New Imidazo[4,5-c]pyridine-piperidine Hybrids as Potential Anti-cancer Agents and In-Silico Studies

被引:9
作者
Rejinthala, Swathi [1 ]
Endoori, Srinivas [2 ]
Thumma, Vishnu [3 ]
Mondal, T. [1 ]
机构
[1] Koneru Lakshmaiah Educ Fdn, Dept Engn Chem, Hyderabad 500075, Telangana, India
[2] Koneru Lakshmaiah Educ Fdn, Coll Engn, Dept Engn Chem, Guntur 522302, Andhra Prades, India
[3] Matrusri Engn Coll, Dept Sci & Humanities, Hyderabad 500059, Telangana, India
来源
CHEMISTRYSELECT | 2024年 / 9卷 / 02期
关键词
Imidazo [4,5-c]pyridines-piperdines hybrids; Anti-cancer; MCF cell line; A549 cell line; Docking studies; Estrogen receptor alpha (ER alpha); BIOLOGICAL EVALUATION; DNA-BINDING; DERIVATIVES; SULFONAMIDE; DESIGN; INHIBITORS; MOIETY; CANCER;
D O I
10.1002/slct.202303299
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Design and synthesis of a series of novel hybrid molecules that combine Imidazo[4,5-c] pyridines with piperdines are presented in this paper. Total 17 derivatives were meticulously synthesized and characterized using H-1 NMR, C-13 NMR, MS and elemental analysis techniques. The in vitroanticancer activities are estimated by verifying their effectiveness against the MCF-7 human breast adenocarcinoma and A549 lung cancer cell line, with cisplatin and doxorubicin serving as reference drugs. Several of these compounds demonstrated significant potential, displaying IC50 values within the range of 12.26-84.5 mu M for A549, and 13.37-69.82 mu M for MCF-7. Notably, compound 11 bis found to be more potent than the standard drug cisplatin with an IC50 of 12.26 +/- 0.8 mu M against A549 cells, while compound 11 d exhibited highest inhibition with an IC50 of 13.37 +/- 0.4 mu M against MCF-7 cells. Although its effectiveness was moderately lower when compared to doxorubicin, it still retained substantial anticancer activity. Molecular docking studies were performed to decouple the binding affinity and ligand interactions of the compounds with the estrogen receptor alpha (ER alpha) (PDB ID: 3ERT). The pharmacokinetic evaluation revealed favourable drug-likeness properties for all the molecules, suggesting their potential as therapeutic agents.
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页数:11
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