| Synthesis, anticancer activity and mitochondrial mediated apoptosis inducing ability of 2,5-diaryloxadiazole-pyrrolobenzodiazepine conjugates. | |
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MedLine Citation:
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PMID: 20732817 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A series of 2,5-diaryloxadiazole linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates have been prepared and evaluated for their anticancer activity. These conjugates have shown promising activity with GI50 values ranging from <0.1 to 0.29 microM. It is observed that some of these conjugates particularly 4a, 4d, 4i and 4l exhibit significant anticancer activity. Some detailed biological assays relating to the cell cycle aspects associated to Bax and caspases have been examined with a view to understand the mechanism of action of these conjugates. |
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Authors:
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Ahmed Kamal; D Dastagiri; M Janaki Ramaiah; E Vijaya Bharathi; J Surendranadha Reddy; G Balakishan; Pranjal Sarma; S N C V L Pushpavalli; Manika Pal-Bhadra; Aarti Juvekar; Subrata Sen; Surekha Zingde |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2010-08-01 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: 18 ISSN: 1464-3391 ISO Abbreviation: Bioorg. Med. Chem. Publication Date: 2010 Sep |
Date Detail:
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Created Date: 2010-09-06 Completed Date: 2010-12-30 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: England |
Other Details:
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Languages: eng Pagination: 6666-77 Citation Subset: IM |
Copyright Information:
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Copyright (c) 2010 Elsevier Ltd. All rights reserved. |
Affiliation:
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Chemical Biology Laboratory, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 607, India. ahmedkamal@iict.res.in |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Antineoplastic Agents / chemical synthesis*, chemistry, therapeutic use Apoptosis* Benzodiazepines / chemical synthesis, chemistry*, therapeutic use Caspases / metabolism Cell Cycle / drug effects Cell Line, Tumor Cyclin-Dependent Kinase 2 / metabolism Humans Male Mice Mice, Inbred NOD Mitochondria / drug effects* Neoplasms / drug therapy Oxadiazoles / chemical synthesis, chemistry* Tumor Suppressor Protein p53 / metabolism Xenograft Model Antitumor Assays bcl-2-Associated X Protein / metabolism |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents; 0/Oxadiazoles; 0/Tumor Suppressor Protein p53; 0/bcl-2-Associated X Protein; 12794-10-4/Benzodiazepines; EC 2.7.11.22/Cyclin-Dependent Kinase 2; EC 3.4.22.-/Caspases |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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