RSC Medicinal Chemistry Blog

This month sees the following articles in MedChemComm that are in the top ten most accessed:

Towards biocompatible nanovalves based on mesoporous silica nanoparticles
Ying-Wei Yang
Med. Chem. Commun., 2011, 2, 1033-1049
DOI: 10.1039/C1MD00158B

Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Matthew A. J. Duncton
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00134E

Are pyridazines privileged structures?
Camille G. Wermuth
Med. Chem. Commun., 2011, 2, 935-941
DOI: 10.1039/C1MD00074H

Molecular obesity, potency and other addictions in drug discovery
Michael M. Hann
Med. Chem. Commun., 2011, 2, 349-355
DOI: 10.1039/C1MD00017A

2-Anilinonicotinyl linked 1,3,4-oxadiazole derivatives: Synthesis, antitumour activity and inhibition of tubulin polymerization
Ahmed Kamal, Y. V. V. Srikanth, Thokhir B. Shaik, M. Naseer A. Khan, Md. Ashraf, M. Kashi Reddy, K. Anil Kumar and Shasi V. Kalivendi
Med. Chem. Commun., 2011, 2, 819-823
DOI: 10.1039/C0MD00177E

Potential atypical antipsychotics: synthesis, binding affinity and SAR of new heterocyclic bioisosteric butyrophenone analogues as multitarget ligands
María Barceló, Enrique Raviña, María J. Varela, José Brea, María I. Loza and Christian F. Masaguer
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00202C

Inhibitors of Stat5 protein signalling
Abbarna A. Cumaraswamy, Aleksandra Todic, Diana Resetca, Mark D. Minden and Patrick T. Gunning
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00175B

Structure–activity relationships of methyl-lysine reader antagonists
J. Martin Herold, Lindsey Ingerman James, Victoria K. Korboukh, Cen Gao, Kaitlyn E. Coil, Dennis J. Bua, Jacqueline L. Norris, Dmitri B. Kireev, Peter J. Brown, Jian Jin, William P. Janzen, Or Gozani and Stephen V. Frye
Med. Chem. Commun., 2012, Advance Article
DOI: 10.1039/C1MD00195G

Discovery of CP-866,087, a mu opioid receptor antagonist for the treatment of alcohol abuse and dependence
Stanton F. McHardy, Steven D. Heck, Sara Guediche, Monica Kalman, Martin P. Allen, Meihua Tu, Dianne K. Bryce, Anne W. Schmidt, Michelle Vanase-Frawley, Ernesto Callegari, Shawn Doran, Nicholas J. Grahame, Stafford McLean and Spiros Liras
Med. Chem. Commun., 2011, 2, 1001-1005
DOI: 10.1039/C1MD00164G

Intramolecular hydrogen bonding to improve membrane permeability and absorption in beyond rule of five chemical space
Alexander Alex, David S. Millan, Manuel Perez, Florian Wakenhut and Gavin A. Whitlock
Med. Chem. Commun., 2011, 2, 669-674
DOI: 10.1039/C1MD00093D

Why not take a look at the articles today and blog your thoughts and comments below.

Fancy submitting an article to MedChemComm? Then why not submit to us today or alternatively email us your suggestions.

This month sees the following articles in MedChemComm that are in the top ten most accessed:

2-Anilinonicotinyl linked 1,3,4-oxadiazole derivatives: Synthesis, antitumour activity and inhibition of tubulin polymerization
Ahmed Kamal, Y. V. V. Srikanth, Thokhir B. Shaik, M. Naseer A. Khan, Md. Ashraf, M. Kashi Reddy, K. Anil Kumar and Shasi V. Kalivendi
Med. Chem. Commun., 2011, 2, 819-823
DOI: 10.1039/C0MD00177E

Towards biocompatible nanovalves based on mesoporous silica nanoparticles
Ying-Wei Yang
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00158B

Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Matthew A. J. Duncton
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00134E

