24376-18-9Relevant articles and documents
Isocyanate-, isothiocyanate-, urea-, and thiourea-substituted boron dipyrromethene dyes as fluorescent probes
Ziessel, Raymond,Bonardi, Laure,Retailleau, Pascal,Ulrich, Gilles
, p. 3093 - 3102 (2006)
Boron dipyrromethene dyes (Bodipy) bearing a meso-phenyl substituent carrying a variety of functional groups can be prepared under mild conditions. A single-crystal X-ray structure determination for the 3,5-dinitrophenyl compound shows the phenyl ring to
Convenient synthesis of isocyanate and isothiocyanate-substituted boron dipyrromethene dyes and derivatives
Bonardi, Laure,Ulrich, Gilles,Ziessel, Raymond
, p. 450 - 454 (2006)
Starting from nitro-substituted phenyl rings, the preparation of boron dipyrromethene dyes carrying amino functions was achieved in good yields. Conversion of the p-aminophenyl group to the corresponding isocyanate and isothiocyanate is feasible under mil
Discovery of a Candidate Containing an (S)-3,3-Difluoro-1-(4-methylpiperazin-1-yl)-2,3-dihydro-1 H-inden Scaffold as a Highly Potent Pan-Inhibitor of the BCR-ABL Kinase including the T315I-Resistant Mutant for the Treatment of Chronic Myeloid Leukemia
Zhang, Dongfeng,Li, Peng,Gao, Yongxin,Song, Yaoyao,Zhu, Yaqin,Su, Hong,Yang, Beibei,Li, Li,Li, Gang,Gong, Ningbo,Lu, Yang,Shao, Huanjie,Yu, Chunrong,Huang, Haihong
, p. 7434 - 7452 (2021/06/25)
BCR-ABL kinase inhibition is an effective strategy for the treatment of chronic myeloid leukemia (CML). Herein, we report compound 3a-P1, bearing a difluoro-indene scaffold, as a novel potent pan-inhibitor against BCR-ABL mutants, including the most refractory T315I mutant. As the privileged (S)-isomer compared to its (R)-isomer 3a-P2, 3a-P1 exhibited potent antiproliferative activities against K562 and Ku812 CML cells and BCR-ABL and BCR-ABLT315I BaF3 cells, with IC50 values of 0.4, 0.1, 2.1, and 4.7 nM, respectively. 3a-P1 displayed a good safety profile in a battery of assays, including single-dose toxicity, hERG K+, and genotoxicity. It also showed favorable mice pharmacokinetic properties with a good oral bioavailability (32%), a reasonable half-life (4.61 h), and a high exposure (1386 h·ng/mL). Importantly, 3a-P1 demonstrated a higher potency than ponatinib in a mice xenograft model of BaF3 harboring BCR-ABLT315I. Overall, the results indicate that 3a-P1 is a promising drug candidate for the treatment of CML to overcome the imatinib-resistant T315I BCR-ABL mutation.
Amide and ester derivatives of chlorido[4-carboxy-1,2-disalicylideneaminobenzene]iron(iii) as necroptosis and ferroptosis inducers
Baecker, Daniel,Gust, Ronald,H?rschl?ger, Carina,Kircher, Brigitte,Ma, Benjamin N.,Sagasser, Jessica,Schultz, Lukas,Steiner, Lucy,Weinreich, Maria
supporting information, p. 6842 - 6853 (2020/06/08)
In continuation of the structure-activity study about 4-substituted chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(iii) complexes as necroptosis and ferroptosis inducers, we introduced a 4-COOH group at the 1,2-phenylenediamine moiety of the lead
BIS-BENZIMIDAZOLE COMPOUNDS AND METHODS OF USING SAME
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Paragraph 001100-001102; 001106-001108, (2019/06/05)
Provided herein are compounds and methods for modulating abnormal repeat expansions of gene sequences. More particularly, provided are inhibitors of RNA and the uses of such inhibitors in regulating nucleotide repeat expansions, e.g., to treat Myotonic Dystrophy Type 1 (DM1 ), Myotonic Dystrophy Type 2 (DM2), Fuchs dystrophy, Huntington Disease, Amyotrophic Lateral Sclerosis, or Frontotemporal Dementia.
