التفاصيل البيبلوغرافية
| العنوان: |
Design, Synthesis, and In-Vitro Biological Evaluation of Novel THQ Derivatives as Anticancer Agents. |
| المؤلفون: |
Dey, Rajdeep1, Shaw, Suman1, Patel, Bhumika1, Bhatt, Hardik1, Patel, Saumya2, Dixit, Nandan2, Chaube, Udit1 uditchoube@gmail.com |
| المصدر: |
Malaysian Journal of Medicine & Health Sciences. 2024 Supplement, Vol. 20, p27-27. 1p. |
| مصطلحات موضوعية: |
*ANTINEOPLASTIC agents, *MTOR inhibitors, *CONTOURS (Cartography), *COLON cancer, *DRUG resistance |
| مستخلص: |
Introduction: The lack of effective treatments and drug resistance provides significant challenges in the treatment of cancer. PI3K/AKT/mTOR pathway was chosen in the current study as a key alternative target for the mitigation of cancer which can resolve the issue of futile treatment and drug resistance. Methods: The mTOR inhibitors were designed based on pharmacophore-based virtual screening findings and the contour map analysis of field-based and atom-based 3D-QSAR models. By combining the virtual hits with the compounds from the preclinical and clinical studies, the common active aspects for activity against mTOR (C1 and C2) were identified leading to a knowledge-based selection of tetrahydroquinoline (THQ) scaffold. Further, these novel tetrahydroquinoline (THQ) derivatives were designed and synthesized. Spectral characterization of these compounds was carried out with the aid of 1H NMR, 13C NMR, and D2O exchange, confirming the formation of the desired compounds. Moreover, these optimized THQ derivatives were evaluated against the various panel of cell lines viz. colon cancer (HT-29), breast cancer (MCF-7), and lung cancer (A-549). Results: Among all the synthesized compounds, compound UC-BzCl-01 showed promising anticancer activity against the panel of these cancer cell lines. Further, FACS analysis of these THQ derivatives was carried out where UC-BzCl-01 demonstrated apoptotic characteristics. Conclusion: Based on the results of the study, UC-BzCl-01 may be explored further as a possible mTOR inhibitor and potential anticancer agent. [ABSTRACT FROM AUTHOR] |
| قاعدة البيانات: |
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