- Synthesis, anticancer evaluation and molecular docking studies of new benzimidazole- 1,3,4-oxadiazole derivatives as human topoisomerase types I poison
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In this study, some benzimidazole-oxadiazole derivatives were synthesised and tested for their in vitro anticancer activities on five cancer cell lines, including HeLa, MCF7, A549, HepG2 and C6. Their structures were elucidated by IR, 1H-NMR,
- Acar ?evik, Ulviye,Atl? Eklio?lu, ?zlem,Atl?d, ?zlem,Kaplanc?kl?, Zafer As?m,Karaduman, Abdullah Burak,Kaya ?avu?o?lu, Betül,Levent, Serkan,Osmaniye, Derya,Sa?l?k, Begüm Nurpelin
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- Design, synthesis, molecular modeling, DFT, ADME and biological evaluation studies of some new 1,3,4-oxadiazole linked benzimidazoles as anticancer agents and aromatase inhibitors
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Breast cancer is the most frequent female cancer and second cause of cancer-related deaths among women around the world. Two thirds of breast cancer patients have hormone-dependent tumors, which is very likely be treated with hormonal therapy. Aromatase i
- Ahmad, Iqrar,Celik, Ismail,Patel, Harun,?zkay, Yusuf,Acar ?evik, Ulviye,I??k, Ay?en,Kaplanc?kl?, Zafer As?m
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- Synthesis and biological evaluation of benzimidazole-oxindole conjugates as microtubule-targeting agents
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A series of benzimidazole-oxindole conjugates were synthesized and evaluated for their cytotoxic activity. The cytotoxicity assay results suggest that conjugates 5c and 5p exhibit promising cytotoxicity against human breast cancer cell line (MCF-7). The Cell cycle analysis revealed that these conjugates induced cell cycle arrest at G2/M phase in MCF-7 cells. The tubulin polymerization assay results suggested that these conjugates inhibit tubulin polymerization with IC50 values 1.12 and 1.59 μM respectively. Immunofluorescence analysis also suggested that these conjugates effectively inhibited the microtubule assembly in MCF-7 cells. Further, molecular docking studies indicated that these conjugates 5c and 5p interact and binds efficiently with the tubulin protein. By and large, the results demonstrated that these benzimidazole-oxindole conjugates possess cytotoxic property by inhibiting the tubulin polymerization.
- Kamal, Ahmed,Nagaseshadri,Nayak, V. Lakshma,Srinivasulu, Vunnam,Sathish, Manda,Kapure, Jeevak Sopanrao,Suresh Reddy
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- Selective autoxidation of benzylamines: Application to the synthesis of some nitrogen heterocycles
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A green and remarkably simple synthesis of nitrogen heterocycles from benzylamines and anilines o-substituted by a cyclizable group has been developed based on selective uncatalyzed autoxidation of benzylamines.
- Nguyen, Thanh Binh,Ermolenko, Ludmila,Al-Mourabit, Ali
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supporting information
p. 2713 - 2717
(2013/10/08)
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- SYNTHESIS AND DNA BINDING PROPERTIES OF A PURINE ANALOGUE OF BISBENZIMIDE
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The synthesis of a purine containing analogue (1) of bisbenzimide (2) and its DNA binding properties are described.Analogue 1 is found to have increased tolerance for binding to GC sites implying the formation of the new hydrogen bonds between guanine-2-N
- Lee, Moses,Spotts, P. Hunter,Eckert, Jeffrey,Walker, Clint,Nobles, Jennifer A.
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p. 2093 - 2097
(2007/10/02)
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