Design and Synthesis of Novel Substituted Indole-acrylamide Derivatives and Evaluation of Their Anti-Cancer Activity as Potential Tubulin-Targeting Agents

2022 ◽  
pp. 132345
Author(s):  
Mohammed Hawash ◽  
Deniz Cansen Kahraman ◽  
Abdurrahman Olgac ◽  
Sezen Guntekin Ergun ◽  
Ernest Hamel ◽  
...  
2021 ◽  
Vol 25 (11) ◽  
pp. 104-109
Author(s):  
Gullapelli Kumaraswamy ◽  
Ravichandar Maroju ◽  
Srinivas Bandari ◽  
Gouthami Dasari ◽  
Gullapelli Sadanandam

A novel series of 2-(1-((1-substitutedphenyl-1H-1,2,3- triazol-4-yl)methoxy)ethyl)-1-((1-substituted phenyl- 1H-1,2,3-triazol-4-yl)methyl)-1H-benzo[d]imidazole (3a-j)derivatives was synthesized in moderate to high yields. The structures of all the synthesized compounds were characterized by 1HNMR, 13CNMR and Mass spectroscopic methods. The title compounds were screened for their anti-oxidant activity and anti-cancer activity. The cancer activity results reveal that the compounds 3j, 3b and 3f are showing promising activity and remaining compounds exhibited moderate activity against all the tested cancer cell lines. The anti-oxidant activity also shows that the compounds 3c and 3d have shown excellent activity and remaining compounds were also found to exhibit moderate activity against the test organisms employed.


2018 ◽  
Vol 143 ◽  
pp. 1968-1980 ◽  
Author(s):  
Junjie Lan ◽  
Lan Huang ◽  
Huayong Lou ◽  
Chao Chen ◽  
Tangjingjun Liu ◽  
...  

2022 ◽  
Vol 0 (0) ◽  
Author(s):  
Sasadhar Majhi

Abstract Cancer is the uncontrolled growth and development of abnormal cells which is a major cause of death in both advanced and emerging countries. Although currently chemotherapy is most broadly used among an extensive range of anti-cancer therapies, it includes many demerits, such as highly toxic, side-effects, expensive and partial lack of targeting specificity. So the design and synthesis of new molecules that perform specifically on target proteins in tumor cells is a focus of contemporary research. So many researchers aim for new drugs that will be more efficient, more selective, and less toxic. Because of the interesting structures and significant biological profile, naturally occurring acridines and xanthines as well as their analogues have attracted considerable interest in researchers and technologists. Natural and synthetic acridine derivatives form a significant category of heterocycles having nitrogen that is of considerable interest for organic chemists and biological communities due to their attractive anti-cancer activity. Another important class of therapeutic agents with diverse biological properties including cytotoxic effects is xanthine derivatives which are collectively called xanthines (a group of alkaloids). Among many significant molecules based on the structure of the purine, there is a group of natural xanthines, involving theobromine, caffeine, and theophylline and analogues of xanthine display anti-cancer activity. Hence the present chapter wishes to concentrate the attention on the synthesis and anti-cancer activity of acridine and xanthine-based compounds brilliantly.


2021 ◽  
Vol 91 (11) ◽  
pp. 2280-2285
Author(s):  
Madhuri Pandiri ◽  
Satheesh Kumar Nukala ◽  
Gouthami Dasari ◽  
Vinitha Badithapuram ◽  
Srinivas Bandari

MedChemComm ◽  
2017 ◽  
Vol 8 (7) ◽  
pp. 1414-1420 ◽  
Author(s):  
Marcella Bassetto ◽  
Salvatore Ferla ◽  
Gilda Giancotti ◽  
Fabrizio Pertusati ◽  
Andrew D. Westwell ◽  
...  

A novel antiproliferative molecular scaffold was designed by rational modification of known antiandrogens, achieving a significant improvement in anti-cancer activity.


2013 ◽  
Vol 683 ◽  
pp. 34-37
Author(s):  
Bin Zeng ◽  
Xiao Hua Zhu

Isatin, an endogenous compound existent in many organisms, shows a wide range of biological activities. In this paper, we like to report the design and synthesis of several isatin derivatives through the acetalization and N-Acylation. Six newly synthesized compounds were characterized on the basis of 1H NMR, and those compounds were determined using two different human cancer cell . Anti-cancer activity showed those compounds IC50<50 μm.


2021 ◽  
Author(s):  
Huilan Li ◽  
Yuanying Fang ◽  
Xiang Li ◽  
Liangxing Tu ◽  
Guoliang Xu ◽  
...  

This study reported design and synthesis of NO-donating polymer to generate biodegradable polymeric micelle containing paclitaxel (NO/PTX) as a nanomedicine delivery system aimed to enhance solubility and anti-cancer activity of...


2016 ◽  
Vol 24 (21) ◽  
pp. 5611-5617 ◽  
Author(s):  
Vijaya Rao Pidugu ◽  
Nagendra Sastry Yarla ◽  
Srinivasa Rao Pedada ◽  
Arunasree M. Kalle ◽  
A. Krishna Satya

Sign in / Sign up

Export Citation Format

Share Document