Identification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology

• Published in: ACS medicinal chemistry letters Vol. 15; no. 2; pp. 189 - 196
• Main Authors: He, Liqi, Zhang, Meng Yao, Cox, Matthew, Zhang, Qian, Donnell, Andrew F., Zhang, Yong, Tarby, Christine, Gill, Patrice, Subbaiah, Murugaiah A. M., Ramar, Thangeswaran, Reddy, Maheswara, Puttapaka, Vijaya, Li, Yi-Xin, Sivaprakasam, Prasanna, Critton, David, Mulligan, Dawn, Xie, Chunshan, Ramakrishnan, Radha, Nagar, Jignesh, Dudhgaonkar, Shailesh, Murtaza, Anwar, Oderinde, Martins S., Schieven, Gary L., Mathur, Arvind, Gavai, Ashvinikumar V., Vite, Gregory, Gangwar, Sanjeev, Poudel, Yam B.
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 08.02.2024; Amer Chemical Soc
• Subjects: Chemistry, Medicinal; Life Sciences & Biomedicine; Pharmacology & Pharmacy; Science & Technology; Tumor; TLR7 agonist; PD1; Immuno-oncology; Cancer

Small molecule toll-like receptor (TLR) 7 agonists have gathered considerable interest as promising therapeutic agents for applications in cancer immunotherapy. Herein, we describe the development and optimization of a series of novel TLR7 agonists through systematic structure–activity relationship...