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.

scholarly journals Synthesis and Biological Evaluation of 1,3,4-Oxadiazolyl benzenesulphonyl benzimidazole derivatives

2018 ◽  
Vol 6 (02) ◽  
pp. 64-71
Author(s):  
Vivek Kumar Gupta ◽  
Baljeet Kaur ◽  
Amandeep Kaur ◽  
Amanpreet Kaur ◽  
Monika Gupta
Keyword(s):  
Inhibitory Effect ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Growth Inhibitory Effect ◽  
Standard Drug ◽  
Growth Inhibitory ◽  
Anti Cancer ◽  
Synthesis And Biological Evaluation ◽  
Membered Heterocycle ◽  
Cancer Activity

Oxadiazoles are a class of heterocyclic aromatic chemical compound of azole family. Oxadiazole is five membered heterocycle having two carbons, two nitrogen, one oxygen and two double bonds. Oxadiazole exists in four isomeric forms depending upon the position of nitrogen atom in the ring. Benzimidazole is a heterocyclic aromatic compound. This bicyclic compound consists of fusion of benzene and imidazole. Benzimidazole may also be considered as cyclic analogues of imidines due to tautomerism effect. In the present study involves synthesis of1,3,4-oxadiazolyl benzenesulphonylbenzimidazole derivatives. All the synthesized compounds were screened against HepG-2 cell line to determine the growth inhibitory effect of compounds.All the synthesized compounds possessed good to moderate anti-cancer activity as compare to standard drug Adriamycin. Two of the synthesized compounds i.e. 8a and 8f were found to possess maximum anti-cancer activity.The structures of the synthesized compounds were established by IR and 1HNMR.

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.

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.

SYNTHESIS AND BIOLOGICAL EVALUATION OF 1-SUBSTITUTED-2-THIENYL- 5-(4-CHLOROPHENYL) PYRAZOLINE DERIVATIVES AS ANTIPROLIFERATIVE AGENTS

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (06) ◽  
pp. 24-30
Author(s):  
Amandeep Kaur ◽  
◽  
Baljeet Kaur ◽  
Monika Gupta
Keyword(s):  
Growth Inhibition ◽  
Anticancer Activity ◽  
Heterocyclic Ring ◽  
Biological Evaluation ◽  
Inhibitory Effects ◽  
Standard Drug ◽  
Growth Inhibitory ◽  
Control Growth ◽  
In Series ◽  
Synthesis And Biological Evaluation

Cancer is not a single disease, but a large group of diseases characterized by uncontrolled, rapid and pathological proliferation of abnormally transformed cells. Pyrazoline is a five-membered heterocyclic ring having two adjacent nitrogen atoms within the ring. It has only one endocyclic double bond and is basic in nature. The present study involves synthesis of 1-substituted-2-thienyl-5-(4-chlorophenyl) pyrazoline derivatives. The synthesized compounds were subjected to anticancer screening against SK-OV-3 cells line to determine the growth inhibitory effects of the compounds. Amongst all the derivatives in series (6a-j), the pyrazoline derivatives exhibited potent anticancer activity. All synthesized compounds possessed good to moderate anticancer activity. Compounds 6b and 6c at concentration 80 μg/mL possessed % control growth inhibition comparable to standard drug andriamycin. The order for the % control growth inhibition of SK-OV-3 was found to be 6h> 6j> 6f> 6i> 6e> 6g> 6d> 6a. All the compounds inhibited 50 % of the cell growth at the conc.

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.

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