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Short Paper | Regular issue | Vol 91, No. 2, 2015, pp.351-362
Published online, 26th January, 2015
DOI: 10.3987/COM-14-13084
Design, Synthesis, and Biological Activity Evaluation of Thiazolidinones Containing Alkynyl and Alkenyl Furans for Disrupting Protein–Protein Interactions between HIF-1α and p300

Norihiko Takeda, Tomoyo Taguchi, Takeshi Nakajima,* and Mitsuyoshi Azuma

*Senju Laboratory of Ocular Sciences, Senju Pharmaceutical Co., Ltd., 1-5-5, Minatojima-Minamimachi, Chuo-ku, Kobe, Hyogo, 650-0047, Japan


Based on the structure of the potent hypoxia-inducible factor (HIF) inhibitor 1, a novel series of furanylidene-thiazolidinones 6 were designed and synthesized using Sonogashira or Suzuki–Miyaura cross-couplings, and subsequent Knoevenagel condensation. In particular, derivatives 6aA, 6cA, 6dA, 6hA, 6iA, and 6cC, bearing an alkynyl or alkenyl group on the furan ring, exhibited four- to five-fold higher activities than 1. These potent compounds will serve as leads for the development of novel small molecules for targeting the HIF-1α/p300 complex.