Nitrostyrene Derivatives of Adenosine 5′-Glutarates Modified with an Alkyl Spacer and their inhibitory activity on epidermal growth factor receptor protein tyrosine kinase

β-Nitrostyrene derivatives of adenosine 5′-glutarates are potent and selective bisubstrate-type inhibitors of the epidermal growth factor receptor protein tyrosine kinase (EGF-R PTK). In an attempt to improve the inhibitory activity, this type of compounds was modified with alkyl spacers of varying length between the nitrostyrene and the glutaryl units. The spacers consisted of 1, 3, 4, and 5 atoms to give compounds of the benzyl, oxyethyl, oxypropyl, and oxybutyl series, respectively (Schemes 1 and 2). Adenosine 5′-esters were prepared in the benzyl and oxypropyl series only. Compared to the compounds in the parent series without spacer (IC₅₀ = 0.7–12 μM ), most of the modified compounds inhibited the EGF-R PTK only marginally or were inactive (IC₅₀ ≥ 100 μM ). The only exceptions were the free acids 19 and 20 with IC₅₀ values of ca. 5 μM . It is noteworthy that esterification of these two hydrogen glutarates with either MeOH or adenosine yielded inactive compounds, which is in contrast to the corresponding substances without spacers.     

Synthesis of Benzazepine Analogues of Noscapine

The synthesis of benzazepine analogues of the opium alkaloid noscapine ( 1 ) is described. The benzazepines 2 and 3 were prepared starting from nornarceine ethyl ester ( 4 ; readily available from 1 ) in several steps. X-Ray analysis of compound 2 revealed that it is not a diastereosisomer mixture but a racemate of the threo-form and thus has the same configuration as 1 .     

Hyperfine magnetic fields at sp-sites in Co2YZ Heusler alloys

The systematics of hyperfine magnetic fields at sp impurities on the Z-sites in Co based Heusler alloys are investigated. New TDPAC measurements of Cd hyperfine fields are reported.     

Concerning seven and eight mutually orthogonal Latin squares

In this paper, three new direct Mutually Orthogonal Latin Squares (MOLS) constructions are presented for 7 MOLS(24), 7 MOLS(75) and 8 MOLS(36); then using recursive methods, several new constructions for 7 and 8 MOLS are obtained. These reduce the largest value for which 7 MOLS are unknown from 780 to 570, and the largest odd value for which 8 MOLS are unknown from 1935 to 419. © 2003 Wiley Periodicals, Inc.