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Design, synthesis and biological activity study of thiazolehydrazone-based small molecule inhibitors of IGF2BP2
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Shi-di ZHANG1, 2, Sai MA1, 2, Ying-zhe WANG1, 2, Yuan-qian CAI1, 2, Yan ZHANG1, 2, Qi-dong YOU1, 2, *, Xiao-ke GUO1, 2, *
Acta Pharmaceutica Sinica | 2024, 59(11) : 3006 - 3016
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Acta Pharmaceutica Sinica | 2024, 59(11): 3006-3016
Design, synthesis and biological activity study of thiazolehydrazone-based small molecule inhibitors of IGF2BP2
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Shi-di ZHANG1, 2, Sai MA1, 2, Ying-zhe WANG1, 2, Yuan-qian CAI1, 2, Yan ZHANG1, 2, Qi-dong YOU1, 2, *, Xiao-ke GUO1, 2, *
Affiliations
  • 1. Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China
  • 2. School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
Published: 2024-11-12 doi: 10.16438/j.0513-4870.2024-0564
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Insulin-like growth factor 2 mRNA binding protein 2 (IGF2BP2) is a recognition protein for N6-methyladenosine (m6A), mediating the stability of downstream mRNA, and is a promising anti-tumor target. Based on the lead compound 1g from previous screening, this study designed and synthesized 52 IGF2BP2 small molecule inhibitors using thiazole hydrazone as the parent nucleus. Among them, 9g, 10g, 37g, 47g and 52g showed good inhibitory activities. This work represents an initial exploration in the development of small molecule inhibitors targeting IGF2BP2, using thiazolehydrazone as the core structure. It lays a foundation for subsequent related research.

thiazole hydrazone derivative  /  insulin-like growth factor 2 mRNA binding protein 2  /  N6-methyladenosine  /  small-molecule inhibitor  /  design and synthesis
Shi-di ZHANG, Sai MA, Ying-zhe WANG, Yuan-qian CAI, Yan ZHANG, Qi-dong YOU, Xiao-ke GUO. Design, synthesis and biological activity study of thiazolehydrazone-based small molecule inhibitors of IGF2BP2[J]. Acta Pharmaceutica Sinica, 2024 , 59 (11) : 3006 -3016 . DOI: 10.16438/j.0513-4870.2024-0564
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Article Info
doi: 10.16438/j.0513-4870.2024-0564
  • Receive Date：2024-06-17
  • Online Date：2025-11-24
  • Published：2024-11-12
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History
  • Received：2024-06-17
  • Revised：2024-08-18
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Affiliations
    1. Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China
    2. School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
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Number of
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鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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