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Anti-Cancer Agents in Medicinal Chemistry

Author(s): Xiaolin Lu, Gaochao Dong, Ying Zheng, Chao Zhang, Yang Qiu, Tao Lua and Xiang Zhou*

DOI: 10.2174/1871520615666160504094945

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Synthesis and Anticancer Study of Novel 4H-Chromen Derivatives

Page: [1070 - 1083] Pages: 14

  • * (Excluding Mailing and Handling)

Abstract

Objective/Method: A series of 4H-chromen-4-one derivatives (A1-A16) have been designed and synthesized, and they were screened for BRAF kinase inhibitory activity. Furthermore, their biological activities were evaluated in vitro.

Result: Compounds A03 and A10 displayed the most potent antiproliferative activity against human osteosarcoma cell line (U2OS) and A16 displayed the most potent antiproliferative activity against human melanoma cancer cell line (A375) in vitro, which was valuable to study further.

Keywords: 4H-Chromen-4-one, anticancer activity, BRAF (V600E) kinase, design, in vitro, synthesis.

Graphical Abstract