Javascript must be enabled to continue!
Unveiling a New Selenocyanate as a Multitarget Candidate with Anticancer, Antileishmanial and Antibacterial Potential
View through CrossRef
Currently, cancer, leishmaniasis and bacterial infections represent a serious public health burden worldwide. Six cinnamyl and benzodioxyl derivatives incorporating selenium (Se) as selenocyanate, diselenide, or selenide were designed and synthesized through a nucleophilic substitution and/or a reduction using hydrides. Ferrocene was also incorporated by a Friedel–Crafts acylation. All the compounds were screened in vitro for their antiproliferative, antileishmanial, and antibacterial properties. Their capacity to scavenge free radicals was also assessed as a first approach to test their antioxidant activity. Benzodioxyl derivatives 2a–b showed cytotoxicity against colon (HT-29) and lung (H1299) cancer cell lines, with IC50 values below 12 µM, and were also fairly selective when tested in nonmalignant cells. Selenocyanate compounds 1–2a displayed potent antileishmanial activity in L. major and L. infantum, with IC50 values below 5 µM. They also exhibited antibacterial activity in six bacterial strains, notably in S. epidermidis with MIC and MBC values of 12.5 µg/mL. Ferrocene-containing selenide 2c was also identified as a potent antileishmanial agent with radical scavenging activity. Remarkably, derivative 2a with a selenocyanate moiety was found to act as a multitarget compound with antiproliferative, leishmanicidal, and antibacterial activities. Thus, the current work showed that 2a could be an appealing scaffold to design potential therapeutic drugs for multiple pathologies.
Title: Unveiling a New Selenocyanate as a Multitarget Candidate with Anticancer, Antileishmanial and Antibacterial Potential
Description:
Currently, cancer, leishmaniasis and bacterial infections represent a serious public health burden worldwide.
Six cinnamyl and benzodioxyl derivatives incorporating selenium (Se) as selenocyanate, diselenide, or selenide were designed and synthesized through a nucleophilic substitution and/or a reduction using hydrides.
Ferrocene was also incorporated by a Friedel–Crafts acylation.
All the compounds were screened in vitro for their antiproliferative, antileishmanial, and antibacterial properties.
Their capacity to scavenge free radicals was also assessed as a first approach to test their antioxidant activity.
Benzodioxyl derivatives 2a–b showed cytotoxicity against colon (HT-29) and lung (H1299) cancer cell lines, with IC50 values below 12 µM, and were also fairly selective when tested in nonmalignant cells.
Selenocyanate compounds 1–2a displayed potent antileishmanial activity in L.
major and L.
infantum, with IC50 values below 5 µM.
They also exhibited antibacterial activity in six bacterial strains, notably in S.
epidermidis with MIC and MBC values of 12.
5 µg/mL.
Ferrocene-containing selenide 2c was also identified as a potent antileishmanial agent with radical scavenging activity.
Remarkably, derivative 2a with a selenocyanate moiety was found to act as a multitarget compound with antiproliferative, leishmanicidal, and antibacterial activities.
Thus, the current work showed that 2a could be an appealing scaffold to design potential therapeutic drugs for multiple pathologies.
Related Results
Phytochemical analysis and in vitro antileishmanial activity of Basella alba extract cultivated in Iraq
Phytochemical analysis and in vitro antileishmanial activity of Basella alba extract cultivated in Iraq
Basella alba, widely known as Malabar spinach, is a fast-growing perennial native to tropical regions Worldwide. B. alba has been widely utilized in traditional medicine because of...
Target site bioanalysis and pharmacokinetics of antileishmanial drugs
Target site bioanalysis and pharmacokinetics of antileishmanial drugs
This thesis focuses on bioanalytical method development and validation of
antileishmanial drugs amphotericin B, miltefosine, and paromomycin in human
plasma and human skin tissue f...
Molecular Docking and Antileishmanial Potential of Isolated Compounds from Asparagus gracilis
Molecular Docking and Antileishmanial Potential of Isolated Compounds from Asparagus gracilis
Background: Leishmaniasis remains a neglected tropical disease with high global disease burden and limited safe therapeutic options. Medicinal plants offer an important source of b...
Antileishmanial Compounds Isolated from Psidium Guajava L. Using a Metabolomic Approach
Antileishmanial Compounds Isolated from Psidium Guajava L. Using a Metabolomic Approach
With an estimated annual incidence of one million cases, leishmaniasis is one of the top five vector-borne diseases. Currently available medical treatments involve side effects, in...
Cedrus deodara
Cedrus deodara
Background & objectives:
The existing antileishmanial drugs for complete cure of visceral leishmaniasis (kala-azar) are limited. The available drugs are either toxi...
ANTILEISHMANIAL ACTIVITY EVALUATION OF BLACK CUMIN EXTRACTS AGAINST LEISHMANIA TROPICA
ANTILEISHMANIAL ACTIVITY EVALUATION OF BLACK CUMIN EXTRACTS AGAINST LEISHMANIA TROPICA
Objectives: In addition to the high cost of antileishmanial drugs, the resistance that develops against these drugs and their side effects has led to the investigation of leishmani...
The Modeling of Super Deep Learning Aiming at Knowledge Acquisition in Automatic Driving
The Modeling of Super Deep Learning Aiming at Knowledge Acquisition in Automatic Driving
In this paper, we proposed a new theory of solving the multitarget control problem by introducing a machine learning framework in automatic driving and implementing the acquisition...
Antileishmanial and Antibacterial Activities of Aminobenzothiazole Sulfonamides
Antileishmanial and Antibacterial Activities of Aminobenzothiazole Sulfonamides
Leishmaniasis and multidrug-resistant (MDR) bacterial infections remain major global health challenges due to drug toxicity and increasing antimicrobial resistance. In this study, ...

