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Schematic representation for the SAR of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as PLK1 inhibitors. R1: medium-sized substituent with hydrogen bond donor and acceptor; R2: open-chain alkyl group with less than three carbon atoms or unsubstituted hydrogen; R3: hydrophobic group with small size and strong electron-withdrawing atom, especially hydrogen bond acceptor; R4: bulky substituents simultaneously with hydrophobic and hydrophilic moiety.
