Org. and Biomol. Chem.

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Design, synthesis, and biological evaluation of novel trifluoromethyl indoles as potent HIV-1 NNRTIs with an improved drug resistance profile

15 May, 2014 - 18:17

Org. Biomol. Chem., 2014, 12,3446-3458
DOI: 10.1039/C3OB42186D, PaperHai-Xia Jiang, Dao-Min Zhuang, Ying Huang, Xing-Xin Cao, Jian-Hua Yao, Jing-Yun Li, Jian-Yong Wang, Chen Zhang, Biao Jiang
A novel series of trifluoromethyl indoles have been designed, synthesized and evaluated for anti-HIV-1 activities.
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Design and synthesis of paracaseolide A analogues as selective protein tyrosine phosphatase 1B inhibitors

15 May, 2014 - 18:17

Org. Biomol. Chem., 2014, 12,3441-3445
DOI: 10.1039/C4OB00214H, PaperJian-Peng Yin, Chun-Lan Tang, Li-Xin Gao, Wei-Ping Ma, Jing-Ya Li, Ying Li, Jia Li, Fa-Jun Nan
Paracaseolide A analogues showed improved PTP1B enzyme inhibitory activity, high selectivity for PTP1B over TC-PTP, and improved cellular effects.
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Synthesis of heterocyclic-fused benzopyrans via the Pd(II)-catalyzed C-H alkenylation/C-O cyclization of flavones and coumarins

15 May, 2014 - 18:17

Org. Biomol. Chem., 2014, 12,3413-3422
DOI: 10.1039/C4OB00180J, PaperYechan Kim, Youngtaek Moon, Dahye Kang, Sungwoo Hong
An efficient and practical method for effecting a tandem C-H alkenylation/C-O cyclization has been achieved via the C-H functionalization of flavone derivatives.
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Dual-color imaging of cytosolic and mitochondrial zinc ions in live tissues with two-photon fluorescent probes

15 May, 2014 - 18:17

Org. Biomol. Chem., 2014, 12,3406-3412
DOI: 10.1039/C4OB00101J, PaperKailash Rathore, Chang Su Lim, Young Lee, Bong Rae Cho
We have developed TP probes for [Zn2+]cyto and [Zn2+]mito, which emit TPEF at widely-separated wavelength regions. The new probes can simultaneously detect [Zn2+]cyto and [Zn2+]mito in live cells, as well as in living tissues by dual-color TPM imaging.
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Regioselective synthesis of novel 4,5-diaryl functionalized 3,4-dihydropyrimidine-2(1H)-thiones via a non-Biginelli-type approach and evaluation of their in vitro anticancer activity

15 May, 2014 - 18:17

Org. Biomol. Chem., 2014, 12,3427-3440
DOI: 10.1039/C4OB00094C, PaperJacek G. Sosnicki, Lukasz Struk, Mateusz Kurzawski, Magdalena Peruzynska, Gabriela Maciejewska, Marek Drozdzik
A novel and regioselective approach to synthesize anticancer 4,5-diaryl functionalized 3,4-dihydropyrimidine-2(1H)-thiones is described.
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Palladium-catalyzed regioselective azidation of allylic C-H bonds under atmospheric pressure of dioxygen

15 May, 2014 - 18:17

Org. Biomol. Chem., 2014, 12,3340-3343
DOI: 10.1039/C4OB00442F, CommunicationHuoji Chen, Wanfei Yang, Wanqing Wu, Huanfeng Jiang
A palladium-catalyzed allylic azidation of alkenes with sodium azide under atmospheric pressure of dioxygen was developed.
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A cyclization-carbonylation-cyclization coupling reaction of (ortho-alkynyl phenyl) (methoxymethyl) sulfides with the palladium(II)-bisoxazoline catalyst

15 May, 2014 - 18:17

Org. Biomol. Chem., 2014, 12,3380-3385
DOI: 10.1039/C4OB00299G, PaperYiyun Jiang, Taichi Kusakabe, Keisuke Takahashi, Keisuke Kato
A CCC-coupling reaction of (o-alkynylphenyl) (methoxymethyl) sulfides, catalyzed by (box)PdII complexes, afforded symmetrical ketones bearing two benzo[b]thiophene groups in good to excellent yields.
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Asymmetric synthesis of chloroisothreonine derivatives via syn-stereoselective Mannich-type additions across N-sulfinyl-[small alpha]-chloroimines

15 May, 2014 - 18:17

Org. Biomol. Chem., 2014, 12,3393-3405
DOI: 10.1039/C4OB00243A, PaperGert Callebaut, Filip Colpaert, Melinda Nonn, Lorand Kiss, Reijo Sillanpaa, Karl W. Tornroos, Ferenc Fulop, Norbert De Kimpe, Sven Mangelinckx
Mannich-type reactions across N-sulfinyl-[small alpha]-chloroaldimines resulted in syn-stereoselective synthesis of chloroisothreonine derivatives as excellent building blocks.
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Selective synthesis of (Z)-2-enynyl-2-hydroxy-imidazolidine-4,5-diones via Cu(I)-mediated multicomponent coupling of terminal alkynes, carbodiimides and oxalyl chloride

13 May, 2014 - 17:54

Org. Biomol. Chem., 2014, 12,3336-3339
DOI: 10.1039/C4OB00185K, CommunicationFei Zhao, Yuexing Li, Yang Wang, Wen-Xiong Zhang, Zhenfeng Xi
(Z)-2-Enynyl-2-hydroxy-imidazolidine-4,5-diones are synthesized via Cu(I)-mediated (Z)-selective geminal coupling among two terminal alkynes, carbodiimides, and oxalyl chloride. Further transformation is explored.
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Symmetry as a new element to control molecular switches

13 May, 2014 - 17:54

Org. Biomol. Chem., 2014, 12,3371-3379
DOI: 10.1039/C4OB00230J, PaperOpen Access Open Access Creative Commons Licence&nbsp This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.Luca Schweighauser, Daniel Haussinger, Markus Neuburger, Hermann A. Wegner
The switching of a tetraazocarbazole macrocycle was investigated and an interdependence of individual azo units was observed depending on their special relationship.
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