β-Glu-PAB (CH2NH2) -Exatecan

β-Glu-PAB (CH2NH2) -Exatecan (Compound 9a) is an inhibitor of topoisomerase I. It binds to the topoisomerase I-DNA complex, preventing the re-ligation of DNA strands, leading to DNA breaks and apoptosis. In the tumor microenvironment, where β-glucuronidase is highly expressed, β-Glu-PAB (CH2NH2) -Exatecan is specifically cleaved to release Exatecan, which then exerts its cytotoxic effects. Additionally, β-Glu-PAB (CH2NH2) -Exatecan serves as an intermediate for the synthesis of Mal ((3S,3aR,6S,6aR) -Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12) -β-Glu-PAB-Exatecan. This compound holds potential for cancer research.

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