Remarkable DNA binding affinity and potential anticancer activity of pyrrolo[2,1- c][1,4]benzodiazepine–naphthalimide conjugates linked through piperazine side-armed alkane spacers

A series of pyrrolobenzodiazepine–naphthalimide conjugates tethered through a piperazine ring system have been designed, synthesized, and evaluated for their anticancer activity. These new conjugates exhibit very high DNA binding affinity and cytotoxic activity against a number of cell lines.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-08, Vol.16 (15), p.7218-7224
Hauptverfasser:	Kamal, Ahmed, Ramu, R., Tekumalla, Venkatesh, Ramesh Khanna, G.B., Barkume, Madan S., Juvekar, Aarti S., Zingde, Surekha M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anticancer activity Antineoplastic agents Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biological and medical sciences Cell Line, Tumor DNA - chemistry DNA binding affinity Dose-Response Relationship, Drug General aspects Humans Medical sciences Molecular Structure Naphthalimides Naphthalimides - chemistry Naphthalimides - pharmacology Nucleic Acid Denaturation Pharmacology. Drug treatments Piperazine ring Pyrrolobenzodiazepines Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	A series of pyrrolobenzodiazepine–naphthalimide conjugates tethered through a piperazine ring system have been designed, synthesized, and evaluated for their anticancer activity. These new conjugates exhibit very high DNA binding affinity and cytotoxic activity against a number of cell lines.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2008.06.034