Synthesis of new chiral 2,5-disubstituted 1,3,4-thiadiazoles possessing gamma-butenolide moiety and preliminary evaluation of in vitro anticancer activity.
A new series of chiral 1,3,4-thiadiazoles derivatives possessing gamma-substituted butenolide moiety were synthesized and evaluated for in vitro anticancer properties. All the compounds showed good anticancer activities against Hela cell lines. Of all the studied compounds, compound 9e exhibited the best inhibitory activity with an IC(50) of 0.9 microM. After being treated with 0.1 microg/mL compound 9e for 24h, the growth inhibition rate of Hela cell lines was 59.2%.
Key Laboratory of Energy Sources and Chemical Engineering, Development Center of Natural Products and Medication and School of Chemistry and Chemical Engineering, Ningxia University, Yinchuan, China.
Meng-Xue
MX
Wei
Lei
L
Feng
Xue-Qiang
XQ
Li
Xue-Zhang
XZ
Zhou
Zhi-Hui
ZH
Shao
D015107:4-Butyrolactone / Q000031:analogs & derivatives* / Q000737:chemistry; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D015195:Drug Design; D006367:HeLa Cells; D006801:Humans; D013237:Stereoisomerism; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology*
D000970:Antineoplastic Agents; D013830:Thiadiazoles; C004511:butenolide; D015107:4-Butyrolactone