Bioorganic & Medicinal Chemistry Volume 21, Issue 3, 2013 Contents REVIEW Recent development of potent analogues of oxazolidinone antibacterial agents pp 577–591 Katarzyna Michalska*, Izabela Karpiuk, Marek Król, Stefan Tyski O N N 5' O H N O F O C B A ARTICLES Design, synthesis, and structure–activity relationship (SAR) of N-[7-(4-hydroxyphenoxy)-6-methylindan- 4-yl]malonamic acids as thyroid hormone receptor b (TRb) selective agonists pp 592–607 Hiroaki Shiohara*, Tetsuya Nakamura, Norihiko Kikuchi, Tomonaga Ozawa, Akane Matsuzawa, Ryuichi Nagano, Hideki Ohnota, Takahide Miyamoto, Kazuo Ichikawa, Kiyoshi Hashizume Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton pp 608–617 Yusuke Mita, Tomomi Noguchi-Yachide, Minoru Ishikawa*, Yuichi Hashimoto Bioorganic & Medicinal Chemistry 21 (2013) 569–576 Contents lists available at SciVerse ScienceDirect Bioorganic & Medicinal Chemistry journal homepage: www.elsevier.com/locate/bmc
Recent development of potent analogues of oxazolidinone antibacterial agents pp 577–591
Katarzyna Michalska*, Izabela Karpiuk, Marek Król, Stefan Tyski
O N N5'
OHN
OF
O
C B A
ARTICLES
Design, synthesis, and structure–activity relationship (SAR) of N-[7-(4-hydroxyphenoxy)-6-methylindan-4-yl]malonamic acids as thyroid hormone receptor b (TRb) selective agonists
Contents lists available at SciVerse ScienceDirect
Bioorganic & Medicinal Chemistry
journal homepage: www.elsevier .com/locate /bmc
Structure-based drug design and potent anti-cancer activity of tricyclic 5:7:5-fused diimidazo[4,5-d:40,50-f][1,3]diazepines
pp 618–631
Atul Kondaskar, Shilpi Kondaskar, James C. Fishbein, Brandon A. Carter-Cooper, Rena G. Lapidus, Mariola Sadowska,Martin J. Edelman, Ramachandra S. Hosmane*
Solvent Exposed region
Chargedregion
Mg ion
Q motif
P loopPhe182
Tyr200
NN N
NN
ONH
N
OMeO
OMe
Phe182Solvent Exposed region
Chargedregion
Mg ion
Q motif
P loop
Tyr200
N
N N
NNH2
O
OH
O P O-
O-
O
O
N
HOH
H
1
2
34
56 7
8
9
A B
12
3
4
56
78
9
(A) Model for interactions between AMP and DDX3. (B) Proposed model for interactions between 1 and DDX3.
Synthesis and biological evaluation of N-alkyl-N-(4-methoxyphenyl)pyridin-2-amines as a new class of tubulinpolymerization inhibitors
pp 632–642
Xiao-Feng Wang, Emika Ohkoshi, Sheng-Biao Wang, Ernest Hamel, Kenneth F. Bastow, Susan L. Morris-Natschke,Kuo-Hsiung Lee, Lan Xie*
Investigations into the synthesis, radiofluorination and conjugation of a new [18F]fluorocyclobutyl prosthetic group andits in vitro stability using a tyrosine model system
Design, synthesis and evaluation of novel heterodimers of donepezil and huperzine fragments as acetylcholinesteraseinhibitors
pp 676–683
Yueqing Hu, Jun Zhang, Oormila Chandrashankra, Fanny C. F. Ip, Nancy Y. Ip*
Heterodimers of donepezil and huperzine A fragments tethered with a tetramethylene linker exhibited high potency and selectivity towards acetylcholinesteraseinhibition.
Biocatalytic synthesis, structural elucidation, antioxidant capacity and tyrosinase inhibition activity of long chain fattyacid acylated derivatives of phloridzin and isoquercitrin
pp 684–692
Ziaullah, Khushwant S. Bhullar, Sumudu N. Warnakulasuriya, H. P. Vasantha Rupasinghe*
O
O
O
OH
OH O
OHOH
OH
OH
OHOH
O
O
O
OH
OH O
OHOH
OH
OH
OHOR
+ H2O
OH
O
O
OH
OH
OH
OH
OH
OH
O
OH
O
O
OH
OH
OH
OR
OH
OH
O+ H2O
i
RCOOH RCOOH
i
Our present investigation describes the biocatalytic preparation, detailed NMR structural assignment, antioxidant capacity and tyrosinase inhibitoryactivity of long chain acylated derivatives of phloridzin and isoquercitrin. (i) Acetone, 3 Å molecular sieves, Novozyme 435�, 45 �C, Stirring, 24 h;R = Oleic, Stearic, Linoleic, Linolenic, Eicosapentaenoic (EPA), Docosahexaenoic Acids (DHA) or their corresponding esters.
