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  • Title: Thienocoumarin derivatives: interaction with nucleic acids and synthetic polydeoxyribonucleotides.
    Author: Gia O, Via LD, Magno SM, Angelini G, Margonelli A, Rodighiero P.
    Journal: J Photochem Photobiol B; 2000 Jul; 56(2-3):132-8. PubMed ID: 11079473.
    Abstract:
    This paper reports the photobiological properties of two new thienocoumarins, 4,6,9-trimethyl-2H-thieno[3,2-g]-1-benzopyran-2-one (compound I) and the 6,9-dimethyl-4-methoxymethyl-2H-thieno[3,2-g]-1-benzopyran-2-one (compound II). Cell growth inhibition studies have revealed significant antiproliferative potency on human tumor cell lines. The photoaddition process of these tritium-labeled derivatives was investigated using various nucleic acid structures (calf thymus DNA, bacterial DNA, and synthetic polydeoxyribonucleotides). The results obtained show that both compounds photobind to DNA to a higher extent than 8-MOP, taken as the reference drug. The capacity to form interstrand crosslinks into DNA helix was also evaluated. Interestingly, notwithstanding the lack of cutaneous phototoxicity, II revealed a good ability to induce diadduct formation.
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