N-(5-fluorobenzothiazol-2-yl)-2-guanidinothiazole-4-carboxamide. A novel, systemically active antitumor agent effective against 3LL Lewis lung carcinoma.
N-(5-Fluorobenzothiazol-2-yl)-2-guanidinothiazole-4-carboxam ide (1) is a member of a series of amides found to substantially increase lifespan in mice bearing established micrometastatic 3LL Lewis lung carcinoma. Amide 1 is effective after either oral or intraperitoneal dosing in acute, subacute, or chronic regimens. 1 is well tolerated in this model with an excellent therapeutic index relative to the cytotoxic anticancer drug adriamycin.
Schnur
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Central Research Division, Pfizer, Inc., Groton, Connecticut 06340.
Fliri
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Kajiji
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Pollack
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D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000627:therapeutic use*; D055598:Chemical Phenomena; D002621:Chemistry; D004317:Doxorubicin / Q000627:therapeutic use; D006146:Guanidines / Q000008:administration & dosage / Q000737:chemistry / Q000627:therapeutic use*; D008175:Lung Neoplasms / Q000188:drug therapy*; D051379:Mice; D015394:Molecular Structure; D013844:Thiazoles / Q000008:administration & dosage / Q000737:chemistry / Q000627:therapeutic use*
D000970:Antineoplastic Agents; D006146:Guanidines; D013844:Thiazoles; C067815:N-(5-fluorobenzothiazol-2-yl)-2-guanidinothiazole-4-carboxamide; D004317:Doxorubicin