I have been working with KLE College of Pharmacy Bangalore (India) since July 2007 in the Department of Pharmaceutical Chemistry (Associate Professor at present). During my master’s (Pharmaceutical Chemistry) and PhD, I worked on nitrogen, oxygen, and sulfur-containing biologically active small heterocyclic molecules. My Post-doctoral research in the Department of Biomaterials Science at the Pusan National University Republic of Korea gave me in-depth knowledge about the functionalization of biopolymers as a drug delivery tool. Multistep synthesis of heterocyclic molecules, their purification and, structural characterization is the area of my research. I believe in teamwork and collaborative research. In the 15 years of teaching & research, I contributed to 35 research articles. Pharmaceutics, Cell, FEBS, Scientific Reports, EJMC, BMCL, Molecular Carcinogenesis and RSC Advances are few among them
EDUCATION
PhD in Pharmaceutical Sciences (JNTU, Hyderabad)
RESEARCH, TEACHING, or OTHER INTERESTS
Drug Discovery, Pharmaceutical Science, Cancer Research, Organic Chemistry
52
Scopus Publications
1437
Scholar Citations
16
Scholar h-index
27
Scholar i10-index
Scopus Publications
Synthesis, In Vitro Cytotoxicity Evaluation and GSK-3β Binding Study of Some Indole–Triazole-Linked Pyrazolone Derivatives Ashok Madarakhandi, Sujeet Kumar, Nishith Teraiya, Gokulakrishnan Sakthivel, Basavaraj Metikurki, Veda B. Hacholli, Dominique Schols, Febina Ravindran, Bibha Choudhary, Subhas S. Karki Chemistry Switzerland, 2026 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.
Functional Characterization of VS-186B, a Novel HDAC Inhibitor with Anticancer Activity Laura A. Sanchez-Michael, Vijayalakshmi Sudarshan, Allison Elias, Denisse A. Gutierrez, Jose A. Lopez-Saenz, Jaqueline Pena-Zacarias, Gabriela C. Torres, Armando Varela-Ramirez, Sujeet Kumar, Subhas S. Karki, Renato J. Aguilera International Journal of Molecular Sciences, 2025 Histone acetylation and deacetylation are key regulators of gene expression and are frequently dysregulated in cancer, contributing to tumorigenesis and drug resistance. Overexpression of histone deacetylases (HDACs) in many cancer types leads to silencing of tumor suppressor genes and uncontrolled proliferation. Tumors often rely on epigenetic mechanisms to escape therapy and develop resistance. This study aimed to identify novel compounds that selectively target cancer cells while minimizing toxicity to non-cancerous cell lines. A series of novel HDAC inhibitors was evaluated using the Differential Nuclear Staining (DNS) assay, flow cytometry, and HDAC inhibition assays. These assays assessed cytotoxicity, selectivity, and mechanisms of cell death. Among seven compounds tested, VS-186B exhibited the highest cytotoxicity and Selective Cytotoxicity Index (SCI), particularly against the human Jurkat T-cell leukemia cell line. Flow cytometry experiments (Annexin V-FITC, ROS, JC-1, and Caspase-3/7 assays) revealed that VS-186B induced apoptosis. VS-186B was more cytotoxic than Curcumin and Vorinostat across most of the cell lines tested and was more specific to hematological cells. Connectivity Map (CMap) analysis showed strong similarity to genes affected by known HDAC inhibitors. Subsequently, HDAC enzymatic assays confirmed that VS-186B inhibits Class I and II HDACs in a dose-dependent manner. VS-186B exhibits promising anticancer potential as a selective HDAC inhibitor since it induces apoptosis in cancer cells without significant cytotoxicity to non-cancerous lines with a similar gene expression profile to known HDAC inhibitors. These findings support further development of VS-186B as an epigenetic treatment for leukemia/lymphoma.
