Antineoplastic Agents. 571. Total Synthesis of Bacillistatin 2

Mechanism-Based Inhibitors of Deoxythymidine Monophosphate Synthesis as Antineoplastic Agents

INTRODUCTION 5-Fluorouracil and methotrexate are antimetabolites widely used in the treatment of neoplastic disease. They act by inactivating the two enzymes involved in the biosynthesis of the pyrimidine nucleotide 2’-deoxythymidine 5’-monophosphate, namely thymidylate synthase and dihydrofolate reductase. The three dimensional structure of each enzyme is known and the mechanisms of the reacti...

Antineoplastic Agents

Antibacterial activities of antineoplastic agents.

Fourteen antineoplastic agents were examined for in vitro antibacterial activity against 101 aerobic and anaerobic bacterial isolates representing indigenous human microflora and selected opportunistic pathogens. Only 5-fluorouracil, mitomycin, and etoposide demonstrated inhibitory effects at achievable plasma concentrations, while the remaining drugs lacked appreciable antibacterial activities.

Handling of injectable antineoplastic agents.

Although the clinical toxicity of antineoplastic drugs has been well documented there is little or no information on the problems that may arise on the handling and mishandling of such agents. This paper attempts to highlight the importance of taking precautions to prevent adverse effects resulting from contact with cytotoxic drugs during handling and to suggest a practical guide for the handli...

Stereoselective Total Synthesis and Enantioselective Formal Synthesis of the Antineoplastic Sesquiterpene Quinone Metachromin A

A primeira síntese total da substância antitumoral de origem marinha metacromina-A (1) foi alcançada através de uma abordagem sintética convergente e aplicável a preparação de análogos para estudos biológicos. A síntese envolveu doze etapas na sua sequência mais longa e dezesseis no total, apresentando como destaques (1) a eficácia na síntese da quinona intermediária 11; (2) a preparação eficie...