Molecular obesity, potency and other addictions in drug discovery
Michael M. Hann
Med. Chem. Commun., 2011, 2, 349-355
DOI: 10.1039/C1MD00017A

Intramolecular hydrogen bonding to improve membrane permeability and absorption in beyond rule of five chemical space
Alexander Alex, David S. Millan, Manuel Perez, Florian Wakenhut and Gavin A. Whitlock
Med. Chem. Commun., 2011, 2, 669-674
DOI: 10.1039/C1MD00093D

The development of quinolone esters as novel antimalarial agents targeting the Plasmodium falciparum bc 1 protein complex
Robin Cowley, Suet Leung, Nicholas Fisher, Mohammed Al-Helal, Neil G. Berry, Alexandre S. Lawrenson, Raman Sharma, Alison E. Shone, Stephen A. Ward, Giancarlo A. Biagini and Paul M. O′Neill
Med. Chem. Commun., 2012, Advance Article
DOI: 10.1039/C1MD00183C

Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes
Jeffrey A. Pfefferkorn, Angel Guzman-Perez, Peter J. Oates, John Litchfield, Gary Aspnes, Arindrajit Basak, John Benbow, Martin A. Berliner, Jianwei Bian, Chulho Choi, Kevin Freeman-Cook, Jeffrey W. Corbett, Mary Didiuk, Joshua R. Dunetz, Kevin J. Filipski, William M. Hungerford, Christopher S. Jones, Kapil Karki, Anthony Ling, Jian-Cheng Li, Leena Patel, Christian Perreault, Hud Risley, James Saenz, Wei Song, Meihua Tu, Robert Aiello, Karen Atkinson, Nicole Barucci, David Beebe, Patricia Bourassa, Francis Bourbounais, Anne M. Brodeur, Rena Burbey, Jing Chen, Theresa D’Aquila, David R. Derksen, Nahor Haddish-Berhane, Cong Huang, James Landro, Amanda Lee Lapworth, Margit MacDougall, David Perregaux, John Pettersen, Alan Robertson, Beijing Tan, Judith L. Treadway, Shenping Liu, Xiayang Qiu, John Knafels, Mark Ammirati, Xi Song, Paul DaSilva-Jardine, Spiros Liras, Laurel Sweet and Timothy P. Rolph
Med. Chem. Commun., 2011, 2, 828-839
DOI: 10.1039/c1md00116g

Discovery of CP-866,087, a mu opioid receptor antagonist for the treatment of alcohol abuse and dependence
Stanton F. McHardy, Steven D. Heck, Sara Guediche, Monica Kalman, Martin P. Allen, Meihua Tu, Dianne K. Bryce, Anne W. Schmidt, Michelle Vanase-Frawley, Ernesto Callegari, Shawn Doran, Nicholas J. Grahame, Stafford McLean and Spiros Liras
Med. Chem. Commun., 2011, 2, 1001-1005
DOI: 10.1039/C1MD00164G

Synthesis and evaluation of novel 5-sulfonyl-indolin-2-ones as potent cytotoxic agents
Yu Luo, Feng Xiao, Shijing Qian, Qiaojun He, Wei Lu and Bo Yang
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00105A

Design, synthesis and antiproliferative activity of urocanic-chalcone hybrid derivatives
Alexander Ciupa, Natalie J. Griffiths, Stephanie K. Light, Pauline J. Wood and Lorenzo Caggiano
Med. Chem. Commun., 2011, 2,1011-1015
DOI: 10.1039/C1MD00155H

Why not take a look at the articles today and blog your thoughts and comments below.

Fancy submitting an article to MedChemComm? Then why not submit to us today or alternatively email us your suggestions.

