Syntheses, photophysical properties, and application of through-bond energy-transfer cassettes for biotechnology.

We have designed fluorescent "through-bond energy-transfer cassettes" that can harvest energy of a relatively short wavelength (e.g., 490 nm), and emit it at appreciably longer wavelengths without significant loss of intensity.

Fluorescent, through-bond energy transfer cassettes for labeling multiple biological molecules in one experiment.

Through-bond energy transfer cassettes based on a fluorescein donor component electronically conjugated to rhodamine-like acceptors have been designed and synthesized. They absorb strongly at 488 nm (Ar-laser emission) and efficiently transfer the energy to the acceptor component that emits strongly. Further, the cassettes are more stable to photobleaching than fluorescein, making them potentially more suitable for single-molecule detection methods than fluorescein itself.

Rigid, conjugated, fluoresceinated thymidine triphosphates: syntheses and polymerase mediated incorporation into DNA analogues.

Syntheses of a unique set of energy transfer dye labeled nucleoside triphosphates, compounds 1-3, are described. Attempts to prepare these compounds were only successful if the triphosphorylation reaction was performed before coupling the dye to the nucleobase, and not the other way around. Compounds were prepared as both the 2'-deoxy (a) and 2',3'-dideoxy- (b) forms.

Microwave-assisted syntheses of regioisomerically pure bromorhodamine derivatives.

[structure: see text] Regioisomerically pure bromo-substituted rhodamine derivatives (bromorosamines) were prepared via microwave-accelerated condensation reactions followed by oxidation with chloranil. Reaction optimization was conveniently performed by monitoring UV absorptions attributed to the product.

Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.

A series of novel compounds have been designed that are potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1), and the activity and physical properties have been characterized. The new structural classes, 3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-6-ones and 3,4-dihydropyrrolo[4,3,2-de]isoquinolin-5-(1H)-ones, have conformationally locked benzamide cores that specifically interact with the PARP-1 protein. The compounds have been evaluated with in vitro cellular assays that measure the ability of the PARP-1 inhibitors to enhance the effect of cytotoxic agents against cancer cell lines.