Efficient synthesis and biological evaluation of 1,3-benzenedicarbonyl dithioureas

The synthesis and biological activity of 1,3-benzenedicarbonyl dithioureas are described. Bioassay results indicated that these compounds exhibited cytotoxicity against various cancer cells. For example, compounds 4a showed the best inhibition activities against KB and CNE2 with IC 50 10.72 and 9.91...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-02, Vol.21 (4), p.1102-1104
Hauptverfasser:	Peng, Hao, Liang, Yongju, Chen, Le, Fu, Liwu, Wang, Haiqin, He, Hongwu
Format:	Artikel
Sprache:	eng
Schlagworte:	1,3-Benzenedicarbonyl dithioureas Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - toxicity Antitumor activity bioassays Biological and medical sciences Cell Line, Tumor chemistry cytotoxicity General aspects Humans inhibitory concentration 50 Medical sciences Pharmacology. Drug treatments Phthalic Acids - chemical synthesis Phthalic Acids - chemistry Phthalic Acids - toxicity Structure-Activity Relationship Synthesis Thiourea - analogs & derivatives Thiourea - chemical synthesis Thiourea - chemistry Thiourea - toxicity
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Zusammenfassung:	The synthesis and biological activity of 1,3-benzenedicarbonyl dithioureas are described. Bioassay results indicated that these compounds exhibited cytotoxicity against various cancer cells. For example, compounds 4a showed the best inhibition activities against KB and CNE2 with IC 50 10.72 and 9.91 μM, respectively.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.12.130