Design, Synthesis and In Vitro Anticancer Activity of a New Class of Bifunctional DNA Intercalators

2010 ◽  
Vol 7 (9) ◽  
pp. 644-649 ◽  
Author(s):  
Ana Maria V. Zbancioc ◽  
Gheorghita N. Zbancioc ◽  
Catalin Tanase ◽  
Anca Miron ◽  
Cornelia Ursu ◽  
...  
MedChemComm ◽  
2016 ◽  
Vol 7 (12) ◽  
pp. 2349-2363 ◽  
Author(s):  
Koneni V. Sashidhara ◽  
L. Ravithej Singh ◽  
Mohammad Shameem ◽  
Sarika Shakya ◽  
Anoop Kumar ◽  
...  

A series of rationally designed new class of hLig1 inhibitors with potentin vitroanti-cancer properties is presented.


2012 ◽  
Vol 50 ◽  
pp. 344-349 ◽  
Author(s):  
E. Rajanarendar ◽  
M. Nagi Reddy ◽  
S. Rama Krishna ◽  
K. Govardhan Reddy ◽  
Y.N. Reddy ◽  
...  

ChemInform ◽  
2012 ◽  
Vol 43 (35) ◽  
pp. no-no
Author(s):  
E. Rajanarendar ◽  
M. Nagi Reddy ◽  
S. Rama Krishna ◽  
K. Govardhan Reddy ◽  
Y. N. Reddy ◽  
...  

2013 ◽  
Vol 36 (1) ◽  
pp. 41-50 ◽  
Author(s):  
Khaled A. M. Abouzid ◽  
Nadia A. Khalil ◽  
Eman M. Ahmed ◽  
Khaled Omar Mohamed

ChemBioChem ◽  
2002 ◽  
Vol 3 (11) ◽  
pp. 1137-1141 ◽  
Author(s):  
David A. Carcache ◽  
Simone R. Hörtner ◽  
Andreas Bertogg ◽  
Christoph Binkert ◽  
Daniel Bur ◽  
...  

2020 ◽  
Vol 20 (15) ◽  
pp. 1559-1571 ◽  
Author(s):  
Sumit Tahlan ◽  
Balasubramanian Narasimhan ◽  
Siong Meng Lim ◽  
Kalavathy Ramasamy ◽  
Vasudevan Mani ◽  
...  

Background: Various analogues of benzimidazole are found to be biologically and therapeutically potent against several ailments. Benzimidazole when attached with heterocyclic rings has shown wide range of potential activities. So, from the above provided facts, we altered benzimidazole derivatives so that more potent antagonists could be developed. In the search for a new category of antimicrobial and anticancer agents, novel azomethine of 2-mercaptobenzimidazole derived from 3-(2- (1H-benzo[d]imidazol-2-ylthio)acetamido)benzohydrazide were synthesized. Results and Discussion: The synthesized analogues were characterized by FT-IR, 1H/13C-NMR and MS studies as well C, H, N analysis. All synthesized compounds were evaluated for in vitro antibacterial activity against Gram-positive (B. subtilis), Gram-negative (E. coli, P. aeruginosa, K. pneumoniae and S. typhi) strains and in vitro antifungal activity against C. albicans and A. niger strains by serial dilution method, the minimum inhibitory concentration (MIC) described in μM/ml. The in vitro anticancer activity of synthesized compounds was determined against human colorectal carcinoma cell line (HCT- 116) using 5-fluorouracil as standard drug. Conclusion: In general, most of the synthesized derivatives exhibited significant antimicrobial and anticancer activities. Compounds 8, 10, 15, 16, 17, 20 and 22 showed significant antimicrobial activity towards tested bacterial and fungal strains and compound 26 exhibited significant anticancer activity.


2020 ◽  
Vol 17 (12) ◽  
pp. 959-968
Author(s):  
Ramamurthy Katikireddy ◽  
Ramu Kakkerla ◽  
M.P.S. Murali Krishna ◽  
Gandamalla Durgaiah ◽  
Y.N. Reddy

A series of benzimidazolyl-1,3,4-oxadiazoles (7a-k) were synthesized and evaluated for in vitro anticancer activity against HeLa, MCF7, A549, and HEK293 cell lines. The results indicate that compounds 7b, 7j and 7k have shown excellent anticancer activity and while most of the compounds were non toxic to normal HEK293 cell lines. Molecular docking results of the synthesized compounds with the target Pin1 protein were also discussed.


INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (12) ◽  
pp. 20-27
Author(s):  
S. S Bhat ◽  
◽  
S. N. MamleDesai ◽  
V. Narvekar ◽  
S. G Shingade ◽  
...  

The present work deals with the synthesis of a series of 6-substituted-4-hydroxy-1-(2-substitued alicyclicaminoacetyl)-3-nitroquinolin-2(1H)-one {IVa-d (1-3)} derivatives and evaluation of their in vitro anticancer activity. Docking study was carried out using EGFR-tyrosine kinase binding site (PDB ID: 1m17) and revealed encouraging results. The sequence of reactions consists of the initial synthesis of 6-substituted 4-hydroxyquinolin-2(1H)-ones (Ia-d), which were further subjected to nitration reaction to give 6- substituted-4-hydroxy-3-nitroquinolin-2(1H)-one (IIa-d). Condensation of compounds (IIa-d) with chloroacetyl chloride resulted in 6-substituted-1-(2-chloroacetyl)-4-hydroxy-3-nitroquinolin-2(1H)-one(IIIa-d), which was subjected to substitution reaction using various secondary amines to yield the title compounds {IVa-d (1-3)}. All the synthesized compounds were characterized by IR, NMR and mass spectral data.All the derivatives were tested for their in vitro anticancer activity using KB (oral cancer) cell lines. Among the synthesized compounds, compound (IVc-2) was found to be the most cytotoxic as compared to the other synthesized derivatives, with IC50 values of 0.2406μM/mL against KB cell line.


2009 ◽  
Vol 52 (3) ◽  
pp. 868-877 ◽  
Author(s):  
Anna-Marie Lord ◽  
Mary F. Mahon ◽  
Matthew D. Lloyd ◽  
Michael D. Threadgill

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