Late-stage halogenation of Scortechinone D via NaX oxidation and inhibitory activity against EGFR tyrosine kinase

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Ade Danova, Edwin Risky Sukandar, Rizky Annisa Ramadhini, Yusuf Eka Maulana, Elvira Hermawati, Fera Kurniadewi, Rita Hairani, Huong Thi Thu Le, Sutin Kaennakam, Warinthorn Chavasiri, Didin Mujahidin, Lia Dewi Juliawaty

2026 Results in Chemistry Vol. 28 Article Cited by 0 SDG 3SDG 17 Quartile

Abstract

Three new scortechinone D derivatives ( 2 – 4 ) were effectively obtained through in situ halogenation of scortechinone D ( 1 ) using Oxone and sodium halide in a mixture of acetonitrile and water (5:1 ratio). All compounds were characterized using 1D and 2D NMR spectroscopy and high-resolution mass spectrometry. Single crystal-XRD was successfully performed on the compound 4 possessing iodo group at C-17. Among the four compounds ( 1 – 4 ) tested, compound 2 showed good inhibitory activity against EGFR tyrosine kinase with an inhibition value of 63.5% at 10 μM and modest toxicity against WI-38 normal cell line with 58.8% growth suppression at the same concentration. Despite the considerable toxicity of the active compound, this discovery offers a novel insight into the reactivity and bioactivity of scortechinone D analogs. © 2026 The Author(s).

Affiliations

Organic Chemistry Division, Department of Chemistry, Faculty of Mathematics and Natural Sciences, Institut Teknologi Bandung, Jl. Ganesha No. 10, West Java, Bandung, 40132, Indonesia; Chemistry Study Program, Universitas Negeri Jakarta, Jakarta, 13220, Indonesia; Department of Chemistry, Faculty of Mathematics and Natural Sciences, Mulawarman University, East Kalimantan, Samarinda, 75123, Indonesia; Department of Agro-Industrial, Food, and Environmental Technology, Faculty of Applied Science, King Mongkut's University of Technology North Bangkok (KMUTNB), Bangkok, 10800, Thailand; Center of Excellence in Natural Products Chemistry, Department of Chemistry, Faculty of Science, Chulalongkorn University, Pathumwan, Bangkok, 10330, Thailand; Department of Chemistry, Ho Chi Minh City University of Education, 280 An Duong Vuong Street, Cho Quan ward, Ho Chi Minh City, 700000, Viet Nam

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