Antitumor activity of SRI 62-834, a cyclic ether analog of ET-18-OCH3.
SRI 62-834, an analog of the antitumor agent ET-18-OCH3 in which the oxygen atom at carbon atom 2 has been incorporated into a five-membered heterocycle, has been prepared and evaluated as an antitumor agent. The compound exhibited good cytotoxicity in vitro against a variety of tumor cell lines and was as effective as ET-18-OCH3 given orally in the mouse Meth A sarcoma model. SRI 62-834 was shown to be an inhibitor of platelet-derived growth factor (PDGF), possibly at the receptor level, and platelet-activating factor (PAF) at the receptor level.
Houlihan
W J
WJ
Sandoz Research Institute, East Hanover, New Jersey 07936.
Lee
M L
ML
Munder
P G
PG
Nemecek
G M
GM
Handley
D A
DA
Winslow
C M
CM
Happy
J
J
Jaeggi
C
C
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002460:Cell Line; D002471:Cell Transformation, Neoplastic / Q000187:drug effects; D003603:Cytotoxins / Q000494:pharmacology; D005663:Furans / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D008807:Mice, Inbred BALB C; D008810:Mice, Inbred C57BL; D010742:Phospholipid Ethers / Q000138:chemical synthesis / Q000494:pharmacology*; D011493:Protein Kinase C / Q000378:metabolism; D011956:Receptors, Cell Surface / Q000187:drug effects; D017479:Receptors, Platelet-Derived Growth Factor; D014407:Tumor Cells, Cultured / Q000187:drug effects* / Q000378:metabolism
D000970:Antineoplastic Agents; D003603:Cytotoxins; D005663:Furans; D010742:Phospholipid Ethers; D011956:Receptors, Cell Surface; C055462:SRI 62-834; C026659:edelfosine; D017479:Receptors, Platelet-Derived Growth Factor; D011493:Protein Kinase C