ChemInform Abstract: SYNTH. UND TUMORHEMMENDE WIRKUNG VON N‐(BIS‐(2‐CHLORAETHYL)‐AMINOMETHYL)‐AMIDEN 21. MITT. UEBER CYTOSTATICA

Abstract

Durch Umsetzung der N‐Chlormethyl‐amide (I) mit Nor‐Lost (II) in Gegenwart von Triäthylamin werden in Äther bei 0°C in guten Ausbeuten die N‐(Bis‐ (2‐chloräthyl)‐aminomethyl)‐amide (III) erhalten.

Evaluation of Nuclear‐substituted Styryl Ketones and Related Compounds for Antitumor and Cytotoxic Properties

“…It is known that Mannich bases have antitumor properties (9,10) and the formation of the water-soluble Mannich bases derived from a,&unsaturated ketones seems of interest. The higher chemical and biological reactivity of allyl alcohol compared to the saturated analog (11,12) suggested the synthesis of substituted allyl alcohols as potential alkylating agents.…”

Synthesis and Physical Properties of Substituted 4-Dimethylaminomethyl-1-phenyl-1-nonen-3-ones Possessing Antitumor Properties

“…In studies of the synthesis of novel antineoplastic agents, it was of interest to prepare a series of nuclear-substituted styryl ketones (I) and the related Mannich bases (11), both groups being a,p-unsaturated ketones. Conjugated olefinic ketones may be regarded as alkylating agents due to their ability to undergo addition reactions with such biologically important nucleophiles as amines and thiols.…”

“…Mannich bases exhibit various biological responses (9) and have shown activity against certain tumors, including the Ehrlich ascites carcinoma (lo), and in the sarcoma 180 screen (11).…”