First Total Synthesis of ω-Phenyl Δ6 Fatty Acids and their Leishmanicidal and Anticancer Properties

Carballeira, Néstor M.; Morales‐Guzmán, Christian; Benedicto, Ester Alvarez; Torres‐Martínez, Zally; Delgado, Yamixa; Griebenow, Kai; Tinoco, Arthur D.; Reguera, Rosa M.; Pérez-Pertejo, Yolanda; Carbajo-Andres, Ruben; Balaña‐Fouce, Rafael

doi:10.2174/1568026618666180516125056

Cited by 5 publications

(6 citation statements)

References 38 publications

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“…Compounds 1 and 2 showed promising activity on L. donovani TOPIB (EC50 14 μM and 36 μM, respectively). Moreover, compounds 1 and 2 showed cytotoxicity toward L. infantum amastigotes (IC50 of 3-6 μM) and L. infantum promastigotes (IC50 of 60-70 μM) [128].…”

Section: Topoisomerase I and Ii (Topi Ec 5621; Topii Ec 5622)mentioning

confidence: 99%

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Toward New Antileishmanial Compounds: Molecular Targets for Leishmaniasis Treatment

Istanbullu¹,

Bayraktar²

2022

Leishmaniasis - General Aspects of a Stigmatized Disease

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The leishmaniases are a group of diseases caused by protozoan parasites—Leishmania sp. Leishmaniasis is classified among the 20 neglected diseases by WHO. Although the disease has been known for more than 120 years, the number of drugs used for the treatment is still limited to 5–6. The first-line drugs against leishmaniasis are pentavalent antimonials, which were introduced to the treatment 70 years ago—despite all their side effects. Molecular targets are becoming increasingly important for efficacy and selectivity in postgenomic drug research studies. In this chapter, we have discussed potential therapeutic targets of antileishmanial drug discovery such as pteridine reductase (PTR1), trypanothione reductase (TR), N-myristoyltransferase (NMT), trypanothione synthetase (TryS), IU-nucleoside hydrolase, and topoisomerases, enzymes and their inhibitors reported in the literature.

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Section: Topoisomerase I and Ii (Topi Ec 5621; Topii Ec 5622)mentioning

confidence: 99%

“…16-phenyl-6-hexadecynoic acid and 16-phenylhexadecanoic acid derivatives were synthesized by Carballeira et al [128]. Compounds 1 and 2 showed promising activity on L. donovani TOPIB (EC50 14 μM and 36 μM, respectively).…”

Section: Topoisomerase I and Ii (Topi Ec 5621; Topii Ec 5622)mentioning

confidence: 99%

Toward New Antileishmanial Compounds: Molecular Targets for Leishmaniasis Treatment

Istanbullu¹,

Bayraktar²

2022

Leishmaniasis - General Aspects of a Stigmatized Disease

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“…Fluorescence (R.F.U.) and cytotoxicity (%) the human cervical cancer cells after 24 h exposure of the synthesized compounds (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11) at 100 uM concentration.…”

Section: Declarationsmentioning

confidence: 99%

“…Fuertes et al reported that anticancer agents may constitute in the near future a good source of lead compounds against leishmaniasis and other parasitic diseases. On the other hand, it is also likely that some antiparasitic drugs may be used for the treatment of certain types of tumors (Carballeira et al, 2018;Perez, Fuertes, Nguewa, Castilla, & Alonso, 2008;Santiago et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Leishmanicidal and anticancer activity of 4-(2-keto-1-benzimidazolinyl) piperidine and 5-chloro-1-(4-piperidyl)-2-benzimidazolinone and their derivatives

Mallick

Saify

Haider

et al. 2022

Preprint

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In the current study a series of 4-(2-keto-1-benzimidazolinyl) piperidine have been newly synthesized and activities of 5-chloro-1-(4-piperidyl)-2-benzimidazolinone derivatives that is already reported have been tested and compared. Furthermore synthesized derivatives have been characterized by physical and spectral methods (HR-EIMS, HR-FABMS, 1H-NMR, 13C-NMR, UV, and FT-IR). All the derivatives were tested for leishmanicidal and anticancer activities. Results demonstrated that among all the derivatives compounds 4, 9, and 10 exhibited significant cytotoxic effects on HeLa cells and therefore tested at 10, 50 and 100 µM concentrations. Among all the eleven derivatives eight derivatives were found having leishmanicidal activity. Compounds 3, 4 and 10 exhibited significant activity with IC50 values in range of 7.06 ± 0.17 µg/mL − 84.6 ± 0.6 µg/mL. Furthermore, an attempt was made to develop a preliminary structure-activity relationship. Compound 4 found to be most active with IC50 = 7.06 ± 0.17 µg/mL against leishmaniasis. Compounds 4 and 10 possess both leishmanicidal and anticancer activities. From this study we identified a new class of compounds having potent leishmanicidal activity and anticancer activity.

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“…Anti-cancer and anti-leishmaniasis effects of herbal compounds such as pentacyclic triterpenoid are well known (Moulisha et al, 2010). Fatty acids from natural sources are inhibitors of therapeutic targets in cancer cells and Leishmania parasites (Carballeira et al, 2011(Carballeira et al, , 2018Carballeira, 2013).…”

Section: Drugs For the Treatment Of Leishmaniasis And Cancer With Commentioning

confidence: 99%

Potential therapeutic targets shared between leishmaniasis and cancer

et al. 2021

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First Total Synthesis of ω-Phenyl Δ6 Fatty Acids and their Leishmanicidal and Anticancer Properties

Cited by 5 publications

References 38 publications

Toward New Antileishmanial Compounds: Molecular Targets for Leishmaniasis Treatment

Toward New Antileishmanial Compounds: Molecular Targets for Leishmaniasis Treatment

Synthesis, Leishmanicidal and anticancer activity of 4-(2-keto-1-benzimidazolinyl) piperidine and 5-chloro-1-(4-piperidyl)-2-benzimidazolinone and their derivatives

Potential therapeutic targets shared between leishmaniasis and cancer

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