Potential antitumor agents. 23.(1) Cytotoxic and differentiating activity of compounds related to hexamethylenebisacetamide.
The synthesis of potential differentiating agents related to hexamethylenebisacetamide (HMBA) is reported. 1,6-Bis(3,3-dimethyl-2-oxo-2,3-dihydroindol-1-yl)hexane (4) and 1,6-bis(4-carbamoyl-thiazol-2-yl)hexane (9) were not soluble enough to allow biological testing. For this reason the dipotassium salt (10) of 1,6-bis(4-carboxy-thiazol-2-yl)hexane (11) was prepared. The salt 10, tested in the human rhabdomyosarcoma cell line (RMZ) and in the murine Friend erythroleukemia cells (MEL), proved more cytotoxic than HMBA, but was devoid of differentiating activity. Compounds 4, 9, 10 and 11, tested on HeLa cells (in vitro) and on Ehrlich ascites (in vivo) did not show antitumor activity.
Andreani
A
A
Dipartimento di Scienze Farmaceutiche, Università di Bologna, Italy.
Rambaldi
M
M
Locatelli
A
A
Andreani
F
F
Lollini
P L
PL
Nanni
P
P
Bossa
R
R
Galatulas
I
I
D000081:Acetamides / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002286:Carcinoma, Ehrlich Tumor / Q000473:pathology; D002454:Cell Differentiation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D017690:Cell Transplantation; D006367:HeLa Cells; D006801:Humans; D004915:Leukemia, Erythroblastic, Acute / Q000473:pathology; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D009368:Neoplasm Transplantation; D012208:Rhabdomyosarcoma / Q000473:pathology; D013055:Spectrophotometry, Infrared; D014407:Tumor Cells, Cultured
D000081:Acetamides; D000970:Antineoplastic Agents; C014026:hexamethylene bisacetamide