Diphenylcyclohexylamine derivatives as new potent multidrug resistance (MDR) modulators |
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Authors: | Dei Silvia Budriesi Roberta Sudwan Paiwan Ferraroni Marta Chiarini Alberto Garnier-Suillerot Arlette Manetti Dina Martelli Cecilia Scapecchi Serena Teodori Elisabetta |
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Institution: | Dipartimento di Scienze Farmaceutiche, Università di Firenze, via U. Schiff 6, 50019 Sesto Fiorentino (FI), Italy. silvia.dei@unifi.it |
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Abstract: | A series of compounds with a diphenylmethyl cyclohexyl skeleton, loosely related to verapamil, has been synthesized and tested as MDR modulators on anthracycline-resistant erythroleukemia K 562 cells. Their residual cardiovascular action (negative inotropic and chronotropic activity as well as vasorelaxant activity) was evaluated on guinea-pig isolated atria preparations and on guinea-pig aortic strip preparations. Most compounds of the series possess a good MDR-reverting activity together with a low cardiovascular action. Among them, compounds 3a1, 7a, and 8a are more potent than verapamil as MDR reverters and lack any cardiovascular action; they can represent useful leads for the development of new safe MDR reversing drugs. |
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