6378-90-1Relevant articles and documents
Synthesis method of benzidine compound
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Paragraph 0047; 0048; 0051; 0052-0053; 0059; 0061, (2018/07/30)
The invention discloses a synthesis method of a benzidine compound. A compound (I) is subjected to catalytic coupling reaction to obtain a compound (II); the compound (II) is subjected to alkaline oracidic hydrolysis reaction process to obtain a compound (III); the compound (III) is subjected to catalytic hydrogenation reduction reaction in an organic system to obtain a benzidine compound (V); orthe compound (II) is subjected to catalytic hydrogenation reduction reaction in an organic solvent to obtain a compound (V); the compound (V) is subjected to alkaline or acidic hydrolysis reaction toobtain a compound (IV). The method disclosed by the invention overcomes various defects of the existing method; the conventional commercial catalysts are used; the reaction time is greatly shortened;the capacity is improved. Noteworthily, the organic solvent can be recovered and reused; hydroiodic acid or hydrobromide generated through coupling reaction can be smoothly converted into iodides orbromide salts with high economic values through treatment. Therefore, the method disclosed by the invention is an economic easy-to-industrialize green method.
Design, synthesis, and anti-tumor evaluation of novel symmetrical bis-benzimidazoles
Yang, Yan-Hui,Cheng, Mao-Sheng,Wang, Qing-He,Nie, Han,Liao, Na,Wang, Jian,Chen, Hong
experimental part, p. 1808 - 1812 (2009/06/28)
A novel symmetrical bis-benzimidazole was designed as DNA minor groove binder. Molecular modeling study showed that it could dock into the minor groove of DNA. Several derivatives were synthesized and confirmed by IR, MS, and 1H NMR. All these novel compounds were screened for cytotoxic activity on SKOV-3, HeLa, and BGC-823 cell lines in vitro. Some compounds showed IC50s in the single-digit micromolar range for cytotoxicity in several tumor cell lines.
Symmetric bis-benzimidazoles: New sequence-selective DNA-binding molecules
Neidle, Stephen,Mann, John,Rayner, Emma L.,Baron, Anne,Opoku-Boahen, Yaw,Simpson, Ian J.,Smith, Nicola J.,Keith R, Fox,Hartley, John A.,Kelland, Lloyd R.
, p. 929 - 930 (2007/10/03)
A series of bis-benzimidazole compounds with a head-to-head orientation have been designed as sequence-specific DNA binders; crystallographic analysis of oligonucleotide complexes has been combined with DNase I footprinting to confirm that the predicted optimal site for the core bisbenzimidazole motif is the four-base-pair sequence 5'-AATT; this sequence specificity results in inhibition of transcription at A/T sites and may be responsible for the cytotoxic and antitumour effects shown by these head-to-head bis-benzimidazoles.