Abstract:Multidrug resistance (MDR) is a common phenomenon in clinical oncology, whereby cancer cells become resistant to chemotherapeutic drugs. A common MDR mechanism is the overexpression of ATP-binding cassette efflux transporters in cancer cells, with P-glycoprotein (P-gp) being one of them. New 3,4-seco-lupane triterpenoids, and the products of their intramolecular cyclization with the removed 4,4-gem-dimethyl group, were synthesized by the selective transformations of the A-ring of dihydrobetulin. Among the semi… Show more
“…Although TQ has shown great potency, its clinical trials was suspended recently due to obvious side effects reported in the phase III clinical trial of lung cancer. 28 Therefore, lots of P-gp inhibitors 29–70 with new scaffolds are continuously being developed to enhance activity and selectivity. However, in order to truly obtain clinically applicable sensitizers for resistant tumors, the exploration in this field is still ongoing.…”
Based on synthetic methodology-based library, a new class of tricyclic spiroindole derivatives as potent P-glycoprotein inhibitors with excellent tumor multidrug resistance reversal activity was discovered.
“…Although TQ has shown great potency, its clinical trials was suspended recently due to obvious side effects reported in the phase III clinical trial of lung cancer. 28 Therefore, lots of P-gp inhibitors 29–70 with new scaffolds are continuously being developed to enhance activity and selectivity. However, in order to truly obtain clinically applicable sensitizers for resistant tumors, the exploration in this field is still ongoing.…”
Based on synthetic methodology-based library, a new class of tricyclic spiroindole derivatives as potent P-glycoprotein inhibitors with excellent tumor multidrug resistance reversal activity was discovered.
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