Syntheses and antitumor activities of neorautenol and shinpterocarpin analogs

  • Bioorg Med Chem Lett. 2023 Jul 15;91:129353. doi: 10.1016/j.bmcl.2023.129353.
Guocheng Huang  1 Van-Hai Hoang  2 Hye-Young Min  3 Ho-Young Lee  3 Jihyae Ann  4 Jeewoo Lee  5
Affiliations
  • 1. College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea.
  • 2. Faculty of Pharmacy & PHENIKAA Institute for Advanced Study, PHENIKAA University, Hanoi 12116, Vietnam.
  • 3. College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea; Creative Research Initiative Center for Concurrent Control of Emphysema and Lung Cancer, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea.
  • 4. College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea. Electronic address: [email protected].
  • 5. College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea. Electronic address: [email protected].
Abstract

The natural products neorautenol and shinpterocarpin and their structural analogs were investigated as novel Anticancer agents. Twenty-four analogs, including analogs containing a polar chain and simplified analogs, were synthesized efficiently by a modified method from previous reports. The antitumor screening of synthesized compounds toward six Cancer cell lines indicated that compounds 37, 42 and 43 with a dialkylaminoethyl-type side chain exhibited more promising activity than neorautenol and shinpterocarpin against lung and colon Cancer lines with a range of 4-9 μM. They showed selective toxicity in normal cells.

Keywords
Antitumor agents; Natural products; Neorautenol; Shinpterocarpin.
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