Cationic porphyrin-quinoxaline conjugate as a photochemically triggered novel cytotoxic agent.

Autor: Kumar D; Department of Chemistry, Birla Institute of Technology and Science, Pilani 333031, India. dalipk@pilani.bits-pilani.ac.in.com, Chandra Shekar KP, Mishra B, Kurihara R, Ogura M, Ito T
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Jun 01; Vol. 23 (11), pp. 3221-4. Date of Electronic Publication: 2013 Apr 06.
DOI: 10.1016/j.bmcl.2013.03.126
Abstrakt: A novel cationic porphyrin-quinoxaline conjugate 8 was prepared in good yield by the coupling of activated quinoxaline carboxylic acid 5 with an appropriate aminoporphyrin. The UV-vis spectra of conjugate 8 with the addition of ctDNA shows substantial hypochromicity (39%) and a red shift (12 nm) in the Soret band indicating intercalation and self stacking along the surface. The binding constant of conjugate 8 with ctDNA was determined to be 1.26×10(6) M(-1). The porphyrin-quinoxaline conjugate 8 displayed enhanced photocytotoxicity (IC50=0.06 μM) when compared to TMPyP against A549 cancer cells.
(Copyright © 2013 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE