Τίτλος:
Synthesis and evaluation of new steroidal lactam conjugates with aniline mustards as potential antileukemic therapeutics
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
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.
Συγγραφείς:
Trafalis, D.
Geromichalou, E.
Dalezis, P.
Nikoleousakos, N.
Sarli, V.
Εκδότης:
ELSEVIER SCIENCE INC 360 PARK AVE SOUTH, NEW YORK, NY 10010-1710 USA
Λέξεις-κλειδιά:
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
DOI:
10.1016/j.steroids.2016.07.009
