科研之友
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摘要
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 HIP-1 alpha/p300 complex.
- 出版日期2015-2-1
