Solid-phase synthesis and antitumor evaluation of 2,4-diamino-6-aryl-1,3,5-triazines.
2,4-Diamino-6-aryl-1,3,5-triazines were synthesized by using a solid-supported approach in which monoarylsubstituted triazines were captured directly from the crude reaction mixture by resin-bound amines. The effects of the synthesized compounds on inhibition activities against tumor cell lines (PC-3, K562, A549, and HO8910) were examined. Most of the obtained compounds demonstrated remarkable antiproliferative activities against K562, PC-3, and HO8910 cell lines. Particularly, compounds 8c exhibited prominent inhibition activity with IC(50) values of 1.01, 2.23, and 1.06 microM, respectively. The structure-activity relationships of 2,4-diamino-6-aryl-1,3,5-triazines are also discussed.
Hu
Zhang
Z
College of Pharmaceutical Science, Zhejiang University, Hangzhou 310058, PR China.
Ma
Ting
T
Chen
Zhe
Z
Ye
Ziqi
Z
Zhang
Guolin
G
Lou
Yijia
Y
Yu
Yongping
Y
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D000970:Antineoplastic Agents; D014227:Triazines