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Synthesis and Biological Evaluation As Microtubule-Active Agents of Several Tetrahydrofuran and Spiroacetal Derivatives
(Bentham Science, 2013)
The stereoselective preparation of several molecules containing structural fragments of the tetrahydrofuran and spiroacetal type is described. Their degree of cytotoxicity and their interactions with tubulin have been ...
Interactions of long-chain homologues of colchicine with tubulin
(Elsevier, 2017-01)
Several colchicine analogues in which the N-acetyl residue has been replaced by aliphatic, straight-chain acyl moieties, have been synthesized. These compounds show high cytotoxic activity at the nanomolar level against ...
Synthesis and Biological Evaluation of a-Tubulin-Binding Pironetin Analogues with Enhanced Lipophilicity
(Wiley-VCH Verlag, 2013)
The preparation of four new lipophilic analogues of the natural pyrone pironetin is described. The nine-carbon side chain of the latter has been replaced in one analogue by a 4-phenylbutyl chain and in the other three ...
Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity
(Elsevier, 2018-04-25)
Our efforts to get therapeutically useful colchicine derivatives for the treatment of cancer have led us to synthetize and biologically evaluate twenty-seven N,N′-disubstituted ureas containing a colchicine moiety and an ...
Synthesis, antiprotozoal activity and cytotoxicity in U-937 macrophages of triclosan–hydrazone hybrids
(Springer Verlag, 2017)
The synthesis and biological activities (cytotoxicity, leishmanicidal, and trypanocidal) of 11 triclosan–hydrazone hybrids are described herein. The structure of the products was elucidated by spectral data (NMR, IR) and ...
Triclosan-caffeic acid hybrids: Synthesis, leishmanicidal, trypanocidal and cytotoxic activities
(Elsevier, 2017-09-29)
The synthesis, cytotoxicity, anti-leishmanial and anti-trypanosomal activities of twelve triclosan-caffeic
acid hybrids are described herein. The structure of the synthesized products was elucidated by a com-
bination ...
Effects of Curcuminoid Pyrazoles on Cancer Cells and on the Expression of Telomerase Related Genes
(Wiley, 2016-07)
A group of 13 curcuminoid pyrazoles was investigated for their cytotoxicity on three tumoral cell lines (HT-29, MCF-7, and HeLa) and one non-tumoral human cell line (HEK-293). The values obtained were compared with those ...
Synthesis, leishmanicidal, trypanocidal and cytotoxic activity of quinoline-hydrazone hybrids
(Elsevier, 2015)
Cutaneous leishmaniasis and Chagas disease are vector-borne parasitic disease causing serious risks to million people living in poverty-stricken areas. Both diseases are a major health problem in Latin America, and currently ...
Design and synthesis of pironetin analogues with simplified structure and study of their interactions with microtubules
(Elsevier, 2011-05)
The preparation of a series of pironetin analogues with simplified structure is described. Their cytotoxic activity and their interactions with tubulin have been investigated. It has been found that, while less active than ...
Synthesis and biological properties of the cytotoxic 14-membered macrolides aspergillide A and B
(Wiley, 2010-11-09)
Total, stereoselective syntheses of the naturally occurring, cytotoxic macrolides aspergillide A and B are described. Olefin metatheses and asymmetric allylations were key steps in the synthetic sequences. Cytotoxicity ...