- Twofold photoswitching of NIR fluorescence and EPR based on the PMI-N-HABI for optical nanoimaging of electrospun polymer nanowires
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In this article, we report the design and synthesis of a fluorescent molecular switch based on perylenemonoimide-hexaarylbiimidazole dyad (PMI-N-HABI), which exhibits not only photoswitchable near-infrared (NIR) fluorescence but also photoswitchable elect
- Gong, Wen-Liang,Xiong, Zu-Jing,Xin, Bo,Yin, Hong,Duan, Jia-Shun,Yan, Jie,Chen, Tao,Hua, Qiong-Xin,Hu, Bin,Huang, Zhen-Li,Zhu, Ming-Qiang
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- Reactive oxygen species (ROS) inducible DNA cross-linking agents and their effect on cancer cells and normal lymphocytes
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Reducing host toxicity is one of the main challenges of cancer chemotherapy. Many tumor cells contain high levels of ROS that make them distinctively different from normal cells. We report a series of ROS-activated aromatic nitrogen mustards that selectively kill chronic lymphocytic leukemia (CLL) over normal lymphocytes. These agents showed powerful DNA cross-linking abilities when coupled with H2O2, one of the most common ROS in cancer cells, whereas little DNA cross-linking was detected without H2O2. Consistent with chemistry observation, in vitro cytotoxicity assay demonstrated that these agents induced 40-80% apoptosis in primary leukemic lymphocytes isolated from CLL patients but less than 25% cell death to normal lymphocytes from healthy donors. The IC50 for the most potent compound (2) was ~5 μM in CLL cells, while the IC 50 was not achieved in normal lymphocytes. Collectively, these data provide utility and selectivity of these agents that will inspire further and effective applications.
- Chen, Wenbing,Balakrishnan, Kumudha,Kuang, Yunyan,Han, Yanyan,Fu, Min,Gandhi, Varsha,Peng, Xiaohua
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p. 4498 - 4510
(2014/07/07)
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- ANTI-CANCER AGENTS
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Described herein are compounds that may be selectively activated to produce active anti-cancer agents in tumor cells. Also disclosed are pharmaceutical compositions comprising the compounds, and methods of treating cancer using the compounds.
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Paragraph 0382; 0388
(2013/03/26)
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- 4′ Diphenylphosphino and bromo derivatives of 10-phenyl-1,4,7-trithia-10-azacyclododecane 4-R-C6H4N(CH2CH2S) 2CH2CH2SCH2CH2
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4-Br-C6H4N(CH2CH2S) 2CH2CH2SCH2CH2 and 4-Ph2P-C6H4N(CH2CH 2S)2CH2CH2SCH2CH 2 have been synthesized and characterized. The former cyclododcane has been obtained from the reaction between 4-BrC6H4N(CH2CH2Cl)2 and S(CH2CH2SH)2 in N,N-dimethylformamide containing Cs2CO3. The latter has been obtained from the former by way of a low temperature lithium-bromine exchange reaction (butyllithium) that provided the carbanion which was subsequently reacted with chlorodiphenylphosphine. In regard to characterization, X-ray methods have been used to study the former (P21 a = 8.356(3) A, b = 12.325(5) A, c = 16.012 (7), β = 100.81, Z = 4), and two crystallographically independent molecules were found. In both molecules, the nitrogen atoms are nearly planar with short N-C(Sp2) bond lengths, and, second, the sulfur atoms are in exodenate positions. For the phosphine, a 31P signal was observed at -7.1 ppm, and this peak position was considered to be indicative of a structure involving a planar nitrogen atom.
- Hoover, Lance R.,Pryor, Travis,Weitgenant, Jeremy A.,Williams, Peter E.,Storhoff, Bruce N.,Huffman, John C.
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p. 155 - 166
(2007/10/03)
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