© 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
- Cytotoxicity of a series of norcantharidin inspired tetrahydroepoxyisoindole carboxamides
Christopher Peter Gordon, Lawson K Spare, Pasquale Falsetta, Jayne Gilbert, David G Harman, Mark A Baker, Feng Li, Adam McCluskey, Jack K Clegg, Jennette A Sakoff and Janice R Aldrich-Wright
Accepted manuscript online: 6 DEC 2016 12:20AM EST | DOI: 10.1002/cmdc.201600573
- Design, Synthesis, and Evaluation of Dasatinib–Amino Acid and Dasatinib–Fatty Acid Conjugates as Protein Tyrosine Kinase Inhibitors
Prof. Rakesh K. Tiwari, Dr. Alex Brown, Dr. Neda Sadeghiani, Dr. Amir Nasrolahi Shirazi, Jared Bolton, Amanda Tse, Prof. Gennady Verkhivker, Prof. Keykavous Parang and Prof. Gongqin Sun
Version of Record online: 5 DEC 2016 | DOI: 10.1002/cmdc.201600387
Conjugated for specificity: 25 derivatives of dasatinib were synthesized by esterification with fatty acids and amino acids to improve the specificity for Src, Csk, and Abl kinases. We reasoned that by extending dasatinib from the ATP binding pocket into variable regions, the resulting derivatives may undergo new kinase-specific interactions, which would lead to greater inhibitory specificity toward a given kinase.
- Discovery of a Novel Scaffold as an Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor Based on the Pyrrolopiperazinone Alkaloid, Longamide B
Zenyu Shiokawa, Emi Kashiwabara, Daisuke Yoshidome, Prof. Dr. Koichi Fukase, Dr. Shinsuke Inuki and Prof. Dr. Yukari Fujimoto
Version of Record online: 5 DEC 2016 | DOI: 10.1002/cmdc.201600446
A new scaffold: The pyrrolopiperazinone alkaloid longamide B and its derivatives were identified as novel IDO1 inhibitors based on docking studies and small library synthesis. The thioamide derivative showed higher IDO1 inhibitory activity than longamide B and displayed activity similar to that of a representative IDO1 inhibitor, 1-methyl-tryptophan. These results suggest that the pyrrolopiperazinone scaffold of longamide B could be used for IDO1 inhibitors.
- A Quinacrine Analogue Selective Against Gastric Cancer Cells: Insight from Biochemical and Biophysical Studies
Ana Gomes, Dr. Iva Fernandes, Dr. Cátia Teixeira, Prof. Nuno Mateus, Prof. M. J. Sottomayor and Prof. Paula Gomes
Version of Record online: 5 DEC 2016 | DOI: 10.1002/cmdc.201600477
The core of the matter: A quinacrine analogue, formerly developed as a dual-stage antimalarial, seems to be a valuable template for additional structural optimization toward specific agents against gastric cancer. Nuclear targeting of this compound and its interactions with calf thymus DNA were assessed, and the evidence suggests that this compound has the ability to reach the nucleus and to interact with DNA.
- Design, synthesis, and evaluation of 2,9-bis[(substituted-aminomethyl)phenyl]-1,10-phenanthroline derivatives as G-quadruplex ligands
Nassima Meriem Gueddouda, Miyanou Rosales Hurtado, Stéphane Moreau, Luisa Ronga, Rabindra Nath Das, Solène Savrimoutou, Sandra Rubio, Adrien Marchand, Oscar Mendoza, Mathieu Marchivie, Lilian Elmi, Albain Chansavang, Vanessa Desplat, Valérie Gabelica, Anne Bourdoncle, Jean-Louis Mergny and Jean Guillon
Accepted manuscript online: 4 DEC 2016 10:18PM EST | DOI: 10.1002/cmdc.201600511