Andrographolide and Mahua Oil-Infused Emulgels: A Comprehensive QbD, In Vitro, and In Silico Strategy for Skin Pigmentation Treatment N. V. L. Sirisha Mulukuri, Ranjitha Acharya, Sujeet Kumar, Nishith Teraiya, Digambar B. Yevale, Pankaj Kumar Chemistry and Biodiversity, 2025 Skin pigmentation disorders such as melasma, hyperpigmentation and age spots are primarily associated with excessive melanin production and are a significant dermatological concern. To address this issue, the present study aimed to develop an effective skin‐lightening formulation by synergising the therapeutic benefits of andrographolide with the skin permeation‐enhancing properties of Mahua oil. A two‐factor factorial design was employed to formulate and optimise the emulgel using a quality by design (QbD) approach. The optimised formulation (AG‐6) was subjected to a series of evaluations, including preliminary characterisation, biocompatibility analysis, in vivo skin uptake studies and tyrosinase inhibition assays. Biocompatibility assessment revealed a 92.64% viability of human dermal fibroblast (HDF) cells after 24 h of AG‐6 treatment, indicating low cytotoxicity. Tyrosinase inhibition was observed at 28.94 µg/mL for AG‐6, which is comparable to the reference standard Kojic acid (25.37 µg/mL). Furthermore, molecular docking studies demonstrated that andrographolide exhibited a stronger binding affinity with tyrosinase‐related protein 1 (TYR1, PDB ID: 5M8L), with a binding energy of −7.9 kcal/mol, as compared to kojic acid (−5.6 kcal/mol). These findings suggest that the optimised emulgel AG‐6 holds significant potential for the management of skin pigmentation disorders.
Investigation of Anti-Cancer Properties of Novel Curcuminoids in Leukemic Cells and Dalton Lymphoma Ascites Model Vijayalakshmi Sudarshan, P. Shyamjith, Sujeet Kumar, Febina Ravindran, Bibha Choudhary, Subhas S. Karki International Journal of Molecular Sciences, 2025 Leukemia, one of the major causes of cancer death, ranks 11th worldwide among cancer-related deaths. The current treatment of leukemia faces challenges recently due to a high burden of side effects. It is well established that curcumin has anticancer and tumor-suppressing activities in several cancers in addition to leukemia. Accordingly, 15 derivatives were designed and prepared to improve the shortcomings of curcumin, such as poor aqueous solubility, chemical instability, and low bioavailability. All 15 were evaluated for cytotoxicity against the leukemic cell line MOLT-4, which led to the prioritization and further evaluation of compound curcuminoid (2E,5E)-2,5-bis((3-(4-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)cyclopentan-1-one 5i. 5i. Compared to curcumin, 5i was significantly more effective in inducing mitochondrial dysfunction in MOLT-4 cells; hence increased ROS production and cytotoxicity. Treatment groups showed change in mitochondrial membrane potential by flow cytometry analysis. Moreover, tumor volume reduction observed with 5i treatment in Dalton’s Lymphoma model was accompanied with low toxicity. Intrinsic pathways of apoptosis was initiated by compound 5i that lowered Bcl-2 expression while augmenting cytochrome c, Bak and Bax levels both in vivo and in vitro. These results showcase the potent antiproliferative as well as cytotoxic effects of 5i at nanomolar doses against leukemia being at least 60 times more effective than curcumin.
Dysfunctional mitochondrial bioenergetics sustains drug resistance in cancer cells Davide Gnocchi, Dragana Nikolic, Silvia Russo, Maria Laura Matrella, Rosa R. Paparella, Sujeet Kumar, Subhas S. Karki, Carlo Sabbà, Tiziana Cocco, Simona Lobasso, Antonio Mazzocca American Journal of Physiology Cell Physiology, 2025 Cancer drug resistance (CDR) is increasingly becoming a concerning clinical problem. The mechanisms behind the onset of CDR are still not well defined. In this study, we demonstrated that a treatment mimicking long-term clinical protocols with commonly used chemotherapeutic agents promotes mitochondrial bioenergetic dysfunction, leading to the acquisition of CDR. In a future perspective, interventions aimed at inhibiting fermentation and restoring OXPHOS efficiency may offer tangible opportunities to reduce the clinical burden of CDR.
