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Design, synthesis, and biological evaluation of new thiazolo[5,4-d]pyrimidine derivatives as potent antiproliferative agents.

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, compound 7i exhibited potent inhibition against human gastric cancer cells MGC-803 and HGC-27 with IC₅₀ values of 4.64 and 5.07 ?M, 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 compound 7i make the thiazolo[5,4-d]pyrimidine an attractive scaffold for designing new derivatives selectively targeting MGC-803 cells.

SUBMITTER: Li ZH

PROVIDER: S-EPMC6071795 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature

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Design, synthesis, and biological evaluation of new thiazolo[5,4-d]pyrimidine derivatives as potent antiproliferative agents.

Li Zhong-Hua ZH Liu Xue-Qi XQ Geng Peng-Fei PF Ma Jin-Lian JL Zhao Tao-Qian TQ Wei Hao-Ming HM Yu Bin B Yu Bin B Liu Hong-Min HM

MedChemComm 20170622 8

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, compound 7i 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 ar ...[more]

PMID: 30108876

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