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Synthesis, Docking Studies and Biological Activity of New Benzimidazole- Triazolothiadiazine Derivatives as Aromatase Inhibitor
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Synthesis, Docking Studies and Biological Activity of New Benzimidazole- Triazolothiadiazine Derivatives as Aromatase Inhibitor
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Journal Article
Synthesis, Docking Studies and Biological Activity of New Benzimidazole- Triazolothiadiazine Derivatives as Aromatase Inhibitor
2020
Overview
In the last step of estrogen biosynthesis, aromatase enzyme catalyzes the conversion of androgens to estrogens. Aromatase inhibition is an important way to control estrogen-related diseases and estrogen levels. In this study, sixteen of benzimidazole-triazolothiadiazine derivatives have been synthesized and studied as potent aromatase inhibitors. First, these compounds were tested for their anti-cancer properties against human breast cancer cell line (MCF-7). The most active compounds
,
,
, and
on MCF-7 cell line were subject to further in vitro aromatase enzyme inhibition assays to determine the possible mechanisms of action underlying their activity. Compound
showed slight less potent aromatase inhibitory activity than that of letrozole with IC
= 0.032 ± 0.042 µM, compared to IC
= 0.024 ± 0.001 µM for letrozole. Furthermore, compound
and reference drug letrozole were docked into human placental aromatase enzyme to predict their possible binding modes with the enzyme. Finally, ADME parameters (absorption, distribution, metabolism, and excretion) of synthesized compounds (
-
) were calculated by QikProp 4.8 software.
Publisher
MDPI AG,MDPI
Subject
/ Antineoplastic Agents - chemical synthesis
/ Antineoplastic Agents - chemistry
/ Antineoplastic Agents - pharmacology
/ Aromatase Inhibitors - chemical synthesis
/ Aromatase Inhibitors - chemistry
/ Aromatase Inhibitors - pharmacology
/ Benzimidazoles - chemical synthesis
/ Benzimidazoles - pharmacology
/ Brain Neoplasms - drug therapy
/ Brain Neoplasms - enzymology
/ Cell Proliferation - drug effects
/ Cell Survival - drug effects
/ docking
/ Enzymes
/ Humans
/ MCF-7
/ Molecular Docking Simulation
/ NIH3T3
/ Nitrogen
/ Placenta
