Design, synthesis, and biological and docking studies of novel epipodophyllotoxin–chalcone hybrids as potential anticancer agents

MedChemComm ◽  
2015 ◽  
Vol 6 (1) ◽  
pp. 94-104 ◽  
Author(s):  
Abid Hussain Banday ◽  
Vinod V. Kulkarni ◽  
Victor J. Hruby
Keyword(s):  
Click Chemistry ◽  
Anticancer Agents ◽  
Topoisomerase Ii ◽  
Docking Studies ◽  
Efficient Synthesis ◽  
Design Synthesis ◽  
Topoisomerase Ii Inhibitors

Click-chemistry based design and efficient synthesis of podophyllotoxin–chalcone conjugates as potential topoisomerase-II inhibitors towards the development of better anticancer leads.

Design, synthesis and evaluation of structurally diverse ortho-acylphenol-diindolylmethane hybrids as anticancer agents

2022 ◽  
Author(s):  
Zhi-Gang Yin ◽  
Xiong-Wei Liu ◽  
Hui-Juan Wang ◽  
Min Zhang ◽  
Xiong-Li Liu ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Anticancer Agents ◽  
Nucleophilic Addition ◽  
Ring Opening ◽  
Building Blocks ◽  
Efficient Synthesis ◽  
Design Synthesis ◽  
Pyrone Ring ◽  
Ring Opening Reaction ◽  
First Time

A highly efficient synthesis of structurally diverse ortho-acylphenol–diindolylmethane hybrids 3 using carboxylic acid-activated chromones as versatile synthetic building blocks is reported here for the first time, through 1,4-nucleophilic addition and followed by a decarboxylation and pyrone ring opening reaction process.

scholarly journals 6,7-Disubstituted-4-anilinoquinazoline: Design, Synthesis and Anticancer Activity as a Novel Series of Potent Anticancer Agents

2020 ◽  
Vol 27 (2) ◽  
pp. 209-218
Author(s):  
Fatemeh Azmian Moghadam ◽  
Mehdi Evazalipour ◽  
Hassan Kefayati ◽  
Saeed Ghasemi
Keyword(s):  
Growth Factor ◽  
Anticancer Agents ◽  
Growth Factor Receptor ◽  
Docking Studies ◽  
Anticancer Activities ◽  
Design Synthesis ◽  
Atp Binding Site ◽  
Novel Approach ◽  
Epidermal Growth ◽  
Endothelial Growth Factor

Background: Epidermal Growth Factor Receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR) are responsible for several pathological conditions such as the development of different kinds of tumors. The combined inhibition of both signal transduction pathways seems to be a promising novel approach for cancer treatment. Methods: In this study, novel 4-anilinoquinazoline derivatives with various substituents on-7 position of quinazoline moiety were designed, synthesized, and evaluated for their antiproliferative activity against A431 and HU02 cell lines. Results: Compounds 8a, 8d, and 8f displayed the most potent anticancer activities against A431(IC50 = 1.78 μM, 8.25 μM, and 7.18 μM, respectively) in comparison with reference standards(erlotinib IC50=8.31 μM and vandetanib IC50=10.62 μM). Molecular docking studies proved that8a as the most potent compound could be efficiently accommodated in the ATP binding site ofEGFR and VEGFR-2 through the formation of essential hydrogen bonds between quinazolineN1 atom and the Met796 backbone of EGFR as well as the Cys919 backbone of VEGFR-2 with a distance of 1.94 Å and 1.398 Å, respectively. Conclusion: Compound 8a as the most potent compound with morpholine and 3-bromoaniline at the 7 and 4 positions of quinazoline scaffold, respectively, deserves more study and structural optimization as an anticancer agent.

Sign in / Sign up

Export Citation Format

Share Document