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Part-IIIAdvances Dihydropyridines and …Pgp inhibition and QSPKR models. Cross-validation using the “leave-one-out” methodwas performed to evaluate the predictive performance of models. For Pgp reversal, themodel obtained by PLS could account for most of the variation in Pgp inhibition (R 2 =0.76) with fair predictive performance (Q 2 = 0.62). Nine structurally related 1,4-DHPsdrugs were used for QSPKR analysis. The models could explain the majority of thevariation in clearance (R 2 = 0.90), and cross-validation confirmed the prediction ability(Q 2 = 0.69) 128 .ROOH 3 COONH 3 C N CH 3H100ROOH 3 COONH 3 C N CH 3101Figure-21. Structure of Type-I 100 and Type-II 101 DHPsOptically pure DHPs substituted at C-4 with 3-nitro phenyl as shown in structure 102 arecapable of potentiating the activity of anticancer agents in tumor cell (synergism). Thisovercoming of resistance is not only limited to resistance to cytostatics but also to othertherapeutics such as for the treatment of malaria. 129427

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