1341200-80-3Relevant academic research and scientific papers
Coolade. A Low-Foaming Surfactant for Organic Synthesis in Water
Lee, Nicholas R.,Cortes-Clerget, Margery,Wood, Alex B.,Lippincott, Daniel J.,Pang, Haobo,Moghadam, Farbod A.,Gallou, Fabrice,Lipshutz, Bruce H.
, p. 3159 - 3165 (2019/04/26)
Several types of reduction reactions in organic synthesis are performed under aqueous micellar-catalysis conditions (in water at ambient temperature), which produce a significant volume of foam owing to the combination of the surfactant and the presence of gas evolution. The newly engineered surfactant “Coolade” minimizes this important technical issue owing to its low-foaming properties. Coolade is the latest in a series of designer surfactants specifically tailored to enable organic synthesis in water. This study reports the synthesis of this new surfactant along with its applications to gas-involving reactions.
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies
Liang, Xuewu,Zang, Jie,Li, Xiaoyang,Tang, Shuai,Huang, Min,Geng, Meiyu,Chou, C. James,Li, Chunpu,Cao, Yichun,Xu, Wenfang,Liu, Hong,Zhang, Yingjie
, p. 3898 - 3923 (2019/04/25)
Concurrent inhibition of Janus kinase (JAK) and histone deacetylase (HDAC) could potentially improve the efficacy of the HDAC inhibitors in the treatment of cancers and resolve the problem of HDAC inhibitor resistance in some tumors. Here, a novel series
Synergistic effects in Fe nanoparticles doped with ppm levels of (Pd + Ni). A new catalyst for sustainable nitro group reductions
Pang, Haobo,Gallou, Fabrice,Sohn, Hyuntae,Camacho-Bunquin, Jeffrey,Delferro, Massimiliano,Lipshutz, Bruce H.
, p. 130 - 135 (2018/01/12)
A remarkable synergistic effect has been uncovered between ppm levels of Pd and Ni embedded within iron nanoparticles that leads to mild and selective catalytic reductions of nitro-containing aromatics and heteroaromatics in water at room temperature. NaBH4 serves as the source of inexpensive hydride. Broad substrate scope is documented, along with several other features including: low catalyst loading, low residual metal in the products, and recycling of the catalyst and reaction medium, highlight the green nature of this new technology.
JAK kinase inhibitor with 4-amino-(1H)-pyrazole structure and preparation method and application thereof
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Paragraph 0097; 0098, (2017/07/01)
The invention discloses a JAK kinase inhibitor with 4-amino-(1H)-pyrazole structure and a preparation method and application thereof. The compound has a structure shown in general formula (I) or (II), and the invention provides a specific preparation meth
Design, Synthesis, and Antitumor Evaluation of 4-Amino-(1H)-pyrazole Derivatives as JAKs Inhibitors
Liang, Xuewu,Zang, Jie,Zhu, Mengyuan,Gao, Qianwen,Wang, Binghe,Xu, Wenfang,Zhang, Yingjie
supporting information, p. 950 - 955 (2016/10/22)
Abnormalities in the JAK/STAT signaling pathway lead to many diseases such as immunodeficiency, inflammation, and cancer. Herein, we designed and synthesized a series of 4-amino-(1H)-pyrazole derivatives as potent JAKs inhibitors for cancer treatment. Res
2,4-Diarylamino-pyrimidines as kinase inhibitors co-targeting IGF1R and EGFRL858R/T790M
Chan, Shingpan,Han, Kun,Qu, Rong,Tong, Linjiang,Li, Yingjun,Zhang, Zhang,Cheng, Huimin,Lu, Xiaoyun,Patterson, Adam,Smaill, Jeff,Ren, Xiaomei,Ding, Jian,Xie, Hua,Ding, Ke
supporting information, p. 4277 - 4281 (2015/11/03)
IGF1R amplification was recently implied to be related to the secondary acquired resistance against the 2nd or 3rd generation EGFR inhibitor therapies. We have successfully identified a series of 2,4-diarylamino-pyrimidines as new IGF1R/EGFRL858R/T79
One-pot synthesis and antiproliferative activity of novel 2,4-diaminopyrimidine derivatives bearing piperidine and piperazine moieties
Ma, Wei-Feng,Yang, Hai-Kui,Hu, Meng-Jin,Li, Qian,Ma, Tian-Zhu,Zhou, Zhong-Zhen,Liu, Rui-Yuan,You, Wen-Wei,Zhao, Pei-Liang
, p. 127 - 134 (2014/07/22)
A series of novel 2,4-diaminopyrimidines containing piperidine and piperazine moieties were synthesized via an efficient one-pot methodology. The bioassay tests demonstrated that compounds 27 and 28 displayed much stronger antitumor activities against four human cancer cell lines (HepG2, A549, MDA-MB-231 and MCF-7) than positive control fluorouracil. Particularly, compound 28 showed a two-fold improvement compared to fluorouracil in inhibiting MDA-MB-231 and A549 cell proliferation with IC50 values of 7.46 and 12.78 μM, respectively. Further flow-activated cell sorting analysis revealed that the most promising compound 28 displayed a significant effect on G 2/M cell-cycle arrest in a dose-dependent manner in MDA-MB-231 cells.
Design, synthesis, and biological evaluation of a series of novel AXL kinase inhibitors
Mollard, Alexis,Warner, Steven L.,Call, Lee T.,Wade, Mark L.,Bearss, Jared J.,Verma, Anupam,Sharma, Sunil,Vankayalapati, Hariprasad,Bearss, David J.
supporting information; experimental part, p. 907 - 912 (2012/01/19)
The receptor tyrosine kinase AXL has emerged in recent years as an potential oncology target due to its overexpression in several types of cancers coupled with its ability to promote tumor growth and metastasis. To identify small molecule inhibitors of AXL, we built a homology model of its catalytic domain to virtually screen and identify scaffolds displaying an affinity for AXL. Further computational and structure-based design resulted in the synthesis of a series of 2,4,5-trisubstitued pyrimidines, which demonstrated potent inhibition of AXL in vitro (IC50 = 19 nM) and strongly inhibited the growth of several pancreatic cell lines.