Identification and characterization of novel ligase I inhibitors Monica Pandey, Sujeet Kumar, Gunaseelan Goldsmith, Mrinal Srivastava, Santhini Elango, Mohammad Shameem, Dibyendu Bannerjee, Bibha Choudhary, Subhas S. Karki, Sathees C. Raghavan Molecular Carcinogenesis, 2017
Synthesis and cytotoxic evaluation of some 2-{4-[(2-oxo-1,2-dihydro-3h-indol-3-ylidene)methyl] phenoxy}-n-phenylacetamide Acta Poloniae Pharmaceutica Drug Research, 2017
Synthesis and Characterization of Piperazine-Linked Eugenol Derivative MG Yenagunte Narayanaswamy, S Kumar, SR Setty, B Metikurki, ... Molbank 2026 (3), M2180 , 2026 2026
Synthesis, In Vitro Cytotoxicity Evaluation and GSK-3β Binding Study of Some Indole–Triazole-Linked Pyrazolone Derivatives Madarakhandi A, Kumar S, Teraiya N, Sakthivel G, Metikurki B, Hacholli VB ... chemistry (Switzerland) 8 (2), 17 , 2026 2026
Functional Characterization of VS-186B, a Novel HDAC Inhibitor with Anticancer Activity Laura A. Sanchez-Michael, Vijayalakshmi Sudarshan, Allison Elias, Denisse A ... International Journal of Molecular Sciences 26, 11354 , 2025 2025 Citations: 2
Assessing the anti-leukemic efficacy of a curcuminoid in cellular and animal models V Sudarshan, P Shyamjith, S Kumar, F Ravindran, N Teraiya, ... European Journal of Medicinal Chemistry, 118177 , 2025 2025 Citations: 3
Impact of NaI/KI blending on structural, optical, and impedance properties of sodium carboxymethyl cellulose biopolymer films S Nalina, S Kumar, T Bhat, V Prakruthi, NS Keerthana, SS Pattanshetty, ... Polymer Bulletin 82 (12), 6455-6485 , 2025 2025
Design, synthesis and anticancer evaluation of novel hydrazide-2-oxindole analogues asGSK-3-beta kinase inhibitors Madarakhandi A, Kumar S, Terayia N, Schols D, Vastrad S.J, Shyamjith P ... RSC Advances 15, 24650 , 2025 2025 Citations: 2
Andrographolide and Mahua Oil-Infused Emulgels: A comprehensive QbD, in vitro, and in silico strategy for skin pigmentation treatment. Sirisha Mulukuri NVL, Acharya R, Kumar S, Teraiya N, Yevale DB, Kumar P Chemistry &Biodiversity, e00166. , 2025 2025
Synthesis of novel pyridazine and pyrimidine linked pyrazole derivatives as DNA ligase 1 and IV inhibitors that induce apoptosis S Aishwarya, GC Torres, JA Lopez-Saenz, DA Gutierrez, S Kumar, ... Chemico-Biological Interactions 414, 111509 , 2025 2025 Citations: 3
Dysfunctional mitochondrial bioenergetics sustains drug resistance in cancer cells D Gnocchi, D Nikolic, S Russo, ML Matrella, RR Paparella, S Kumar, ... American Journal of Physiology-Cell Physiology 328 (4), C1150-C1159 , 2025 2025 Citations: 11
Investigation of anti-cancer properties of novel curcuminoids in leukemic cells and Dalton lymphoma ascites model V Sudarshan, P Shyamjith, S Kumar, F Ravindran, B Choudhary, SS Karki International Journal of Molecular Sciences 26 (7), 3186 , 2025 2025 Citations: 2
Synthesis, in silico ADME, Molecular Docking and in vitro Cytotoxicity Evaluation of Indolin-2-one linked Stilbene Derivatives Dimple Pirgal, Subhas S. Karki, Sujeet Kumar, Basavaraj Metikurki Asian Journal of Chemistry 37 (3), 737-744 , 2025 2025
Synthesis, molecular docking, dynamics study and preliminary cytotoxicity study of some coumarin linked imidazothiadiazoles S Kumar, PV Sravani, S Gokulakrishnan, S Khushwah, B Metikurki, ... Journal of Molecular Structure 1321, 139943 , 2025 2025 Citations: 2
1, 4-Disubstituted-1, 2, 3-triazole Linked Cyclic Ketones Ascytotoxic Agents A Kumar, S Kumar, A Das, B Metikurki, D Schols, SSS Karki Asian Journal of Chemistry 37 (8) , 2025 2025