This month sees the following articles in MedChemComm that are in the top ten most accessed:

Molecular obesity, potency and other addictions in drug discovery
Michael M. Hann
Med. Chem. Commun., 2011, 2, 349-355
DOI: 10.1039/C1MD00017A

Synthesis and biological evaluation of 2,3-bis(het)aryl-4-azaindole derivatives as protein kinase inhibitors
Frédéric Pin, Frédéric Buron, Fabienne Saab, Lionel Colliandre, Stéphane Bourg, Françoise Schoentgen, Remy Le Guevel, Christiane Guillouzo and Sylvain Routier
Med. Chem. Commun., 2011, 2, 899-903
DOI: 10.1039/C1MD00141H

Design, synthesis, and structure–activity relationships of 1,3,4-oxadiazol-2(3H)-ones as novel FAAH inhibitors
László E. Kiss, Humberto S. Ferreira, Alexandre Beliaev, Leonel Torrão, Maria João Bonifácio and David A. Learmonth
Med. Chem. Commun., 2011, 2, 889-894
DOI: 10.1039/C1MD00136A

Minisci reactions: Versatile CH-functionalizations for medicinal chemists
Matthew A. J. Duncton
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00134E

Intramolecular hydrogen bonding to improve membrane permeability and absorption in beyond rule of five chemical space
Alexander Alex, David S. Millan, Manuel Perez, Florian Wakenhut and Gavin A. Whitlock
Med. Chem. Commun., 2011, 2, 669-674
DOI: 10.1039/C1MD00093D

Are pyridazines privileged structures?
Camille G. Wermuth
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00074H

Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes
Jeffrey A. Pfefferkorn, Angel Guzman-Perez, Peter J. Oates, John Litchfield, Gary Aspnes, Arindrajit Basak, John Benbow, Martin A. Berliner, Jianwei Bian, Chulho Choi, Kevin Freeman-Cook, Jeffrey W. Corbett, Mary Didiuk, Joshua R. Dunetz, Kevin J. Filipski, William M. Hungerford, Christopher S. Jones, Kapil Karki, Anthony Ling, Jian-Cheng Li, Leena Patel, Christian Perreault, Hud Risley, James Saenz, Wei Song, Meihua Tu, Robert Aiello, Karen Atkinson, Nicole Barucci, David Beebe, Patricia Bourassa, Francis Bourbounais, Anne M. Brodeur, Rena Burbey, Jing Chen, Theresa D’Aquila, David R. Derksen, Nahor Haddish-Berhane, Cong Huang, James Landro, Amanda Lee Lapworth, Margit MacDougall, David Perregaux, John Pettersen, Alan Robertson, Beijing Tan, Judith L. Treadway, Shenping Liu, Xiayang Qiu, John Knafels, Mark Ammirati, Xi Song, Paul DaSilva-Jardine, Spiros Liras, Laurel Sweet and Timothy P. Rolph
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/c1md00116g

Development of substituted 7-phenyl-4-aminobenzothieno[3,2-d] pyrimidines as potent LIMK1 inhibitors
Brad E. Sleebs, Danny Ganame, Alla Levit, Ian P. Street, Alison Gregg, Hendrik Falk and Jonathan B. Baell
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00138H

Redesigning the designer drug ecstasy: non-psychoactive MDMA analogues exhibiting Burkitt’s lymphoma cytotoxicity
Michael N. Gandy, Matthew McIldowie, Katie Lewis, Agata M. Wasik, Danielle Salomonczyk, Keith Wagg, Zak A. Millar, David Tindiglia, Philippe Huot, Tom Johnston, Sherri Thiele, Blake Nguyen, Nicholas M. Barnes, Jonathan M. Brotchie, Mathew T. Martin-Iverson, Joanne Nash, John Gordon and Matthew J. Piggott
Med. Chem. Commun., 2010, 1, 287-293
DOI: 10.1039/C0MD00108B

Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors
Brad E. Sleebs, Alla Levit, Ian P. Street, Hendrik Falk, Tim Hammonds, Ai Ching Wong, Mark D. Charles, Michael F. Olson and Jonathan B. Baell
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00137J

Why not take a look at the articles today and blog your thoughts and comments below.

