Gokulakrishnan Sakthivel
Research Subjects
Research Interests
Gokulakrishnan Sakthivel has a total of 9 co-authors. Here are the top co-authors by number of shared publications:
- Ashok Madarakhandi
Department of Pharmaceutical Chemistry, KLE College of Pharmacy, Rajajinagar, Bengaluru 560010, Karnataka, India
1 shared publication - Basavaraj Metikurki
Department of Pharmaceutical Chemistry, Nitte College of Pharmaceutical Sciences, Nitte (Deemed to be University), Yelahanka, Bengaluru 560064, India
1 shared publication - Bibha Choudhary
Institute of Bioinformatics and Applied Biotechnology
1 shared publication - Dominique Schols
Molecular, Structural and Translational Virology Research Group, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, KU Leuven, Herestraat 49, Box 1049, 3000 Leuven, Belgium
1 shared publication - Febina Ravindran
Institute of Bioinformatics and Biotechnology, Electronic City, Phase 1, Bengaluru 560100, Karnataka, India
1 shared publication - Nishith Teraiya
Department of Pharmaceutical Chemistry, K.B Institute of Pharmaceutical Education and Research, Kadi Sarva Vishvavidyalaya, Gandhinagar 382023, India
1 shared publication
Latest Publications
- Open Access
Synthesis, In Vitro Cytotoxicity Evaluation and GSK-3β Binding Study of Some Indole–Triazole-Linked Pyrazolone Derivatives
Glycogen synthase kinase-3 beta (GSK-3β) is a multifunctional serine/threonine kinase mediating multiple cellular functions, such as differentiation, apoptosis, and cell proliferation. Because of their ability to alter carcinogenic pathways, GSK-3β inhibitors are being explored for the development of anticancer molecules. In the present study, we synthesized and evaluated the cytotoxic properties of a series of twenty indole–triazole-linked pyrazolone derivatives, 10Aa–Ed. All derivatives were characterized by FTIR, 1H/13C NMR, and high-resolution mass spectrometry (HRMS) methods. All compounds and standards, sunitinib and 5-Fluorouracil (5-FU), were screened against four adherent cell lines, including pancreatic adenocarcinoma (Capan-1), colorectal carcinoma (HCT-116), glioblastoma(LN229), and lung carcinoma (NCI-4460), and four non-adherent cell lines, including acute myeloid leukemia (HL-60), chronic myeloid leukemia (K562), T lymphoblast (MOLT4), and non-Hodgkin lymphoma (Z138). Among the screened derivatives, molecule 10Aa showed cytotoxicity against MOLT 4, Z138, and HL60 with CC50 values of 14.45 μM, 15.34 μM, and 17.56 μM, respectively. GSK-3β kinase inhibition was evaluated with the 10Aa, which is capable of inhibiting GSK-3β in a dose-dependent manner. Additionally, molecular docking was performed to estimate the correlation between invitro data and GSK-3β binding affinity. The outcomes of the invitro experiments demonstrated strong concordance with the insilico data. The discovery yielded compounds 10Aa and 10Cd, which can be modified to create effective anticancer agents that target GSK-3β.
Open AccessSynthesis, In Vitro Cytotoxicity Evaluation and GSK-3β Binding Study of Some Indole–Triazole-Linked Pyrazolone Derivatives
Glycogen synthase kinase-3 beta (GSK-3β) is a multifunctional serine/threonine kinase mediating multiple cellular functions, such as differentiation, apoptosis, and cell proliferation. Because of their ability to alter carcinogenic pathways, GSK-3β inhibitors are being explored for the development of anticancer molecules. In the present study, we synthesized and evaluated the cytotoxic properties of a series of twenty indole–triazole-linked pyrazolone derivatives, 10Aa–Ed. All derivatives were characterized by FTIR, 1H/13C NMR, and high-resolution mass spectrometry (HRMS) methods. All compounds and standards, sunitinib and 5-Fluorouracil (5-FU), were screened against four adherent cell lines, including pancreatic adenocarcinoma (Capan-1), colorectal carcinoma (HCT-116), glioblastoma(LN229), and lung carcinoma (NCI-4460), and four non-adherent cell lines, including acute myeloid leukemia (HL-60), chronic myeloid leukemia (K562), T lymphoblast (MOLT4), and non-Hodgkin lymphoma (Z138). Among the screened derivatives, molecule 10Aa showed cytotoxicity against MOLT 4, Z138, and HL60 with CC50 values of 14.45 μM, 15.34 μM, and 17.56 μM, respectively. GSK-3β kinase inhibition was evaluated with the 10Aa, which is capable of inhibiting GSK-3β in a dose-dependent manner. Additionally, molecular docking was performed to estimate the correlation between invitro data and GSK-3β binding affinity. The outcomes of the invitro experiments demonstrated strong concordance with the insilico data. The discovery yielded compounds 10Aa and 10Cd, which can be modified to create effective anticancer agents that target GSK-3β.