Synthesis of Novel Alkyl Amide Functionalized Trifluoromethyl Substituted Furo/thieno Pyridine Derivatives: Their Anticancer Activity and CoMFA and CoMSIA Studies

2019 ◽  
Vol 56 (7) ◽  
pp. 1986-1998 ◽  
Author(s):  
Srinu Bhoomandla ◽  
Shravan Kumar Gunda ◽  
Srawanthi Kotoori ◽  
Phani Raja Kanuparthy
2018 ◽  
Vol 23 (3) ◽  
pp. 541-554
Author(s):  
Ruchi Verma ◽  
Indira Bairy ◽  
Mradul Tiwari ◽  
G. Varadaraj Bhat ◽  
G. Gautham Shenoy

Tetrahedron ◽  
2020 ◽  
Vol 76 (39) ◽  
pp. 131473
Author(s):  
Phanida Thongaram ◽  
Suparerk Borwornpinyo ◽  
Phongthon Kanjanasirirat ◽  
Kedchin Jearawuttanakul ◽  
Mesayamas Kongsema ◽  
...  

2020 ◽  
Vol 16 ◽  
Author(s):  
Bhagwat S. Jadhav ◽  
Vipul P. Purohit ◽  
Ramesh S. Yamgar ◽  
Rajesh S. Kenny ◽  
Suraj N. Mali ◽  
...  

Background: Tuberculosis (TB) continues to be the most threatening cause of death in recent years. There is urgent need of search more potent, less toxic antitubercular agents. Methods: A set of five new 1,3,4-oxadiazolyl-imidazo-1,2-pyridine derivatives (4a-4e) was synthesized and screened invitro for their antibacterial activity against Mycobacterium tuberculosis (H37 RV strain) ATCC No-27294. Results: Compound 4b displayed potent antitubercular activity at MIC 6.25 µg/mL. In-silico molecular docking studies were performed for evaluation of the binding patterns of compounds 4a-4e in the binding site of proteins like, Pantothenate synthatase and enoyl acyl reductase inhibitor. The outcomes of the in- vitro antitubercular studies were in well agreement with the molecular docking studies. These newly synthesized compounds were found to have good ADMET profile. We also explored possible anticancer activity using in-silico methods. Conclusion: These results shows that readily synthesized 1,3,4-oxadiazolyl-imidazo-1,2-pyridine derivatives (4a-4e) are attracting new class of potent anti-TB targets as well as possible anticancer activity that worth additional opportunities for improvements.


2017 ◽  
Vol 43 (7) ◽  
pp. 4311-4311
Author(s):  
Fatma A. Bassyouni ◽  
Hanaa A. Tawfik ◽  
Abdel Mohsen Soliman ◽  
Mohamed Abdel Rehim

2020 ◽  
Vol 90 (7) ◽  
pp. 1331-1335
Author(s):  
Suresh Babu Kokkiligadda ◽  
Sivanadh Musunuri ◽  
Bhimcharan Maiti ◽  
M. V. Basaveswara Rao ◽  
Gattu Sridhar

2021 ◽  
Vol 33 (6) ◽  
pp. 1331-1335
Author(s):  
Bhadru Bhukya ◽  
Hanmanthu Guguloth

A series of novel oxadiazole functionalized pyrazolo[3,4-b]pyridine derivatives (6a-n)was synthesized using 6-thiophenyl-4-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyridin-3-amine (1) through reaction with 2-bromoethyl acetate, followed by hydrazine hydrate to afford hydrazide derivatives (5). These compounds were further treated with aromatic acids in the presence of phosphoryl chloride and obtained oxadiazole functionalized pyrazolo[3,4-b]pyridine derivatives (6a-n). All the synthesized compounds 6a-n were screened for anticancer activity against four cancer cell lines such as HeLa - cervical cancer (CCL-2); COLO 205-colon cancer (CCL-222); HepG2-liver cancer (HB-8065); MCF7-breast cancer (HTB-22). Compounds 6i, 6m and 6n were found to have more prominent anticancer activity at micromolar concentration.


2011 ◽  
Vol 38 (7) ◽  
pp. 1291-1310 ◽  
Author(s):  
Fatma A. Bassyouni ◽  
Hanaa A. Tawfik ◽  
Abdel Mohsen Soliman ◽  
Mohamed Abdel Rehim

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