Synthesis of imidazothiadiazole–benzimidazole conjugates as mitochondrial apoptosis inducers

MedChemComm ◽  
2014 ◽  
Vol 5 (11) ◽  
pp. 1644-1650 ◽  
Author(s):  
Ahmed Kamal ◽  
Swapna Ponnampalli ◽  
M. V. P. S. Vishnuvardhan ◽  
M. P. Narasimha Rao ◽  
Kishore Mullagiri ◽  
...  

A series of imidazothiadiazole–benzimidazole conjugates (3a–z) were synthesized and evaluated for their cytotoxic activity against a set of four selected human cancer cell lines. Compounds3band3yexhibited significant antiproliferative activity against the ME-180 (cervical) cell line.

2016 ◽  
Vol 14 (26) ◽  
pp. 6304-6315 ◽  
Author(s):  
Trieu N. Trinh ◽  
Eileen A. McLaughlin ◽  
Mohammed K. Abdel-Hamid ◽  
Christopher P. Gordon ◽  
Ilana R. Bernstein ◽  
...  

A series of quinolone-2-(1H)-ones derived from a Ugi-Knoevenagel three- and four-component reaction were prepared exhibiting low micromolar cytotoxicity against a panel of eight human cancer cell lines known to possess the Hedgehog Signalling Pathway (HSP) components, as well as the seminoma TCAM-2 cell line.


2021 ◽  
Author(s):  
Elizaveta A. Kvyatkovskaya ◽  
Kseniya K. Borisova ◽  
Polina P. Epifanova ◽  
Aleksey A. Senin ◽  
Victor N. Khrustalev ◽  
...  

A 3,5a-epoxyfuro[2,3,4-de]isoquinoline scaffold, the product of ROCM of 1,4:5,8-diepoxynaphthalenes, is a promising antiproliferative agent toward breast and prostate human cancer cell lines.


2013 ◽  
Vol 6 (2) ◽  
pp. 246-252 ◽  
Author(s):  
Justin T. Fischedick ◽  
Milica Pesic ◽  
Ana Podolski-Renic ◽  
Jasna Bankovic ◽  
Ric C.H. de Vos ◽  
...  

2020 ◽  
Vol 11 (5) ◽  
pp. 686-690 ◽  
Author(s):  
Sylvestre P. J. T. Bachollet ◽  
Vito Vece ◽  
Alison N. McCracken ◽  
Brendan T. Finicle ◽  
Elizabeth Selwan ◽  
...  

Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3625 ◽  
Author(s):  
Antipova ◽  
Samoylenkova ◽  
Savchenko ◽  
Zavyalova ◽  
Revishchin ◽  
...  

Oligonucleotides with an antiproliferative activity for human cancer cells have attracted attention over the past decades; many of them have a G-quadruplex structure (GQ), and a cryptic target. In particular, DNA oligonucleotide HD1, a minimal GQ, could inhibit proliferation of some cancer cell lines. The HD1 is a 15-nucleotide DNA oligonucleotide that folds into a minimal chair-like monomolecular antiparallel GQ structure. In this study, for eight human cancer cell lines, we have analyzed the antiproliferative activities of minimal bimodular DNA oligonucleotide, biHD1, which has two HD1 modules covalently linked via single T-nucleotide residue. Oligonucleotide biHD1 exhibits a dose-dependent antiproliferative activity for lung cancer cell line RL-67 and cell line of central nervous system cancer U87 by MTT-test and Ki-67 immunoassay. The study of derivatives of biHD1 for the RL-67 and U87 cell lines revealed a structure-activity correlation of GQ folding and antiproliferative activity. Therefore, a covalent joining of two putative GQ modules within biHD1 molecule provides the antiproliferative activity of initial HD1, opening a possibility to design further GQ multimodular nanoconstructs with antiproliferative activity—either as themselves or as carriers.


2008 ◽  
Vol 3 (10) ◽  
pp. 1934578X0800301 ◽  
Author(s):  
Giuseppina Cioffi ◽  
Antonio Vassallo ◽  
Laura Lepore ◽  
Fabio Venturella ◽  
Fabrizio Dal Piaz ◽  
...  

Three new oleanane saponins (1–3), together with four known ones (4–7), were isolated from the aerial parts of Polyscias guilfoylei. Their structures were elucidated by 1D and 2D NMR experiments, including 1D TOCSY, DQF-COSY, ROESY, HSQC, and HMBC spectroscopy, as well as ESIMS analysis. The antiproliferative activity of all compounds was evaluated using three murine and human cancer cell lines; J774.A1, HEK-293, and WEHI-164. All the compounds were inactive except for 3β- O-[β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl]-echinocystic acid 28-[ O-β-D-glucopyranosyl-(1→6) O-β-D-glucopyranosyl] ester (3), which was active against all the cell lines.


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