Fancy submitting an article to MedChemComm? Then why not submit to us today or alternatively email us your suggestions.

This month sees the following articles in MedChemComm that are in the top ten most accessed:

Intramolecular hydrogen bonding to improve membrane permeability and absorption in beyond rule of five chemical space
Alexander Alex, David S. Millan, Manuel Perez, Florian Wakenhut and Gavin A. Whitlock
Med. Chem. Commun., 2011, 2, 669-674
DOI: 10.1039/C1MD00093D

Molecular obesity, potency and other addictions in drug discovery
Michael M. Hann
Med. Chem. Commun., 2011, 2, 349-355
DOI: 10.1039/C1MD00017A

Chemical space as a source for new drugs
Jean-Louis Reymond, Ruud van Deursen, Lorenz C. Blum and Lars Ruddigkeit
Med. Chem. Commun., 2010, 1, 30-38
DOI: 10.1039/c0md00020e

Are pyridazines privileged structures?
Camille G. Wermuth
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00074H

Identification of target family directed bioisosteric replacements
Anne Mai Wassermann and Jürgen Bajorath
Med. Chem. Commun., 2011, 2, 601-606
DOI: 10.1039/C1MD00066G

Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes
Jeffrey A. Pfefferkorn, Angel Guzman-Perez, Peter J. Oates, John Litchfield, Gary Aspnes, Arindrajit Basak, John Benbow, Martin A. Berliner, Jianwei Bian, Chulho Choi, Kevin Freeman-Cook, Jeffrey W. Corbett, Mary Didiuk, Joshua R. Dunetz, Kevin J. Filipski, William M. Hungerford, Christopher S. Jones, Kapil Karki, Anthony Ling, Jian-Cheng Li, Leena Patel, Christian Perreault, Hud Risley, James Saenz, Wei Song, Meihua Tu, Robert Aiello, Karen Atkinson, Nicole Barucci, David Beebe, Patricia Bourassa, Francis Bourbounais, Anne M. Brodeur, Rena Burbey, Jing Chen, Theresa D’Aquila, David R. Derksen, Nahor Haddish-Berhane, Cong Huang, James Landro, Amanda Lee Lapworth, Margit MacDougall, David Perregaux, John Pettersen, Alan Robertson, Beijing Tan, Judith L. Treadway, Shenping Liu, Xiayang Qiu, John Knafels, Mark Ammirati, Xi Song, Paul DaSilva-Jardine, Spiros Liras, Laurel Sweet and Timothy P. Rolph
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/c1md00116g

Aromatic chloride to nitrile transformation: medicinal and synthetic chemistry
Lyn H. Jones, Nicholas W. Summerhill, Nigel A. Swain and James E. Mills
Med. Chem. Commun., 2010, 1, 309-318
DOI: 10.1039/C0MD00135J

Carbazole‒pyrrolo[2,1-c][1,4]benzodiazepine conjugates: design, synthesis, and biological evaluation
Ahmed Kamal, Rajesh V. C. R. N. C. Shetti, M. Janaki Ramaiah, P. Swapna, K. Srinivasa Reddy, A. Mallareddy, M. P. Narasimha Rao, Mukesh Chourasia, G. Narahari Sastry, Aarti Juvekar, Surekha Zingde, Pranjal Sarma, S. N. C. V. L. Pushpavalli and Manika Pal-Bhadra
Med. Chem. Commun., 2011, 2, 780-788
DOI: 10.1039/c1md00072a

Optimized glucuronidation of dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD
Laura Hilton, Rachel Osborne, Amy S. Kenyon, Helen Baldock, Mark E. Bunnage, Jane Burrows, Nick Clarke, Michele Coghlan, David Entwistle, David Fairman, Neil Feeder, Kim James, Rhys M. Jones, Nadia Laouar, Graham Lunn, Stuart Marshall, Sandra D. Newman, Sheena Patel, Matthew D. Selby, Fiona Spence, Emilio F. Stuart, Susan Summerhill, Michael A. Trevethick, Karen N. Wright, Michael Yeadon, David A. Price and Lyn H. Jones
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/c1md00140j

Matrix-based multiparameter optimisation of glucokinase activators: the discovery of AZD1092
Michael J. Waring, Craig Johnstone, Darren McKerrecher, Kurt G. Pike and Graeme Robb
Med. Chem. Commun., 2011, 2, 775-779
DOI: 10.1039/c1md00092f

Why not take a look at the articles today and blog your thoughts and comments below.

