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  3. Design, synthesis and biological evaluation of novel quinazoline derivatives as immune checkpoint inhibitors

Design, synthesis and biological evaluation of novel quinazoline derivatives as immune checkpoint inhibitors

  • Bioorg Med Chem Lett. 2024 Aug 1:108:129796. doi: 10.1016/j.bmcl.2024.129796.
Tam Thuy Lu Vo 1,  Van-Hai Hoang 2,  Phan Thi Phuong Dung 3,  Nguyen Anh Chi 3,  Vu Minh Huy 3,  Son Tung Ngo 4,  Yen Thi Kim Nguyen 5,  Tran Thi Thu Hien 6,  Tham H Hoang 7,  Yen Thi Do 8,  Ji Hae Seo 9,  Phuong-Thao Tran 10
Affiliations

Affiliations

  • 1 Department of Biochemistry, Keimyung University School of Medicine, Daegu 42601, South Korea; Faculty of Pharmacy and Nursing, Tay Do University, 68 Lo Hau Thanh My, Can Tho 900000, Viet Nam.
  • 2 Faculty of Pharmacy, PHENIKAA University, Hanoi 12116, Viet Nam; PHENIKAA Institute for Advanced Study (PIAS), PHENIKAA University, Yen Nghia, Hadong, Hanoi 12116, Viet Nam.
  • 3 Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi 100000, Viet Nam.
  • 4 Laboratory of Biophysics, Institute for Advanced Study in Technology, Ton Duc Thang University, Ho Chi Minh City 72915, Viet Nam; Faculty of Pharmacy, Ton Duc Thang University, Ho Chi Minh City 72915, Viet Nam.
  • 5 Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 08826, South Korea.
  • 6 Vietnam University of Traditional Medicine, 2 Tran Phu, Ha Dong, Hanoi 100000, Viet Nam.
  • 7 Center for Biomedical Informatics, Vingroup Big Data Institute, 458 Minh Khai Street, Hai Ba Trung, Hanoi 100000, Viet Nam.
  • 8 Department of Biochemistry, Keimyung University School of Medicine, Daegu 42601, South Korea.
  • 9 Department of Biochemistry, Keimyung University School of Medicine, Daegu 42601, South Korea. Electronic address: seoJh@kmu.ac.kr.
  • 10 Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi 100000, Viet Nam. Electronic address: thaotp@hup.edu.vn.
PMID: 38754563 DOI: 10.1016/j.bmcl.2024.129796
Abstract

In this work, we report 14 novel quinazoline derivatives as Immune Checkpoint inhibitors, IDO1 and PD-L1. The antitumor screening of synthesized compounds on ovarian Cancer cells indicated that compound V-d and V-l showed the most activity with IC50 values of about 5 μM. Intriguingly, compound V-d emerges as a stand out, triggering cell death through caspase-dependent and caspase-independent manners. More importantly, V-d presents its ability to hinder tumor sphere formation and re-sensitized cisplatin-resistant A2780 cells to cisplatin treatment. These findings suggest that compound V-d emerges as a promising lead candidate for the future development of immuno Anticancer agents.

Keywords

Immune check point; Indoleamine 2,3-dioxygenase 1; Ovarian cancer; Quinazoline.

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