Synthesis and biological evaluation of halogenated curcumin analogs as potential nuclear receptor selective agonists pp 693–702
Shane Batie, Jamie H. Lee, Rabia A. Jama, Drew O. Browder, Luis A. Montano, Chanh C. Huynh, Lisa M. Marcus,Dorian G. Tsosie, Zeynab Mohammed, Vu Trang, Pamela A. Marshall, Peter W. Jurutka*, Carl E. Wagner*
O
HO
OH O
O
OH
R1
HO
OH OR1
OH
R2 R2CurcuminHalogenated Analog
VDR and RXR Agonists
R3 R3
SiO2 nanoparticles as platform for delivery of nucleoside triphosphate analogues into cells pp 703–711
Svetlana V. Vasilyeva*, Vladimir N. Silnikov, Natalia V. Shatskaya, Asya S. Levina, Marina N. Repkova, Valentina F. Zarytova
Effects of fluorines on nonsecosteroidal vitamin D receptor agonists pp 712–721
Automated parallel synthesis of 50-triphosphate oligonucleotides and preparation of chemically modified50-triphosphate small interfering RNA
pp 722–732
Ivan Zlatev*, Jeremy G. Lackey, Ligang Zhang, Amy Dell, Kathy McRae, Sarfraz Shaikh, Richard G. Duncan,Kallanthottathil G. Rajeev, Muthiah Manoharan*
Automated parallel and high-throughput synthesis of 50-triphosphate oligonucleotides enables the preparation of chemically modified 50-triphosphatesmall interfering RNAs designed to address RNA interference gene knockdown and directed immunostimulation.
Synthesis of 13C-labeled and functionalized Hyaluronan derivatives for biophysical studies and surface modifications pp 733–741
Stephan Rigol, Liang Xia, Athanassios Giannis*
O
NHO
OHO
OH
HO
OHO
OO
NHO
OHO
OH
OHO
O
OH
HO
OO
OH
HO**
*
**
*
A convergent synthesis of 13C-labeled and non-labeled Hyaluronic acid tetrasaccharide for biophysical studies and surface modifications is presented.
Enhanced bioactivity of silybin B methylation products pp 742–747
Arlene A. Sy-Cordero, Tyler N. Graf, Scott P. Runyon, Mansukh C. Wani, David J. Kroll, Rajesh Agarwal, Scott J. Brantley,Mary F. Paine, Stephen J. Polyak, Nicholas H. Oberlies*
Design, synthesis, and structure–activity relationships of a series of 4-benzyl-5-isopropyl-1H-pyrazol-3-ylb-DD-glycopyranosides substituted with novel hydrophilic groups as highly potent inhibitors of sodium glucoseco-transporter 1 (SGLT1)
Alkaloid constituents from flower buds and leaves of sacred lotus (Nelumbo nucifera, Nymphaeaceae) withmelanogenesis inhibitory activity in B16 melanoma cells
Synthesis, topoisomerase-targeting activity and growth inhibition of lycobetaine analogs pp 814–823
Simone A. Baechler, Markus Fehr, Michael Habermeyer, Andreas Hofmann, Karl-Heinz Merz, Heinz-Herbert Fiebig,Doris Marko*, Gerhard Eisenbrand
Exploration of 1-(3-chloro-4-(4-oxo-4H-chromen-2-yl)phenyl)-3-phenylurea derivatives as selective dual inhibitors ofRaf1 and JNK1 kinases for anti-tumor treatment
pp 824–831
Feng Jin, Dan Gao, Cunlong Zhang, Feng Liu, Bizhu Chu, Yan Chen, Yu Zong Chen, Chunyan Tan*, Yuyang Jiang*
A series of 1-(3-chloro-4-(4-oxo-4H-chromen-2-yl)phenyl)-3-phenylurea derivatives were designed, synthesized and explored for their inhibitoryactivities against kinases and tumor cell lines.
OTHER CONTENTS
Corrigenda pp 832–834
Bioorganic & Medicinal Chemistry Reviews and Perspectives pp I–III
*Corresponding authorSupplementary data available via SciVerse ScienceDirect
COVER
Botulinum neuortoxins are the most lethal toxins known to man and are considered by the Centers for Disease Control and Prevention (CDC) tobe a ‘‘Category A’’ agent placing them as one of the six highest priority bioterrorist agents. There are no approved pharmacological treatmentsfor botulinum neurointoxication. The work detailed combines studies using synthesis, crystallography, modeling, kinetic and cellular researchto advance pharmacological intervention against this neurotoxin. [Šilhár, P.; Silvaggi, N.R.; Pellett, S.; Capková, K.; Johnson, E.A; Allen, K.N;Janda, K.D. Bioorg. Med. Chem. DOI: 10.1016/j.bmc.2012.12.001]
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