamers can thus act as targeting agents for small-molecule drugs, as they are intrinsically non-cytotoxic at relatively high doses. Moreover, with sufficient length, they show a particular cell targeting preference; they are rapidly and more effectively internalized in human blood myeloid cells, such as monocytes and granulocytes.
- A Dual Topoisomerase Inhibitor of Intense Pro-Apoptotic and Antileukemic Nature for Cancer Treatment
Christopher Meier, Tamara N. Steinhauer, Fabian Koczian, Birte Plitzko, Katharina Jarolim, Ulrich Girreser, Simone Braig, Doris Marko, Angelika M. Vollmar and Bernd Clement
Accepted manuscript online: 18 JAN 2017 01:25PM EST | DOI: 10.1002/cmdc.201700026
- Old Drug Scaffold, New Activity: Thalidomide Correlated Compounds Exerting Different Effects on Breast Cancer Cell Growth and Progression
Alessia Carocci, alessia catalano, Domenico Iacopetta and Maria Stefania Sinicropi
Accepted manuscript online: 18 JAN 2017 01:25PM EST | DOI: 10.1002/cmdc.201600629
- Synthesis and Evaluation of Anti-inflammatory N-Substituted 3,5-Bis(2-(trifluoromethyl)benzylidene)piperidin-4-ones
Dr. Zixin Xie, Zaikui Zhang, Shufang Yu, Donghua Cheng, Huan Zhang, Chao Han, Handeng Lv and Prof. Dr. Faqing Ye
Version of Record online: 18 JAN 2017 | DOI: 10.1002/cmdc.201600606
Taking the heat off: The 24 curcumin analogues in this study were found to have no toxicity toward mouse bone marrow cells, and some of them showed potent anti-inflammatory activity by inhibiting LPS-stimulated TNFα, IL-6, IL-1β, PGE2, and NO production in rat macrophages. Pharmacokinetic studies indicated that compound c6 has better bioavailability than curcumin in vivo. Both c6 and c10 may be valuable leads for the development of new anti-inflammatory agents.
- Synthesis and Biological Evaluation of Novel 2-Aminonicotinamide Derivatives as Antifungal Agents
Tingjunhong Ni, Ran Li, Fei Xie, Jing Zhao, Xin Huang, Maomao An, Chengxu Zang, Zhan Cai, Prof. Dr. Dazhi Zhang and Prof. Dr. Yuanying Jiang
Version of Record online: 18 JAN 2017 | DOI: 10.1002/cmdc.201600545
Infections unanchored! A series of novel 2-aminonicotinamide derivatives were designed, synthesized, and evaluated for in vitro antifungal activity. Compounds 11 g and 11 h have excellent activity against Candida albicans, with MIC80 values of 0.0313 μg mL−1, and exhibit broad-spectrum antifungal activity against fluconazole-resistant C. albicans, C. parapsilosis, C. glabrata, and Cryptococcus neoformans, with a MIC80 range of 0.0313–2.0 μg mL−1. Further investigation suggested that compound 11 g targets the cell wall and decreases glycosylphosphatidylinositol anchor content on the cell surface of C. albicans.