Fancy submitting an article to MedChemComm? Then why not submit to us today or alternatively email us your suggestions.

This month sees the following articles in MedChemComm that are in the top ten most accessed:

Intramolecular hydrogen bonding to improve membrane permeability and absorption in beyond rule of five chemical space
Alexander Alex, David S. Millan, Manuel Perez, Florian Wakenhut and Gavin A. Whitlock
Med. Chem. Commun., 2011, 2, 669-674
DOI: 10.1039/C1MD00093D

Molecular obesity, potency and other addictions in drug discovery
Michael M. Hann
Med. Chem. Commun., 2011, 2, 349-355
DOI: 10.1039/C1MD00017A

Are pyridazines privileged structures?
Camille G. Wermuth
Med. Chem. Commun., 2011, Advance Article
DOI: 10.1039/C1MD00074H

Identification of target family directed bioisosteric replacements
Anne Mai Wassermann and Jürgen Bajorath
Med. Chem. Commun., 2011, 2, 601-606
DOI: 10.1039/C1MD00066G

Synthesis and biological evaluation of tetrazole containing compounds as possible anticancer agents
Chebolu Naga Sesha Sai Pavan Kumar, Dusmant Kumar Parida, Amlipur Santhoshi, Anil Kumar Kota, Balasubramanian Sridhar and Vaidya Jayathirtha Rao
Med. Chem. Commun., 2011, 2, 486-492
DOI: 10.1039/C0MD00263A

Expanding the horizon of chemotherapeutic targets: From MDM2 to MDMX (MDM4)
Antonio Macchiarulo, Nicola Giacchè, Andrea Carotti, Fabiola Moretti and Roberto Pellicciari
Med. Chem. Commun., 2011, 2, 455-465
DOI: 10.1039/C0MD00238K

Boronic acids in medicinal chemistry: anticancer, antibacterial and antiviral applications
Paul C. Trippier and Christopher McGuigan
Med. Chem. Commun., 2010, 1, 193-198
DOI: 10.1039/C0MD00119H

Aromatic chloride to nitrile transformation: medicinal and synthetic chemistry
Lyn H. Jones, Nicholas W. Summerhill, Nigel A. Swain and James E. Mills
Med. Chem. Commun., 2010, 1, 309-318
DOI: 10.1039/C0MD00135J

Synthesis and biological activity evaluation of N-protected isatin derivatives as inhibitors of ICAM-1
Shashwat Malhotra, Sakshi Balwani, Ashish Dhawan, Brajendra K. Singh, Sarvesh Kumar, Rajesh Thimmulappa, Shyam Biswal, Carl E. Olsen, Erik Van der Eycken, Ashok K. Prasad, Balaram Ghosh and Virinder S. Parmar
Med. Chem. Commun., 2011, 2, 743-751
DOI: 10.1039/C0MD00262C

Overcoming retinoic acid receptor-a based testicular toxicity in the optimisation of glucokinase activators
Michael J. Waring, Iain J. Brogan, Matthew Coghlan, Craig Johnstone, Huw B. Jones, Brendan Leighton, Darren McKerrecher, Kurt G. Pike and Graeme R. Robb
Med. Chem. Commun., 2011, 2, 771-774
DOI: 10.1039/C1MD00090J

Why not take a look at the articles today and blog your thoughts and comments below.

Fancy submitting an article to MedChemComm? Then why not submit to us today or alternatively email us your suggestions.