Applications of Precise Chemistry in Drug Discovery★

doi:10.6023/cjoc20205031

Chinese Journal of Organic Chemistry ›› 2025, Vol. 45 ›› Issue (9): 3075-3097.DOI: 10.6023/cjoc20205031 Previous Articles Next Articles

REVIEWS

“精准化学”在药物发现中的应用^★

刘荣^a, 左应林^a^,^b^,^c^,^*(), 张英俊^a^,^b^,^c^,^*(), 张霁^a^,^b^,^c^,^*()

^a 广东东阳光药业股份有限公司广东东莞 523871
^b 抗感染新药研发全国重点实验室广东东莞 523871
^c 广东省抗病毒药物研发企业重点实验室广东东莞 523871

收稿日期:2025-05-30 修回日期:2025-08-06 发布日期:2025-09-11
基金资助:
抗感染新药研发全国重点实验室(2015DQ780357); 广东省抗病毒药物研发企业重点实验室(2020B1212070003); 广东省抗病毒药物研发企业重点实验室(2023B1212070004)

Applications of Precise Chemistry in Drug Discovery^★

Rong Liu^a, Yinglin Zuo^a^,^b^,^c^,^*(), Yingjun Zhang^a^,^b^,^c^,^*(), Ji Zhang^a^,^b^,^c^,^*()

^a Sunshine Lake Pharma Co., Ltd., Dongguan, Guangdong 523871
^b State Key Laboratory of Anti-Infective Drug Development, Dongguan, Guangdong 523871
^c Enterprise Key Laboratory of Anti-viral Drug Development for Guangdong Province, Dongguan, Guangdong 523871

Received:2025-05-30 Revised:2025-08-06 Published:2025-09-11
Contact: *E-mail: zuoyinglin@hec.cn; zhangyingjun@hec.cn; zhangji@hec.cn
About author:
^★ Academic Papers of the 27^th Annual Meeting of the China Association for Science and Technology.
Supported by:
State Key Laboratory of Anti-infective Drug Development(2015DQ780357); Enterprise Key Laboratory of Anti-viral Drug Development for Guangdong Province(2020B1212070003); Enterprise Key Laboratory of Anti-viral Drug Development for Guangdong Province(2023B1212070004)

To enhance the efficiency of drug research and synthesis, the implementation of “Precision Chemistry” characterized by molecular-level precise design and control of drug molecules to achieve highly efficient, selective, and predictable chemical reactions has become imperative. While “Precision Chemistry” aligns with existing goals of “Green Chemistry” such as atom economy and waste minimization, its core emphasis lies in precision and efficiency. These two concepts intersect rather than being subordinate to each other. This review demonstrates the philosophy of “Precision Chemistry” through practical examples of drug discovery and synthesis of anti-cancer drugs, anti-infection drugs, targeted protein degradation drugs, cardiovascular/metabolic drugs, anti-inflammatory drugs, aiming to better understanding the “Precision Chemistry” concept to serve pharmaceutical research and process well.

Key words: Precise Chemistry, drug discovery, drug synthesis, targeted drugs, green chemistry

Cite this article

Rong Liu, Yinglin Zuo, Yingjun Zhang, Ji Zhang. Applications of Precise Chemistry in Drug Discovery^★[J]. Chinese Journal of Organic Chemistry, 2025, 45(9): 3075-3097.

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Fig. & Tab. 20

Figure 1. Precise chemistry in drug discovery

Figure 2. Anti-cancer drug discovery based on precise modification of camptothecin

Figure 3. Antidoby-drug conjugates discovery based on precise modification of camptothecin

Figure 4. Drug discovery based on precise modification of thalidomide, lenalidomide

Figure 5. DAC drug discovery based on precise modification of pomalidomide

Figure 6. MAC drug discovery based on precise modification of lenalidomide

Figure 7. Mechanism and binding interaction of ibrutinib

Figure 8. Covalent BTK inhibitor drug discovery based on precise modification of ibrutinib

Figure 9. BTK degrader drug discovery based on precise modification of ibrutinib

Figure 10. Drug discovery based on precise modification of pleuromutilin

Figure 11. Mechanism and binding interaction of pleuromutilin and precise modification of pleuromutilin at C12, C14, C17

Figure 12. Drug discovery based on precise modification of erythromycin

Figure 13. Binding interaction of daclatasvir

Figure 14. Drug discovery based on precise modification of daclatasvir

Figure 15. The first statin drug discovery based on precise modification of mevastatin

Figure 16. The 2nd and 3rd statin drug discovery based on precise modification of 1st statin

Figure 17. Drug discovery based on precise modification of pitavastatin

Figure 18. Drugs of COX-II inhibitors

Figure 19. Drug discovery based on precise modification of celecoxib and etoricoxib via C—H activation

Figure 20. Theranostics base on late-stage functionalization of drugs

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“精准化学”在药物发现中的应用^★

Applications of Precise Chemistry in Drug Discovery^★

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“精准化学”在药物发现中的应用★

Applications of Precise Chemistry in Drug Discovery★

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“精准化学”在药物发现中的应用^★

Applications of Precise Chemistry in Drug Discovery^★