Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors |
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| Authors: | Al-Mawsawi Laith Q Dayam Raveendra Taheri Laleh Witvrouw Myriam Debyser Zeger Neamati Nouri |
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| Affiliation: | Department of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA 90089, USA. |
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| Abstract: | The previously discovered salicylhydrazide class of compounds displayed potent HIV-1 integrase (IN) inhibitory activity. The development of this class of compounds as antiretroviral agents was halted due to cytotoxicity in the nanomolar to sub-micromolar range. We identified a novel class of non-cytotoxic hydrazide IN inhibitors utilizing the minimally required salicylhydrazide substructure as a template in a small-molecule database search. The novel hydrazides displayed low micromolar IN inhibitory activity and are several hundred-fold less cytotoxic than previously disclosed salicylhydrazide IN inhibitors. |
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