Skalski et al.
JOCArticle
FIGURE 8. Calculated absorption and fluorescence spectra for a
model of 3a, which lacks deoxyribose and ribose sugars. The
vibrational frequencies and excited state displacements were calcu-
lated using DFT methods.
has also been found to be a candidate for clinical therapeutic
applications.19 The high specificity and yield of the cross-link
formed between 5F-4SU/5Cl-4SU and T presents new possibi-
lities in each of these realms of application. The geometry
formed in these solution studies is consistent with applications
in DNA heteroduplexes using a 5F-4SU/5Cl-4SU modified
nucleotide in an opposite flanking position to T. The creation of
a fluorescent crosslink under these conditions has potential
applications in both in vitro and in vivo identification of DNA
sequences.
FIGURE 7. Dissociation and rearrangement energies for reactions.
(A) The dissociation energies for the H-X (X = H, F, Cl, Br, I) series
is presented. (B) The rearrangement energy from the thietane-X
intermediate with atom X is presented for isomer 3a. (C) The
rearrangement energy is presented for isomer 3b.
Experimental Section
Synthesis of 1 and 2. 20,30,50-Tri-O-acetyl-5-halogeno-4-
thiouridines (X = F, Cl) were prepared as previously des-
cribed11 and subjected to de-O-acetylation with 2.5% ammo-
nium hydroxide in methanol/water mixture (1:1, v:v) to give the
corresponding unprotected nucleosides 1 and 2.
Photoreactions of 1 and 2 with T. For analytical scale experi-
ments aqueous solutions of 1 or 2 (0.2 mmol) containing an
equimolar amount of thymidine were placed in a 1 cm ꢀ 1 cm
UV cell, deoxygenated by bubbling argon, and irradiated on an
optical bench using a 200 W high-pressure mercury lamp
equipped with an interference filter to isolate the 366 nm line.
The progress of the reaction was monitored by UV spectro-
scopy and HPLC. The quantum yields for the disappearance of
1 and 2 were measured using benzophenone/benzhydrol actino-
metry.20
Preparative Irradiation for Product Analysis. The solutions of
1 or 2 (400 mL, 0.2 mmol) with T (2 equiv) were irradiated, in
portions, in a 80 mL photoreactor with a 150 W high pressure
mercury lamp through a Pyrex filter under an argon atmo-
sphere. Irradiation was continued to ca. 95% conversion of the
substrate as checked by HPLC. Irradiated solutions were col-
lected and concentrated under reduced pressure. The photo-
products were isolated from the residue by preparative HPLC
and identified by means of high resolution mass spectrometry
and NMR data as discussed above.
result in a fluorescent photoproduct. The case of iodine, 5I-
4SU is not comparable since loss of I by photolysis is facile.
12,13 The absorption and fluorescence spectra for the model of
3a, in which the sugar residue was replaced by a methyl group,
were also calculated (Figure 8) and are in agreement with the
measured spectra of 3a shown in Figure 3.
In summary, we have studied the formation of the photo-
product of 5X-4SU and T and shown that for X = F and Cl
there is a unique pair of isomeric photoproducts that form. The
photoproducts are fluorophores with higher fluorescence yield
than any known pyrimidine-pyrimidine adducts. The reaction
does not occur for X = H, Br, or I in agreement with cal-
culations. Thiouridine and thiothymidine have a wide range of
applications including template-directed photoligation,14
photoaffinity probes,3,15-17 and therapeutics.18 The 5Br-4SU
(13) Kawai, K.; Saito, I.; Sugiyama, H. Tetrahedron Lett. 1999, 40, 5721–
5724.
(14) Liu, J. Q.; Taylor, J. S. Nucleic Acids Res. 1998, 26, 3300–3304.
(15) Podar, M.; Perlman, P. S. RNA 1999, 5, 318–329.
(16) Saintome, C.; Clivio, P.; Fourrey, J. L.; Woisard, A.; Favre, A.
Tetrahedron Lett. 1994, 35, 873–876.
Computational Methods. The optimized ground state geome-
tries and potential energy surfaces Thietane-X-1,2 and diaster-
eomers 3a,b were obtained using the GGA functional21
(17) Saintome, C.; Clivio, P.; Fourrey, J. L.; Woisard, A.; Laugaa, P.;
Favre, A. Tetrahedron 2000, 56, 1197–1206.
(18) Parker, W. B.;Shaddix,S. C.; Rose, L. M.;Tiwari,K. N.;Montogmery,
J. A.; Secrist, J. A. III; Bennett, L. L., Jr. Biochem. Pharmacol. 1995, 50, 687–
695.
(20) Murov, S. L.; Carmichael, I.; Hug, G. L. Handbook of Photo-
chemistry, 2nd ed.; Marcel Dekker: New York, 1993; p 307.
(19) Xu, Y. Z.; Zhang, X.; Wu, H. C.; Massey, A.; Karran, P. Bioorg.
Med. Chem. Lett. 2004, 14, 995–997.
(21) Perdew, J. P.; Chevary, J. A.; Vosko, S. H.; Jackson, K. A.; Pederson,
M. R.; Singh, D. J.; Fiolhais, C. Phys. Rev. B 1992, 46, 6671–6687.
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