Design, synthesis, and biological evaluation of new thiazolo[5, 4-d]pyrimidine derivatives as potent antiproliferative agents. Issue 8 (7th July 2017)

• Record Type: Journal Article
• Authors: Li, Zhong-Hua; Liu, Xue-Qi; Geng, Peng-Fei; Ma, Jin-Lian; Zhao, Tao-Qian; Wei, Hao-Ming; Yu, Bin; Liu, Hong-Min
• Is Part Of: MedChemComm. Volume 8:Issue 8(2017)
• Page Start: 1655
• Page End: 1658
• Publication Date: 2017-07-07
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c7md00165g
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : The thiazolo[5, 4- d ]pyrimidine derivative7i exhibited potent inhibition against MGC-803 and HGC-27 with IC50 values of 4.64 and 5.07 μM, respectively and around 12-fold selectivity between MGC-803 and GES-1. Abstract : A series of thiazolo[5, 4- d ]pyrimidine derivatives were synthesized and evaluated for their antiproliferative activities against several human cancer cell lines. Structure–activity relationship studies were carried out, showing that most of the target compounds had good inhibition against the tested cell lines. Among them, compound7i exhibited potent inhibition against human gastric cancer cells MGC-803 and HGC-27 with IC50 values of 4.64 and 5.07 μM, respectively and around 12-fold selectivity between MGC-803 and GES-1, indicating a relatively low toxicity to normal cells. The potency and low toxicity of compound7i make the thiazolo[5, 4- d ]pyrimidine an attractive scaffold for designing new derivatives selectively targeting MGC-803 cells.