On the formation of 4-[N,N-bis(2-chloroethyl)amino]phenyl acetic acid esters of hecogenin and aza-homo-hecogenin and their antileukemic activity.

Abstract

The p-[N,N-bis(2-chloroethyl)amino]phenylacetic acid esters of hecogenin and aza-homo-hecogenin have been prepared and their antineoplastic activity was evaluated against two basic drug screening systems in rodents, P388 lymphocytic and L1210 lymphoid murine leukemias. Among the compounds tested, the p-[N,N-bis(2-chloroethyl)amino]phenylacetic acid ester of aza-homo-hecogenin was appeared to possess a significant higher antileukemic effect. These results support that the alkylating esters of hecogenin produce important antitumor activity as well as, indicate that the aza-homo-hecogenin ester exhibits significantly higher activity due to lactam group (-NHCO-) modification.

• Authors: Charalambos Camoutsis, Dimitrios Trafalis, George Pairas, Athanasios Papageorgiou
• Journal: Farmaco (Societa chimica italiana : 1989) (Farmaco) Vol. 60 Issue 10 Pg. 826-9 (Oct 2005) ISSN: 0014-827X [Print] France
• PMID: 16139280 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Azasteroids
• Phenylacetates
• Sapogenins
• hecogenin

Topics

• Animals
• Antineoplastic Agents (chemistry, pharmacology, therapeutic use)
• Azasteroids (chemistry, pharmacology, therapeutic use)
• Drug Screening Assays, Antitumor
• Leukemia L1210 (drug therapy)
• Leukemia P388 (drug therapy)
• Mice
• Molecular Structure
• Phenylacetates (chemistry, pharmacology, therapeutic use)
• Sapogenins (chemistry, pharmacology, therapeutic use)
• Structure-Activity Relationship