2013•Medicinal ChemistryRequires access

Design, Synthesis, and In vitro Antitumor Evaluation of Novel Phenylaminopyrimidine Derivatives

Youguang Zheng, Minghao Zheng, Yi Liu, Yunsheng Xue, Ling Zhang, Lin An, Ling Liu, Min Ji

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Abstract

Two series of novel phenylaminopyrimidine derivatives were designed and synthesized. All target compounds were determined against the human acute monocytic leukemia cell line U937 and the human chronic myeloid leukemia cell line K562 in vitro. Some of the target compounds demonstrated significant inhibitory activity against both cell lines. Compared with the control drug VX-680, 8a, 8e, 8g, 8h, 8j, and 8k demonstrated more potent antitumor activity. The structures of all target compounds were identified by 1H-NMR, 13C-NMR, IR, MS, and EA. Keywords: Phenylaminopyrimidine derivatives, U937, K562, antitumor activity, Leukemia, clinical trials, Oxidation, benzenes, cancer cell, acetic acid

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What this paper is about

Two series of novel phenylaminopyrimidine derivatives were designed and synthesized. All target compounds were determined against the human acute monocytic leukemia cell line U937 and the human chronic myeloid leukemia cell line K562 in vitro. Some of the target compounds demonstrated significant inhibitory activity against both cell lines. Compared with the control drug VX-680, 8a, 8e, 8g, 8h, 8j, and 8k demonstrated more potent antitumor activity. The structures of all target compounds were identified by 1H-NMR, 13C-NMR, IR, MS, and EA. Keywords: Phenylaminopyrimidine derivatives, U937, K562, antitumor activity, Leukemia, clinical trials, Oxidation, benzenes, cancer cell, acetic acid

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Available abstract

Two series of novel phenylaminopyrimidine derivatives were designed and synthesized. All target compounds were determined against the human acute monocytic leukemia cell line U937 and the human chronic myeloid leukemia cell line K562 in vitro. Some of the target compounds demonstrated significant inhibitory activity against both cell lines. Compared with the control drug VX-680, 8a, 8e, 8g, 8h, 8j, and 8k demonstrated more potent antitumor activity. The structures of all target compounds were identified by 1H-NMR, 13C-NMR, IR, MS, and EA. Keywords: Phenylaminopyrimidine derivatives, U937, K562, antitumor activity, Leukemia, clinical trials, Oxidation, benzenes, cancer cell, acetic acid

Key concepts: Myeloid leukemia, K562 cells, In vitro, Cell culture, U937 cell, Leukemia, Chemistry, Acute monocytic leukemia

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Design, Synthesis, and In vitro Antitumor Evaluation of Novel Phenylaminopyrimidine Derivatives — Research Paper | ScholarLens