- Entropy Versus Enthalpy Controlled Temperature/Redox Dual-Triggered Cages for Selective Anion Encapsulation and Release
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New C3-symmetric imidazole ligands were designed with phosphine and phosphine oxide linkers (LP and LPO, respectively) to demonstrate a dual-triggered dynamic closed coordination cage. Both LP and LPO
- Hamashima, Kyosuke,Yuasa, Junpei
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supporting information
(2021/12/16)
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- SUBSTITUTED BENZIMIDAZOLE CARBOXAMIDES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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The invention provides substituted benzimidazole carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat a medical disorder, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.
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Paragraph 00297; 00309-00310; 00371
(2021/04/01)
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- Deprotection of N-benzylbenzimidazoles and N-benzylimidazoles with triethylsilane and Pd/C
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The benzyl group is a protecting group for benzimidazoles and imidazoles that can survive acidic, basic, oxidizing, and reducing conditions. Deprotection, however, can require vigorous and potentially non-chemoselective methods. The triethylsilane–Pd/C reduction system is an exceptionally mild, convenient, and efficient method for deprotecting N-benzylbenzimidazoles that are unsubstituted at the 2- and 4-positions as well as suitably substituted N-benzylimidazoles.
- Graham, Thomas H.
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supporting information
p. 2688 - 2690
(2017/11/14)
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- Synthesis and antiproliferative evaluation of novel benzoimidazole- contained oxazole-bridged analogs of combretastatin A-4
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A series of novel oxazole-bridged analogs of combretastatin A-4 bearing a benzo[d]-imidazole as B ring were synthesized and evaluated for antiproliferative activities against five human cancer cell lines. Among all the synthesized compounds, the N-unsubstituted benzoimidazole analog 5 and the analogs 6b, 7a and 7b with a small hydrophobic group on nitrogen atom of benzoimidazole ring were identified as the most potent inhibitors of tumor cell growth with IC50 values at nanomolar levels (5, IC50 = 8.4 nM, HT29; 6b, 7a, 7b, IC50 = 9.6 nM, 3.8 nM, 3.0 nM, A549). In a murine H22 tumor xenograft model, compound 5 exhibited significant antitumor activity. The binding mode of compound 5 in the colchicine binding site of tubulin was probed.
- Zhou, Jie,Jin, Jing,Zhang, Yi,Yin, Yuwen,Chen, Xiaoguang,Xu, Bailing
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p. 222 - 232
(2013/10/01)
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- Synthesis and cytotoxic evaluation of N-(4-methoxy-1H-benzo[d]imidazol-7- yl)-arylsulfonamide and N-aryl-(4-methoxy-1H-benzo[d]imidazol)-7-sulfonamide analogs of combretastatin A-4
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Two series of novel benzoimidazole sulfonamides as combretastatin A-4 analogs were synthesized. The cytotoxicities of the title compounds were evaluated against five different cancer cell lines. Among the tested compounds, four compounds displayed cytotoxicities against the HCT8 cell line. Compound 6a has shown the strongest potency against the tested human tumor cell lines with an IC50 value ranging from submicromolar to micromolar level.
- Zhou, Jie,Zhang, Yi,Cui, Yi-Wen,Li, Zhan-Mei,Song, Hong-Rui,Dong, Jin-Hua,Chen, Xiao-Guang,Xu, Bai-Ling
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scheme or table
p. 330 - 340
(2011/06/19)
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