Synthesis, in vitro anticancer and antimycobacterial evaluation of new 5-(2,5-dimethoxyphenyl)-1,3,4-thiadiazole-2-amino derivatives

Cytotoxic Properties of 1,3,4-Thiadiazole Derivatives—A Review

“…Some compounds have shown good inhibitory effect in the test, with the best cytotoxicity inhibition of 68.28% (HT-29) and 62.95% (MDA-MB-23) for derivatives with benzyl substituent 37 ( Figure 19 ). The derivatives were also tested on human normal cell line and they exhibited selectivity for cancer cells in that test [ 29 ].…”

Synthesis of 2,5‐Disubstituted‐1,3,4‐oxadiazole Derivatives and Their Evaluation as Anticancer and Antimycobacterial Agents

“…Introduction of electron withdrawing group fluorine (EWG) and electron donating group methoxy (EDG) in to the phenyl ring of both the series i. e., 9 & 10 , the activity profile is 9 d (4‐OCH 3 ) (4.05% inhibition) < 9 a (‐Ph) (10.14% inhibition) < 9 e (4‐F) (12.36% inhibition); 10 d (4‐OCH 3 ) (5.68% inhibition) < 10 a (‐Ph) (24.75% inhibition) < 10 e (4‐F) (30.15% inhibition) against the MDA231 cell line appears to follow the trend of electronic effects of EDG < Ph < EWG in exhibiting cytotoxic activity. The higher activity of fluorine derivative might be due to enhanced electron density, less steric issues hence improved pharmacokinetic properties, physicochemical properties, lipophilicity, electronegativity and endurance for metabolic destruction due to presence of a halogen bond . Similarly, for the structures 9 a (‐Ph), 9 b (3‐NO 2 ), 9 f (3‐Br) and 10 a (‐Ph), 10 b (3‐NO 2 ), 10 f (3‐Br) the activity pattern is the compound with the substituent having more ‐I effect displayed higher activity i. e., 3‐NO 2 > ‐Ph > 3‐Br against MDA231 cell lines thus illustrating the importance of size of the bulky bromine atom plays a crucial role in the activity.…”

“…Pathogen Mycobacterium tuberculosis is responsible for the spread of air borne disease Tuberculosis (TB) which seems to conglomerate tuberculomas. Perhaps, tuberculomas are recognized as one of the oldest cause of cancer and can affect several organs such as lungs, brain, breast, ovaries etc . From the obtained data, it is palpable that analogues 9 i , 10 i displayed highest activity among the assayed with MIC values at 39.23 μM and 40.24 μM respectively.…”

New Potent 5α- Reductase and Aromatase Inhibitors Derived from 1,2,3-Triazole Derivative

“…The pharmaceutical importance of 1,2,3-triazole ring is due to its efficacy as c-Met kinase inhibitors [1], aromatase inhibitors [2], 5α-reductase inhibitors [3], virostatic [4], antiproliferative agents [5][6][7], GABA-antagonists [8], antimicrobial agents [9,10], anti-bacterial agents [11], novel inhibitors of human immunodeficiency virus type1 protease [12], glycosidase inhibitors, antimalarial agents [13], antihistaminic agents [14], nucleosides [15], as synthetic intermediates for some antibiotic compounds [16], and also for treatment of Alzheimer's disease [17].…”