Exploring novel nitrofuranyl sulfonohydrazides as anti‐Leishmania and anti‐cancer agents: Synthesis, in vitro efficacy and hit identification

Leishmaniasis and cancer are two deadly diseases that plague the human population. There are a limited number of drugs available for the treatment of these diseases; however, their overuse has resulted in pathogenic resistance. Recent studies have indicated the repurposing of nitro‐containing compou...

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Bibliographic Details
Published in:Chemical biology & drug design 2022-08, Vol.100 (2), p.267-279
Main Authors: Kannigadu, Christina, Aucamp, Janine, N'Da, David D.
Format: Article
Language:English
Subjects:
leishmaniasis
leukemia
melanoma
nitrofuran
sulfonohydrazide
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Summary:Leishmaniasis and cancer are two deadly diseases that plague the human population. There are a limited number of drugs available for the treatment of these diseases; however, their overuse has resulted in pathogenic resistance. Recent studies have indicated the repurposing of nitro‐containing compounds to be a new avenue into finding new treatments. In this study, new nitrofuranyl sulfonohydrazide derivatives were synthesized and evaluated for their in vitro antileishmanial and anticancer activities. The analogue 2h, featuring biphenyl moiety exhibited selective (SI > 10) submicromolar activity (IC50 0.97 μM) against acute promyelocytic leukemia cells hence was identified anticancer hit. This study revealed no antileishmanial hit. However, several promising analogues were uncovered and are worthy of further structural modifications to improve their toxicity and bioactivity profiles. Series of nitrofuranyl sulfonohydrazides were synthesized and evaluated in vitro for antileishmanial and anti‐cancer activities. Analogue 2h (IC50 0.97 μM; SI 17) was identified as anticancer hit against acute promyelocytic leukemia. No antileishmanial hit was uncovered.
ISSN:1747-0277
1747-0285
DOI:10.1111/cbdd.14097