Compounds having structure (1) 
wherein R 1 is —H a protecting group, a linker or a binding partner; and R 2 and R 34 are as defined in the specification. The invention also provides intermediates and methods make the structure (1) compounds, as well as methods to use the compounds as labels in diagnostic assays and to enhance binding to complementary bases.

Pyrimidine derivatives for labeled binding partners

Publisher Summary This chapter focuses on the structure and function of alkyltransferase protein. O 6 -alkylguanine-DNA alkyltransferase is a remarkable protein that alone can, in a single step, remove adducts from DNA that are formed at the O 6 -position of guanine and the O 4 -position of thymine and can, thus, restore the original DNA. Production of such adducts is a major contributor to the toxic, mutagenic, and carcinogenic effects of alkylating agents. Alkyltransferase activity has been detected in many species, including microorganisms, insects, fish, and mammals. The unique activity of alkyltransferase suggests that it is an ideal target for biochemical modulation. The efficient repair of toxic lesions formed at the O 6 -position of guanine without additional enzymes or cofactors provides a less complex target to modulate than other DNA repair proteins. Furthermore, the high degree of correlation that exists between alkyltransferase activity and sensitivity to nitrosoureas indicates that elimination of this protein may reverse resistance in many cases. Two methods have been used to overcome alkylnitrosourea resistance by inactivation of alkyltransferase. One uses methylating agents that indirectly decrease alkyltransferase levels by introducing O 6 -methylguanine residues in DNA that are then repaired by the alkyltransferase. The second method uses direct alkyltransferase inactivators such as O 6 -methylguanine.

Structure, function, and inhibition of O6-alkylguanine-DNA alkyltransferase.

Synthesis of carbocyclic nucleosides

A method for preparing a polyurethane foam article in a mold by applying to a mold surface a water-based mold release composition which includes a release effective system which is in a solid (hardened) state at the mold pour temperature and a liquid state at the demold temperature, pouring a polyurethane foam composition into the mold, curing the foam composition and demolding the foam article. The use of such release effective system in the aqueous mold release composition provides for a reduction in surface defects of the polyurethane foam article. Also disclosed is the incorporation of a poly(siloxane-glycol) surfactant having a cloud point ranging from 25°-50° C. into a water-based mold release composition including an aqueous emulsion or dispersion of at least one release effective substance and desirably at least one emulsifying agent provides for improved surface quality of the foam product.

Water based mold release compositions for making molded polyurethane foam

The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate and/or modulate kinase receptor, particularly c-Met, KDR, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

c-Met modulators and methods of use

Synthesis of the carbocyclic analogs of uracil nucleosides

Carbocyclic analogs of thymine nucleosides and related 1‐substituted thymines

Carbocyclic analogues of 3'-deoxyuridines, 3'-deoxyuridines, and uridines with substituents at position 5 of the uracil moiety were prepared by direct halogenation (5-bromo and 5-iodo groups) and by displacement of the 5-bromo group by amino and substituted-amino groups. The analogue of 5-(hydroxymethyl)uridine was prepared via reaction of the isopropylidene derivative of the uridine analogue with paraformaldehyde. The carbocyclic analogues of thymidine and of 5-bromo-, 5-iodo-, and 5-(methylamino)-2'-deoxyuridine were highly active in vitro against herpes simplex virus, types 1 and 2. The corresponding analogues of 5-substituted 3'-deoxyuridines and of 5-substituted uridines were not active in this assay.

Carbocyclic analogues of 5-substituted uracil nucleosides: synthesis and antiviral activity.

Carbocyclic analogs of cytosine nucleosides

There are disclosed carbocyclic analogs of 2-amino-6-substituted-purine 2'-deoxyribofuranosides and 2-amino-6-substituted-8-azapurine 2'-deoxyribofuranosides. The compounds are useful in the treatment of viral infections.

C. Allen O'Dell

Papers

Synthesis of the carbocyclic analogs of uracil nucleosides

Carbocyclic analogs of thymine nucleosides and related 1‐substituted thymines

Carbocyclic analogues of 5-substituted uracil nucleosides: synthesis and antiviral activity.

Carbocyclic analogs of cytosine nucleosides

Carbocyclic analogs of purine 2'-deoxyribofuranosides