scholarly journals Correction: Synthesis and biological evaluation of hybrids from farnesylthiosalicylic acid and hydroxylcinnamic acid with dual inhibitory activities of Ras-related signaling and phosphorylated NF-κB

2021 ◽  
Author(s):  
Yong Ling ◽  
Zhiqiang Wang ◽  
Xuemin Wang ◽  
Ying Zhao ◽  
Wei Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

Correction for ‘Synthesis and biological evaluation of hybrids from farnesylthiosalicylic acid and hydroxylcinnamic acid with dual inhibitory activities of Ras-related signaling and phosphorylated NF-κB’ by Yong Ling et al., Org. Biomol. Chem., 2014, 12, 4517–4530, DOI: 10.1039/C4OB00023D.

scholarly journals Synthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position

MedChemComm ◽  
2018 ◽  
Vol 9 (3) ◽  
pp. 545-553 ◽  
Author(s):  
David Cousin ◽  
Marc G. Hummersone ◽  
Tracey D. Bradshaw ◽  
Jihong Zhang ◽  
Christopher J. Moody ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Growth Inhibitory ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

The synthesis and biological evaluation of imidazotetrazines substituted at N-3 is described.

Synthesis and biological evaluation of oleanolic acid derivative–chalcone conjugates as α-glucosidase inhibitors

RSC Advances ◽  
2014 ◽  
Vol 4 (21) ◽  
pp. 10862-10874 ◽  
Author(s):  
Chu Tang ◽  
Linhui Zhu ◽  
Yu Chen ◽  
Rui Qin ◽  
ZhiNan Mei ◽  
...  
Keyword(s):  
Acid Derivative ◽  
Oleanolic Acid ◽  
Biological Evaluation ◽  
Glucosidase Inhibitors ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation ◽  
Oleanolic Acid Derivative

Series of oleanolic acid derivative–chalcone conjugates were designed, synthesized and their α-glucosidase inhibitory activities were investigatedin vitro.

Synthesis and steroid sulfatase inhibitory activities of N-phosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates

MedChemComm ◽  
2016 ◽  
Vol 7 (6) ◽  
pp. 1146-1150 ◽  
Author(s):  
Mateusz Daśko ◽  
Maciej Masłyk ◽  
Konrad Kubiński ◽  
Justyna Aszyk ◽  
Janusz Rachon ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Steroid Sulfatase ◽  
Coumarin 7 ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

In the present work, we report convenient methods for the synthesis and biological evaluation of N-phosphorylated derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as potential steroid sulfatase (STS) inhibitors.

Solution-phase synthesis and biological evaluation of triostin A and its analogues

2016 ◽  
Vol 14 (6) ◽  
pp. 2090-2111 ◽  
Author(s):  
Kozo Hattori ◽  
Kota Koike ◽  
Kensuke Okuda ◽  
Tasuku Hirayama ◽  
Masahiro Ebihara ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Biological Evaluation ◽  
Solution Phase ◽  
Phase Synthesis ◽  
Total Syntheses ◽  
Solution Phase Synthesis ◽  
Triostin A ◽  
Inhibitory Activities ◽  
High Yields ◽  
Synthesis And Biological Evaluation

We have accomplished preparative solution-phase total syntheses of triostin A (17.5% in 13 steps) and its analogues with high yields to demonstrate their significant inhibitory activities on HIF-1 activation and cell proliferation.

scholarly journals Synthesis and biological evaluation of dehydroabietic acid-pyrimidine hybrids as antitumor agents

RSC Advances ◽  
2020 ◽  
Vol 10 (31) ◽  
pp. 18008-18015
Author(s):  
Lin Huang ◽  
Rong Huang ◽  
Fuhua Pang ◽  
Anke Li ◽  
Guobao Huang ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Dehydroabietic Acid ◽  
Biological Evaluation ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

A series of novel dehydroabietic acid derivatives containing pyrimidine moieties were designed and synthesized. Some of them displayed more potent inhibitory activities compared with 5-FU.

scholarly journals Synthesis and biological evaluation of indazole derivatives as anti-cancer agents

RSC Advances ◽  
2021 ◽  
Vol 11 (26) ◽  
pp. 15675-15687
Author(s):  
Wei Wei ◽  
Zhihao Liu ◽  
Xiuli Wu ◽  
Cailing Gan ◽  
Xingping Su ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Breast Cancer Cell Line ◽  
Cell Apoptosis ◽  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Migration And Invasion ◽  
Anti Cancer ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

One of the synthesized indazole derivatives, 2f, displayed inhibitory activities against proliferation, migration and invasion of breast cancer cell line 4T1, with the potential of inducing cell apoptosis, and suppressing tumor growth in vivo.

