Synthesis and cytotoxicity of methyl-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dione derivatives.
2- and 3-Methyl-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dione and related derivatives were synthesized and evaluated in vitro by NCI against eight cancer types. Compounds 12-15 showed significant activity against melanoma, NCI-H23 non-small cell lung cancer, and MDA-MB-435 and MDA-N breast cancer cell lines; 2-hydroxymethyl-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dion e (13) showed the highest activity against melanoma (mean log GI50 = -7.74) and the highest overall potency (mean log GI50 = -6.99).
Chao
Y H
YH
Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill 27599-7360, USA.
Kuo
S C
SC
Ku
K
K
Chiu
I P
IP
Wu
C H
CH
Mauger
A
A
Wang
H K
HK
Lee
K H
KH
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
C120943:2-hydroxymethyl-4,8-dihydrobenzo(1,2-b-5,4-b')dithiophene-48-dione; D000970:Antineoplastic Agents; D013876:Thiophenes