Novel cyanoguanidines with potent oral antitumour activity

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 24, 1997, Pages 3095-3100

  Schou, Charlotte ^a   Ottosen, Erik R ^a   Petersen, Hans Jørgen ^a   Björkling, Fredrik ^a   Latini, Scilla ^a   Hjarnaa, Pernille V ^a   Bramm, Erik ^a   Binderup, Lise ^a  

^a Leo Pharmaceutical Products ^*  (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; DAUNORUBICIN; GUANIDINE DERIVATIVE; N (6 CHLOROPHENOXYHEXYL) N' CYANO N'' (4 PYRIDYL)GUANIDINE; PACLITAXEL; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; BREAST CANCER; CANCER CELL CULTURE; CONTROLLED STUDY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VITRO STUDY; INFRARED SPECTROPHOTOMETRY; INTRAPERITONEAL DRUG ADMINISTRATION; LUNG CANCER; LUNG SMALL CELL CANCER; MOUSE; NONHUMAN; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; ORAL DRUG ADMINISTRATION; STRUCTURE ACTIVITY RELATION; SUBCUTANEOUS DRUG ADMINISTRATION;

ANIMALIA; MINK CELL FOCUS-FORMING VIRUS; MUS MUSCULUS;

EID: 0031472361     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)10152-4     Document Type: Article

References (11)

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5. Aabo, K.; Roed, H.; Videlov, L.L.; Spang-Thomsen, M. Cancer Res. 1994, 54, 3295-3299.
6. Nagy, J.A.; Meyers, M.S.; Masse, E.M.; Herzberg, K.T.; Dvorak, H.F. Cancer Res. 1995, 55, 369-375.
7. Gáti, E.; Pokorny, É.; Somfai-relle, R.; Szentirmay, Z. Int. J. Tiss. Reac. 1984, 6, 43-51.
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11. 5O) Calcd. C: 61.34, H: 5.96; N: 18.83. Found C: 61.20, H:6.00, N: 18.92. Alternative procedure: N-(6-(4-Chlorophenoxy)hexyl)-N′-4-pyridylthiourea (4.0 g, 11 mmol) was suspended in acetonitrile (23 ml) and dicyclohexylcarbodiimide (4.5 g, 22 mmol), cyanamide (0.92 g, 22 mmol) and triethylamine (0.15 ml, 1.1 mmol) were added. The mixture was stirred at room temperature for 9 days, and the reaction mixture was filtered and washed with acetonitrile. The white solid containing the product and dicyclohexylthiourea was triturated with chloroform (20 ml) overnight and filtered to give the product as white crystals. Yield 2.36 g (57 %). Spectroscopic data as above.