Ethynylogation approach in antitumor lipid pharmacochemistry: from dialkynyl-carbinols to trialkynyl-carbinols
Тип публікації :
Стаття
Дата випуску :
2017
Автор(и) :
Bourkhis, Maroua
Listunov, Dymytrii
Gaspard, Hafida
Joly, Etienne
Abderrahim, Raoudha
Maraval, Valérie
Génisson, Yves
Chauvin, Remi
Мова основного тексту :
Англійська
eKNUTSHIR URL :
Том :
5
Випуск :
1
ISSN :
2312-3222
Початкова сторінка :
24
Кінцева сторінка :
34
Цитування :
[APA 7] Bourkhis, M., Listunov, D., Gaspard, H., Joly, E., Abderrahim, R., Maraval, V., Génisson, Y., & Chauvin, R. (2017). Ethynylogation approach in antitumor lipid pharmacochemistry: from dialkynyl-carbinols to trialkynyl-carbinols. French-Ukrainian Journal of Chemistry, 5(1), 24–34. https://doi.org/10.17721/fujcV5I1P24-34
[ДСТУ] Ethynylogation approach in antitumor lipid pharmacochemistry: from dialkynyl-carbinols to trialkynyl-carbinols / M. Bourkhis et al. French-Ukrainian Journal of Chemistry. 2017. Vol. 5, no. 1. P. 24—34. DOI: 10.17721/fujcV5I1P24-34 (date of access: 25.07.2026).
A recently proposed "ethynylogation" pharmacochemical approach, first envisaged in the series of anticancer lipidic dialkynylcarbinols (DACs) H–C≡C–CH(OH)–C≡C–R at the levels of the H–C⋮ and ⋮C–R bonds for R = n-C12H25, is completed here at the level of the (HO)C–H bond. The so-devised mono-lipidic trialkynylcarbinol (TAC) target (HC≡C)2C(OH)–C≡CR and its bis-lipidic counterpart HC≡C–C(OH)(C≡CR)2 were synthesized in 4 steps and with 33 % and 23 % overall yield, respectively. Their antitumor cytotoxicity has been evaluated towards HCT116 cells: while the latter TAC is totally inactive, the former DAC-ethynylogous TAC still exhibits a significant toxicity with an IC50 of 10 µM.
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