Synthesis, biological evaluation and in silico studies with 4-benzylidene-2-phenyl-5(4H)-imidazolone-based benzenesulfonamides as novel selective carbonic anhydrase IX inhibitors endowed with anticancer activity

2019 ◽  
Vol 90 ◽  
pp. 103102 ◽  
Author(s):  
Wagdy M. Eldehna ◽  
Mohamed A. Abdelrahman ◽  
Alessio Nocentini ◽  
Silvia Bua ◽  
Sara T. Al-Rashood ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Anticancer Activity ◽  
In Silico ◽  
Biological Evaluation ◽  
Carbonic Anhydrase Ix ◽  
In Silico Studies

scholarly journals Synthesis, biological evaluation, and in silico studies of novel chalcone- and pyrazoline-based 1,3,5-triazines as potential anticancer agents

RSC Advances ◽  
2020 ◽  
Vol 10 (56) ◽  
pp. 34114-34129
Author(s):  
Leydi M. Moreno ◽  
Jairo Quiroga ◽  
Rodrigo Abonia ◽  
Antonino Lauria ◽  
Annamaria Martorana ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
In Silico ◽  
Biological Evaluation ◽  
In Silico Studies

A novel series of triazin-chalcones (7,8)a–g and triazin-N-(3,5-dichlorophenyl)pyrazolines (9,10)a–g were synthesized and evaluated for their anticancer activity against nine different cancer strains.

Synthesis, investigation of biological effects and in silico studies of new benzimidazole derivatives as aromatase inhibitors

2020 ◽  
Vol 75 (9-10) ◽  
pp. 353-362
Author(s):  
Begüm Nurpelin Sağlık ◽  
Ahmet Mücahit Şen ◽  
Asaf Evrim Evren ◽  
Ulviye Acar Çevik ◽  
Derya Osmaniye ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
In Silico ◽  
Biological Effects ◽  
Docking Studies ◽  
Benzimidazole Derivatives ◽  
Binding Modes ◽  
Reference Drug ◽  
In Silico Studies ◽  
New Compounds ◽  
Mcf 7

AbstractInhibition of aromatase enzymes is very important in the prevention of estrogen-related diseases and the regulation of estrogen levels. Aromatase enzyme is involved in the final stage of the biosynthesis of estrogen, in the conversion of androgens to estrogen. The development of new compounds for the inhibition of aromatase enzymes is an important area for medicinal chemists in this respect. In the present study, new benzimidazole derivatives have been designed and synthesized which have reported anticancer activity in the literature. Their anticancer activity was evaluated against human A549 and MCF-7 cell lines by MTT assay. In the series, concerning MCF-7 cell line, the most potent compounds were the 4-benzylpiperidine derivatives 2c, 2g, and 2k with IC50 values of 0.032 ± 0.001, 0.024 ± 0.001, and 0.035 ± 0.001 µM, respectively, compared to the reference drug cisplatin (IC50 = 0.021 ± 0.001 µM). Then, these compounds were subject to further in silico aromatase enzyme inhibition assays to determine the possible binding modes and interactions underlying their activity. Thanks to molecular docking studies, the effectiveness of these compounds against aromatase enzyme could be simulated. Consequently, it has been found that these compounds can be settled very properly to the active site of the aromatase enzyme.

Preliminary biological evaluation of 125I-labeled anti-carbonic anhydrase IX monoclonal antibody in the mice bearing HT-29 tumors

2011 ◽  
Vol 32 (12) ◽  
pp. 1190-1193 ◽  
Author(s):  
Jianbo Li ◽  
Lingli Shi ◽  
Cheng Wang ◽  
Xiaohui Zhang ◽  
Lina Jia ◽  
...  
Keyword(s):  
Monoclonal Antibody ◽  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Carbonic Anhydrase Ix ◽  
Ht 29

In silico studies, synthesis and anticancer activity of novel diphenyl ether-based pyridine derivatives

2018 ◽  
Vol 23 (3) ◽  
pp. 541-554
Author(s):  
Ruchi Verma ◽  
Indira Bairy ◽  
Mradul Tiwari ◽  
G. Varadaraj Bhat ◽  
G. Gautham Shenoy
Keyword(s):  
Anticancer Activity ◽  
In Silico ◽  
Diphenyl Ether ◽  
Pyridine Derivatives ◽  
In Silico Studies
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