Aims: To synthesize small molecule alkylating compounds and analyze the kinetics of the alkylation in aqueous solution. Determine molecular properties and the drug likeness of these four compounds as potential antineoplastic agents and apply statistical analysis to identify interrelationships of properties. Study Design: Four compounds were synthesized, characterized, and studied for alkylation...

Mammary and skin tumors induced in rodents by ¿Y-methyl-/V-nitrosourea treatment have a (.:( to A: I transition mutation in codon 12 of I I-/Õ/.Y, probably resulting from alkylation of <>" of guanine by the carcinogen. This codon contains two guanines (5'-GGA-3'), but mutations are observed only in the central base pair of this codon. The same selectivity for mutations of -GGA-sequences has a...

In this paper we describe new multi-catalysis cascade (MCC) reactions for the one-pot synthesis of highly functionalized non-symmetrical malonates. These metal-free reactions are either five-step (olefination/hydrogenation/alkylation/ketenization/esterification) or six-step (olefination/hydrogenation/alkylation/ketenization/esterification/alkylation), and employ aldehydes/ketones, Meldrum's aci...

DNA damage is unavoidable, and organisms across the evolutionary spectrum possess DNA repair pathways that are critical for cell viability and genomic stability. To understand the role of base excision repair (BER) in protecting eukaryotic cells against alkylating agents, we generated Schizosaccharomyces pombe strains mutant for the mag1 3-methyladenine DNA glycosylase gene. We report that S. p...

Mammary and skin tumors induced in rodents by N-methyl-N-nitrosourea treatment have a G:C to A:T transition mutation in codon 12 of H-ras, probably resulting from alkylation of O6 of guanine by the carcinogen. This codon contains two guanines (5'-GGA-3'), but mutations are observed only in the central base pair of this codon. The same selectivity for mutations of -GGA-sequences has also been ob...

Alkylation of ribonuclease A by iodoacetamide at pH 5.5 yields two products: inactive 3-carboxamidomethylhistidine12.ribonuclease and fully active S-carboxamidomethylmethionine ribonuclease. No derivative substituted at histidine-119 was detected. This is in marked contrast to the products obtained on alkylation by iodoacetate at pH 5.5. The rate of alkylation of histidine in ribonuclease by io...

Perchlorate (ClO(4)(-)) is a persistent contaminant found in drinking groundwater sources in the United States. Ion exchange (IX) with selective and disposable resins based on cross-linked styrene divinylbenzene (STY-DVB) beads is currently the most commonly utilized process for removing low concentrations of ClO(4)(-) (10-100 ppb) from contaminated drinking water sources. However, due to the l...

By incubating Ehrlich cells with isotopically labeled nitrogen mustards the relation between the extent of alkylation of cell constituents and the reduction of growth potential can be studied. Data obtained by such studies show that both CQM and HN2 react with a wide variety of cell constituents. Of the macromolecular constituents, the proteins undergo the greatest amount of alkylation, but the...