Design, synthesis and biological evaluation of novel 6-substituted pyrrolo [3,2-d] pyrimidine analogues as antifolate antitumor agents.

Tian, Chao; Wang, Meng; Han, Zifei; Fang, Fang; Zhang, Zhili; Wang, Xiaowei; Liu, Junyi

Tian, Chao; Wang, Meng; Han, Zifei; Fang, Fang; Zhang, Zhili; Wang, Xiaowei; Liu, Junyi.

Affiliation

Tian C; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Wang M; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Han Z; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Fang F; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Zhang Z; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Wang X; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Liu J; Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China; State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China. Electronic address: jyliu@bjmu.edu.cn.

Eur J Med Chem ; 138: 630-643, 2017 Sep 29.

Article in En | MEDLINE | ID: mdl-28711701

Subject(s)

Antineoplastic Agents/pharmacology; Drug Design; Enzyme Inhibitors/pharmacology; Folic Acid Antagonists/pharmacology; Folic Acid/metabolism; Pyrimidines/pharmacology; Pyrroles/pharmacology; Antineoplastic Agents/chemical synthesis; Antineoplastic Agents/chemistry; Cell Death/drug effects; Cell Line, Tumor; Cell Proliferation/drug effects; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/chemistry; Folic Acid Antagonists/chemical synthesis; Folic Acid Antagonists/chemistry; Humans; Molecular Structure; Pyrimidines/chemical synthesis; Pyrimidines/chemistry; Pyrroles/chemical synthesis; Pyrroles/chemistry; Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase/metabolism; Thymidylate Synthase/antagonists & inhibitors; Thymidylate Synthase/metabolism

Key words

6-substituted pyrrolo[3,2-d]pyrimidines; Anti-proliferation; Colony formation inhibition; Dihydrofolate reductase; G2/M-phase increased; Structureactivity relationship; Thymidylate synthase

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrimidines / Pyrroles / Drug Design / Enzyme Inhibitors / Folic Acid / Folic Acid Antagonists / Antineoplastic Agents Limits: Humans Language: En Journal: Eur J Med Chem Year: 2017 Document type: Article Affiliation country: China Country of publication: France

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