Synthesis of 1,2,3-triazole-linked pyrrolobenzodiazepine conjugates employing ‘click’ chemistry: DNA-binding affinity and anticancer activity

1,2,3-Triazole based molecules are useful pharmacophores for several DNA-alkylating and cross-linking agents. A series of A/C8, C/C2 and A/C8- C/C2-linked 1,2,3-triazole–PBD conjugates have been synthesized by employing ‘click’ chemistry. These molecules have exhibited promising DNA-binding affinity...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2008-02, Vol.18 (4), p.1468-1473
Main Authors: Kamal, Ahmed, Shankaraiah, N., Devaiah, V., Laxma Reddy, K., Juvekar, Aarti, Sen, Subrata, Kurian, Nisha, Zingde, Surekha
Format: Article
Language:English
Subjects:
1,2,3-Triazoles
Anticancer activity
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Benzodiazepines - chemical synthesis
Benzodiazepines - chemistry
Benzodiazepines - pharmacology
Biological and medical sciences
Cell Line, Tumor
DNA - chemistry
DNA - metabolism
DNA-binding affinity
General aspects
Humans
Kinetics
Medical sciences
Neoplasms - drug therapy
Neoplasms - genetics
Pharmacology. Drug treatments
Pyrroles - chemical synthesis
Pyrroles - chemistry
Pyrroles - pharmacology
Pyrrolo[2,1- c][1,4]benzodiazepines
Triazoles - chemical synthesis
Triazoles - chemistry
Triazoles - pharmacology
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Summary:1,2,3-Triazole based molecules are useful pharmacophores for several DNA-alkylating and cross-linking agents. A series of A/C8, C/C2 and A/C8- C/C2-linked 1,2,3-triazole–PBD conjugates have been synthesized by employing ‘click’ chemistry. These molecules have exhibited promising DNA-binding affinity and anticancer activity in selected human cancer cell lines.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.12.063