Mechanism-Inspired Design of Bifunctional Catalysts for the Alternating Ring-Opening Copolymerization of Epoxides and Cyclic Anhydrides
Abel, Brooks A.,Lidston, Claire A. L.,Coates, Geoffrey W.
supporting information, p. 12760 - 12769 (2019/08/26)
Advances in catalysis have enabled the ring-opening copolymerization of epoxides and cyclic anhydrides to afford structurally and functionally diverse polyesters with controlled molecular weights and dispersities. However, the most common systems employ b
Synthesis and anticancer activity of novel water soluble benzimidazole carbamates
Cheong, Jae Eun,Zaffagni, Michela,Chung, Ivy,Xu, Yingjie,Wang, Yiqiang,Jernigan, Finith E.,Zetter, Bruce R.,Sun, Lijun
, p. 372 - 385 (2018/01/01)
Metastases account for more than 90% of all cancer deaths and respond poorly to most therapies. There remains an urgent need for new therapeutic modalities for the treatment of advanced metastatic cancers. The benzimidazole methylcarbamate drugs, commonly
Synthesis and investigation of novel benzimidazole derivatives as antifungal agents
Chandrika, Nishad Thamban,Shrestha, Sanjib K.,Ngo, Huy X.,Garneau-Tsodikova, Sylvie
, p. 3680 - 3686 (2016/07/20)
The rise and emergence of resistance to antifungal drugs by diverse pathogenic fungal strains have resulted in an increase in demand for new antifungal agents. Various heterocyclic scaffolds with different mechanisms of action against fungi have been investigated in the past. Herein, we report the synthesis and antifungal activities of 18 alkylated mono-, bis-, and trisbenzimidazole derivatives, their toxicities against mammalian cells, as well as their ability to induce reactive oxygen species (ROS) in yeast cells. Many of our bisbenzimidazole compounds exhibited moderate to excellent antifungal activities against all tested fungal strains, with MIC values ranging from 15.6 to 0.975?μg/mL. The fungal activity profiles of our bisbenzimidazoles were found to be dependent on alkyl chain length. Our most potent compounds were found to display equal or superior antifungal activity when compared to the currently used agents amphotericin B, fluconazole, itraconazole, posaconazole, and voriconazole against many of the strains tested.
Design and synthesis of a novel candidate compound NTI-007 targeting sodium taurocholate cotransporting polypeptide [NTCP]-APOA1-HBx-Beclin1-mediated autophagic pathway in HBV therapy
Zhang, Jin,Fu, Lei-Lei,Tian, Mao,Liu, Hao-Qiu,Li, Jing-Jing,Li, Yan,He, Jun,Huang, Jian,Ouyang, Liang,Gao, Hui-Yuan,Wang, Jin-Hui
, p. 976 - 984 (2015/03/04)
Sodium taurocholate cotransporting polypeptide (NTCP) is a multiple transmembrane transporter predominantly expressed in the liver, functioning as a functional receptor for HBV. Through our continuous efforts to identify NTCP as a novel HBV target, we designed and synthesized a series of new compounds based on the structure of our previous compound NT-5. Molecular docking and MD simulation validated that a new compound named NTI-007 can tightly bind to NTCP, whose efficacy was also measured in vitro virological examination and cytotoxicity studies. Furthermore, autophagy was observed in NTI-007 incubated HepG2.2.15 cells, and results of q-PCR and Western blotting revealed that NTI-007 induced autophagy through NTCP-APOA1-HBx-Beclin1-mediated pathway. Taken together, considering crucial role of NTCP in HBV infection, NTCP-mediated autophagic pathway may provide a promising strategy of HBV therapy and given efficacy of NTI-007 triggering autophagy. Our study suggests pre-clinical potential of this compound as a novel anti-HBV drug candidate.
A practical fluorogenic substrate for high-throughput screening of glutathione S-transferase inhibitors
Fujikawa, Yuuta,Morisaki, Fumika,Ogura, Asami,Morohashi, Kana,Enya, Sora,Niwa, Ryusuke,Goto, Shinji,Kojima, Hirotatsu,Okabe, Takayoshi,Nagano, Tetsuo,Inoue, Hideshi
supporting information, p. 11459 - 11462 (2015/08/18)
We report a new fluorogenic substrate for glutathione S-transferase (GST), 3,4-DNADCF, enabling the assay with a low level of nonenzymatic background reaction. Inhibitors against Noppera-bo/GSTe14 from Drosophila melanogaster were identified by high throu
