2. Academic Validation
  3. Structural Modification of Noscapine via Photoredox/Nickel Dual Catalysis for the Discovery of S-Phase Arresting Agents

Structural Modification of Noscapine via Photoredox/Nickel Dual Catalysis for the Discovery of S-Phase Arresting Agents

  • ACS Med Chem Lett. 2024 Jan 5;15(2):230-238. doi: 10.1021/acsmedchemlett.3c00462.
Defeng Li 1,  Chuanxu Liu 2,  Tingyu Guo 1,  Jiajie Zhu 1,  Jiaqi Guo 1,  Ting Luo 1,  Yuhuan Liu 1,  Wenhao Shen 3,  Biao Jiang 3,  Wei Wang 4,  Qianqian Yin 3,  Yongqiang Zhang 1
Affiliations

Affiliations

  • 1 Shanghai Frontiers Science Center of Optogenetic Techniques for Cell Metabolism, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology, Shanghai 200237, P. R. China.
  • 2 Department of Lymphoma, Fudan University Shanghai Cancer Center, Shanghai 200032, P. R. China.
  • 3 Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, Shanghai 201210, P. R. China.
  • 4 Department of Pharmacology and Toxicology and BIO5 Institute, University of Arizona, Tucson, Arizona 85721-0207, United States.
PMID: 38352836 DOI: 10.1021/acsmedchemlett.3c00462
Abstract

Herein, we disclose a powerful strategy for the functionalization of the antitumor natural alkaloid noscapine by utilizing photoredox/nickel dual-catalytic coupling technology. A small collection of 37 new noscapinoids with diverse (hetero)alkyl and (hetero)cycloalkyl groups and enhanced sp3 character was thus synthesized. Further in vitro antiproliferative activity screening and SAR study enabled the identification of 6o as a novel, potent, and less-toxic Anticancer agent. Furthermore, 6o exerts superior cellular activity via an unexpected S-phase arrest mechanism and could significantly induce cell Apoptosis in a dose-dependent manner, thereby further highlighting its potential in drug discovery as a promising lead compound.

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