In the Search for New Anticancer Drugs, XXI. Spin Labeled Nitrosoureas

Sosnovsky, George; Li, SW; Nu, Rao

doi:10.1515/znc-1987-7-832

Cited by 16 publications

(1 citation statement)

References 8 publications

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“…This compound causes inhibi- [10, 12 -14, 17, 80] in clinical development include tomudex (24) and other folate antimetabolites [10,80], which can compete with reduced folates and, thus, inhibit TS. Tomudex is a water-soluble quinazoline antifolate which enters cells via the reduced folate carrier (RFC) and undergoes rapid intracellular polyglutamation, resulting in longer residence time inside the cell and, thus, a greater in vivo activity [81].…”

Section: Folate Antagonists and Thymidylate Synthase Inhibitorsmentioning

confidence: 99%

Critical appraisals of approaches for predictive designs in anticancer drugs

Gnewuch

Sosnovsky

2002

Cellular and Molecular Life Sciences (CMLS)

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The present review provides a critical appraisal of the most important areas in cancer drug research and, ultimately, in clinical oncology and therapy, with emphasis on the elucidation of possible predictive designs for the development of new anticancer drugs. These assessments encompass the well-established anticancer drugs and congeners which have been employed over the years in clinical therapy, and the more recent exploratory agents still requiring further rigorous scrutiny in the clinical environment. These areas mainly include the bioreversible redox carriers, the boron neutron capture compounds, some new mitosis-interactive agents, cell cycle modifiers, biological-response mpdifiers, oncogene inhibitors, drug-antibody conjugates, cancer cell suppression and destruction agents, antiangiogenesis and antimetastasis agents, apoptosis-promoting agents, and gene therapy and vaccines.

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Section: Folate Antagonists and Thymidylate Synthase Inhibitorsmentioning

confidence: 99%

Critical appraisals of approaches for predictive designs in anticancer drugs

Gnewuch

Sosnovsky

2002

Cellular and Molecular Life Sciences (CMLS)

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Reductive Aminations of Carbonyl Compounds with Borohydride and Borane Reducing Agents

2002

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Reductive amination is an important tool for synthetic organic chemists in the construction of carbon‐nitrogen bonds. This reaction, also termed reductive alkylation, involves condensation of an aldehyde or ketone with an amine in the presence of a reducing agent. A wide variety of substrates can be used including aliphatic and aromatic aldehydes and ketones, and even benzophenones. A range of amines from ammonia to aromatic amines, including those with electron‐withdrawing substituents, can be employed. For particularly sluggish reactions, such as those involving weakly electrophilic carbonyl groups, poorly nucleophilic amines, or sterically congested reactive centers, additives such as molecular sieves or Lewis acids are often useful. This chapter focuses on those conditions in which the carbonyl component, amine, and reducing reagent react in the same vessel. This review is restricted to reductive aminations using borohydride and borane reducing agents. This chapter concentrates on reductive amination chemistry mediated by borohydride and other boron‐containing reducing agents from 1971, the year when sodium cyanoborohydride was introduced, through the middle of 1999. In addition to reductive aminations of aldehyde and ketone substrates, reactions of related structures including acetals, aminals, ketals, carboxylic acids, nitriles, and dicarbonyls that form a nitrogen‐containing ring are reviewed. Intramolecular processes in which the substrate contains both the carbonyl and amine moieties are described. The intramolecular variant is a useful method for preparing cyclic amines. All of the various boron‐containing hydride sources in reductive aminations, including labeled metal hydrides, are reviewed. Instances of reductive aminations that failed are described. Applications of this method to a solid support in parallel synthesis in combinatorial chemistry as well as reductive aminations that proceed in tandem with a second reaction such as reductive lactamizations are discussed.

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