Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Editor-in-Chief: Natalia Ortúzar
Impact Factor: 3.046
ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 74/254 (Pharmacology & Pharmacy)
Online ISSN: 1860-7187
September 23, 2014
Diederich to Give Bohlmann Lecture
Congratulations to François Diederich (ETH Zürich), who will be giving this year's Bohlmann Lecture at the Technische Universität Berlin in November. Diederich is a member of ChemMedChem's International Advisory Board, and recently reported on small-molecule inhibitors of trypanothione reductase.
Recently Published Articles
- Molecular-Target-Based Anticancer Photosensitizer: Synthesis and in vitro Photodynamic Activity of Erlotinib–Zinc(II) Phthalocyanine Conjugates
Dr. Feng-Ling Zhang, Qi Huang, Prof. Jian-Yong Liu, Prof. Ming-Dong Huang and Prof. Jin-Ping Xue
Article first published online: 21 OCT 2014 | DOI: 10.1002/cmdc.201402373
Waging war on cancer: Herein we report a series of conjugates with phthalocyanine as the “warhead” and erlotinib, a molecular-target-based anticancer drug, as the “guidance system”. These conjugates combine the high activity of photodynamic therapy with the highly effective targeting capacity of molecular-target-based anticancer therapy, thereby acting as “missile-style” target-directed photosensitizers for potential use in cancer treatments.
- Design of gem-Difluoro-bis-Tetrahydrofuran as P2 Ligand for HIV-1 Protease Inhibitors to Improve Brain Penetration: Synthesis, X-ray Studies, and Biological Evaluation
Prof. Dr. Arun K. Ghosh, Sofiya Yashchuk, Akira Mizuno, Nilanjana Chakraborty, Johnson Agniswamy, Yuan-Fang Wang, Manabu Aoki, Pedro Miguel Salcedo Gomez, Masayuki Amano, Prof. Irene T. Weber and Dr. Hiroaki Mitsuya
Article first published online: 21 OCT 2014 | DOI: 10.1002/cmdc.201402358
High-performance fluoros: We report the design, synthesis, biological, and X-ray structural studies of HIV-1 protease inhibitors (PIs) containing gem-difluoro-bis-THF as the P2 ligand. These PIs exhibited much better lipophilicity profiles and blood–brain barrier permeability than darunavir in an in vitro model. A high-resolution structure of a PI–HIV-1 protease complex shows ligand fluorine atoms involved in interesting interactions in the S2 subsite. The PIs also maintained excellent activity against multi-PI-resistant clinical HIV-1 variants.
- Identification of Structural Features of 2-Alkylidene-1,3-Dicarbonyl Derivatives that Induce Inhibition and/or Activation of Histone Acetyltransferases KAT3B/p300 and KAT2B/PCAF
Prof. Dr. Sabrina Castellano, Dr. Ciro Milite, Alessandra Feoli, Dr. Monica Viviano, Prof. Dr. Antonello Mai, Prof. Ettore Novellino, Prof. Dr. Alessandra Tosco and Prof. Dr. Gianluca Sbardella
Article first published online: 21 OCT 2014 | DOI: 10.1002/cmdc.201402371
Ups and downs: Chemical manipulation of the carbonyl functional groups of a series of analogues of diethyl pentadecylidenemalonate 1 (SPV106), a mixed inhibitor/activator of lysine acetyltransferases that we recently identified, yielded different activity profiles against KAT2B and KAT3B (pure KAT2B activator, pan-inhibitor, or mixed KAT2B activator/KAT3B inhibitor).
- Stimuli-Responsive Polymeric Nanoparticles for Nanomedicine
Carina I. C. Crucho
Article first published online: 16 OCT 2014 | DOI: 10.1002/cmdc.201402290
Bringing life from cell death: Stimuli-responsive polymeric nanoparticles can respond to the microenvironment of a particular disease and its cells. Internal triggers as well as external devices permit temporally and spatially controlled drug delivery. The development of well-defined nanomedicines is critical for their behavior in vivo.
- Conjugation of Cisplatin Analogues and Cyclooxygenase Inhibitors to Overcome Cisplatin Resistance
Wilma Neumann, Brenda C. Crews, Dr. Menyhárt B. Sárosi, Cristina M. Daniel, Kebreab Ghebreselasie, Dr. Matthias S. Scholz, Prof. Dr. Lawrence J. Marnett and Prof. Dr. Evamarie Hey-Hawkins
Article first published online: 15 OCT 2014 | DOI: 10.1002/cmdc.201402353
Studying dual action: Platinum prodrugs ensure a concerted transport of cisplatin analogues and cyclooxygenase inhibitors into tumor cells. These conjugates provide tools to elucidate the synergistic effects that were observed in combination treatments with such drugs, and could provide insight into the involvement of cyclooxygenase in tumorigenesis.