Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
340.16093409
InChI
InChI=1S/C20H24N2OS/c1-4-22(5-2)13-12-21-16-11-10-14(3)20-18(16)19(23)15-8-6-7-9-17(15)24-20/h6-11,21H,4-5,12-13H2,1-3H3
InChI Key
InChIKey=FBQPGGIHOFZRGH-UHFFFAOYSA-N
IUPAC Name
1-{[2-(diethylamino)ethyl]amino}-4-methyl-9H-thioxanthen-9-one
Traditional IUPAC Name
lucanthone
SMILES
CCN(CC)CCNC1=C2C(=O)C3=CC=CC=C3SC2=C(C)C=C1
pKa (strongest acidic)
18.84
pKa (Strongest Basic)
8.69
Refractivity
106.01 m3·mol-1
Dược Lực Học :
Although lucanthone has structural and biochemical similarities to Actinomycin D, it has no hematological or gastro-intestinal toxicity at clinically tolerated doses. In trials, Lucanthone was found to be safe, practical and effective and was proposed for use in clinical protocols for the treatment of cancer. The specificity of lucanthone in combination with radiation for the treatment of brain tumors arises from the fact that lucanthone acts preferentially on cycling cells (most of the normal brain cells are non-cycling) and the fact that lucanthone crosses the blood brain barrier efficiently.
Cơ Chế Tác Dụng :
One of the schistosomicides, it has been replaced largely by hycanthone and more recently praziquantel. (From Martindale The Extrapharmacopoeia, 30th ed., p46). It is currently being tested as a radiation sensitizer.
Recent data suggests that lucanthone inhibits post-radiation DNA repair in tumor cells. The ability of lucanthone to inhibit AP endonuclease and topoisomerase II probably account for the specific DNA repair inhibition in irradiated cells.
Dược Động Học :
▧ Absorption :
Orally available
Chỉ Định :
Intended for use as a radiation sensitizer in the treatment of brain cancer.