TY - JOUR
TI - Synthesis and evaluation of new steroidal lactam conjugates with aniline mustards as potential antileukemic therapeutics
AU - Trafalis, D.
AU - Geromichalou, E.
AU - Dalezis, P.
AU - Nikoleousakos, N.
AU - Sarli, V.
JO - Steroids
PY - 2016
VL - 115
TODO - null
SP - 1-8
PB - ELSEVIER SCIENCE INC 360 PARK AVE SOUTH, NEW YORK, NY 10010-1710 USA
SN - 0039-128X
TODO - 10.1016/j.steroids.2016.07.009
TODO - 3 [4 [bis(2 chloroethyl)amino]phenoxy]propanoic acid;  alkylating agent;  aniline mustard derivative;  antileukemic agent;  enga dl02e;  enga l06e;  enga l07e;  enga l08e;  lactam derivative;  melphalan;  propionic acid;  sodium chloride;  steroidal lactam;  unclassified drug;  aniline mustard;  antineoplastic agent;  chlormethine;  lactam;  steroid, animal experiment;  animal model;  antineoplastic activity;  Article;  biological activity;  controlled study;  drug screening;  drug structure;  drug synthesis;  female;  human;  human cell;  in vitro study;  in vivo study;  LD10;  LD50;  leukemia cell line;  male;  mouse;  murine leukemia;  nonhuman;  animal;  Bagg albino mouse;  chemistry;  Jurkat cell line;  K-562 cell line;  Leukemia P388;  structure activity relation;  synthesis;  tumor cell line, Aniline Mustard;  Animals;  Antineoplastic Agents;  Cell Line, Tumor;  Female;  Humans;  Jurkat Cells;  K562 Cells;  Lactams;  Leukemia P388;  Male;  Mechlorethamine;  Mice, Inbred BALB C;  Steroids;  Structure-Activity Relationship
TODO - Alkylating agents are still nowadays one of the most important classes of cytotoxic drugs, which display a wide range of therapeutic use for the treatment of various cancers. We have synthesized and tested four hybrid homo-azasteroidal alkylating esters for antileukemic activity against five sensitive to alkylating agents human leukemia cell lines in vitro and against P388 murine leukemia in vivo. Comparatively, melphalan and 3-(4-(bis(2-chloroethyl)amino)phenoxy)propanoic acid (POPAM) were also examined. All the homo-aza-steroidal alkylators showed relatively lower acute toxicity, very promising and antileukemic activity both in vitro and in vivo. © 2016 Elsevier Inc.
ER -