Synthesis and biological evaluation of chalcone-triazole hybrid derivatives as 15-LOX inhibitors

2018 ◽  
Vol 73 (2) ◽  
pp. 77-83 ◽  
Author(s):  
Ali Asadipour ◽  
Saeedeh Noushini ◽  
Setareh Moghimi ◽  
Mohammad Mahdavi ◽  
Hamid Nadri ◽  
...  
Keyword(s):  
Aldol Condensation ◽  
Click Reaction ◽  
Biological Evaluation ◽  
Reaction Sequence ◽  
Inhibitory Activities ◽  
Lox Inhibitors ◽  
Synthesis And Biological Evaluation

AbstractAn efficient aldol condensation/click reaction sequence is employed for the synthesis of chalcone-triazole-based derivatives in moderate to good yields. The ability of target compounds to inhibit 15-lipoxygenase enzyme was investigated and moderate to low inhibitory activities were observed for the synthesized compounds.

Design, Synthesis and Biological Evaluation of the Novel Antitumor Agent Aurone Derivatives

2013 ◽  
Vol 781-784 ◽  
pp. 1235-1239
Author(s):  
Qian Nan Guo ◽  
Lei Lv ◽  
Yao Zhou ◽  
Peng Yu ◽  
Yuou Teng
Keyword(s):  
Biological Activities ◽  
Antitumor Agent ◽  
Biological Evaluation ◽  
The Novel ◽  
Pharmacological Activities ◽  
Design Synthesis ◽  
H Nmr ◽  
Wide Range ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

Aurones belong to a class of heterocyclic flavonoids which contains a benzofuran element associated with a benzylidene linked in position 2. Aurones possess a wide range of pharmacological activities and biological activities, such as antitumor, antifungal, phytoalexin and so on. A novel series of 2-ayl-yl (5-methacrylate) aurone analogues were synthesized in six steps with the overall yield of 11%-13% and characterized by 1H NMR. Among the key intermediates and target compounds, 2-(2-furan-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7a) and 2-(2-thienyl-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7b) have never been reported before. Primary biological activities evaluation showed that 7a exhibited good inhibitory activities against K562 with an IC50 of 2.18 μM and against HepG2 with an IC50 of 3.95μM.

scholarly journals Synthesis and Biological Evaluation of Thalidomide Derivatives as Potential Anti-Psoriasis Agents

2018 ◽  
Vol 19 (10) ◽  
pp. 3061 ◽  
Author(s):  
Kai-Wei Tang ◽  
Zih-Chan Lin ◽  
Yeh-Long Chen ◽  
Cherng-Chyi Tzeng ◽  
Jia-You Fang ◽  
...  
Keyword(s):  
Structural Optimization ◽  
Inhibitory Activity ◽  
Methoxy Group ◽  
Biological Evaluation ◽  
Hacat Cells ◽  
Cell Cytotoxicity ◽  
Tnf Α ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

Several thalidomide derivatives were synthesized and evaluated for their anti-inflammatory activity. Introduction of the benzyl group to the parent thalidomide is unfavorable in which 2-(1-benzyl-2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione (4a) was inactivated. However, the inhibitory activities on TNF-α and IL-6 expression in HaCaT cells were improved by the substitution of a chloro- or methoxy- group at the phenyl position of 4a. The IL-6 inhibitory activity decreased in an order of 5c (69.44%) > 4c (48.73%) > 6c (3.19%) indicating the 3-substituted derivative is more active than the 4-substituted counterpart, which in turn is more active than the 2-substituted counterpart. Among them, 2-[1-(3-chlorobenzyl)-2,6-dioxopiperidin-3-yl]isoindoline-1,3-dione (5c) was found to inhibit TNF-α and IL-6 expression in HaCaT cells with a higher potency than thalidomide and no significant cell cytotoxicity was detected at 10 μM. In psoriasis, Compound 5c reduced IL-6, IL-8, IL-1β and IL-24 in imiquimod-stimulated models. Our results indicated that compound 5c is a potential lead of novel anti-psoriasis agents. Structural optimization of compound 5c and its in vivo assay are ongoing.

Highly selective one pot synthesis and biological evaluation of novel 3-(allyloxy)-propylidene acetals of some natural terpenoids

RSC Advances ◽  
2015 ◽  
Vol 5 (113) ◽  
pp. 93122-93130 ◽  
Author(s):  
Ponnam Devendar ◽  
Arigari Niranjana Kumar ◽  
M. S. Bethu ◽  
Amtul Zehra ◽  
R. Pamanji ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
One Pot ◽  
One Pot Synthesis ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

Synthesis, in vitro antiproliferative and α-glucosidase inhibitory activities of novel 3-(allyloxy)-propylidene acetals of some natural terpenoids.

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