Discovery of new pyrazole-4-carboxamide analogues as potential anticancer agents targeting dual Aurora kinase A and B Digambar Yevale, Nishith Teraiya, Twinkle Lalwani, Mayur Dalasaniya, Saumya ... European Journal of Medicinal Chemistry, 116917 , 2024 2024 Citations: 17
Synthesis, In silico Study and Cytotoxicity Evaluation of Some Newly Synthesized Stilbene Derivatives Dimple Pirgal, Subhas S. Karki, Sujeet Kumar, Basavraj Metikurki Asian Journal of Chemistry 36 (8), 1882-1888 , 2024 2024
Statistical modeling, optimization and characterization of andrographolide loaded emulgel for its therapeutic application on skin cancer through enhancing its skin permeability M Sirisha, S Kumar, D Moumita, GD Rajesh, P Kumar Saudi Pharmaceutical Journal 32 (2024), 102068 , 2024 2024 Citations: 10
Abstract 2396 Novel Ligase 1 and 4 Inhibitor Compounds as Potential Drugs for Cancer Treatment GT Quesada, L Sanchez-Michael, D Gutierrez, A Varela-Ramirez, P Jain, ... Journal of Biological Chemistry 300 (3) , 2024 2024
PP053 SP11, a promising coumarin-imidazothiadiazole derivative, targets HSP90 and client proteins to inhibit tumor growth MV Shahana, S Nirgude, F Ravindran, S Kumar, S Sharma, R Mahadeva, ... ESMO Open 8 (1) , 2023 2023 Citations: 1
Enhancing the Thermoelectric Power Factor by Lowering the Electrical Resistivity of Bi 2 Se 3 /NaI Composites Prepared by Solid-State Reaction Vivekananda, PK Prarthana, M Archana, R Gowrishree, T Bhat, ... Journal of Electronic Materials 52 (12), 8076-8085 , 2023 2023
Synthesis of novel pyrazole-oxindole conjugates with cytotoxicity in human cancer cells via apoptosis Subhas S Karki, Pravesh J, Gutierrez D A, Kumar S, Aguilera R J Chemistry & Biodiversity , 2023 2023 Citations: 3
MOST CITED SCHOLAR PUBLICATIONS
An inhibitor of nonhomologous end-joining abrogates double-strand break repair and impedes cancer progression M Srivastava, M Nambiar, S Sharma, SS Karki, G Goldsmith, M Hegde, ... Cell 151 (7), 1474-87 , 2012 2012 Citations: 469
Synthesis and biological evaluation of novel 2-aralkyl-5-substituted-6-(4′-fluorophenyl)-imidazo [2, 1-b][1, 3, 4] thiadiazole derivatives as potent anticancer agents SS Karki, K Panjamurthy, S Kumar, M Nambiar, SA Ramareddy, ... European journal of medicinal chemistry 46 (6), 2109-16 , 2011 2011 Citations: 142
A Novel Resveratrol Based Tubulin Inhibitor Induces Mitotic Arrest and Activates Apoptosis in Cancer Cells. E Thomas, V Gopalakrishnan, M Hegde, S Kumar, SS Karki, SC Raghavan, B Choudhary Scientific Reports 6, 34653 , 2016 2016 Citations: 93
Novel levamisole derivative induces extrinsic pathway of apoptosis in cancer cells and inhibits tumor progression in mice M Hegde, SS Karki, E Thomas, S Kumar, K Panjamurthy, ... PloS one 7 (9), e43632 , 2012 2012 Citations: 70
Investigation of anti-cancer and migrastatic properties of novel curcumin derivatives on breast and ovarian cancer cell lines. Koroth J, Nirgude S, Tiwari S, Gopalakrishnan V, Mahadeva R, Kumar S, Karki ... BMC Complementary and Alternative Medicine 19 (273), 1-16 , 2019 2019 Citations: 62
Identification of a novel BCL2-specific inhibitor that binds predominantly to the BH1 domain. NK D Iyer, SV Vartak, A Mishra, G Goldsmith, S Kumar, M Srivastava, M Hegde ... The FEBS Journal 283, 3408-3437 , 2016 2016 Citations: 53
Odorless glutathione microneedle patches for skin whitening. SY Lee, Y., Kumar, S., Kim, S.H., Seong, K.Y., Lee, H., Kim, C., Jung, Y.S ... Pharmaceutics 12 (2), 1-12 , 2020 2020 Citations: 51
Synthesis and antiproliferative activity of imidazo [2, 1-b][1, 3, 4] thiadiazole derivatives S Kumar, V Gopalakrishnan, M Hegde, V Rana, SS Dhepe, ... Bioorganic & Medicinal Chemistry Letters 24 (19), 4682-4688 , 2014 2014 Citations: 48
2-(4-Chlorobenzyl)-6-arylimidazo [2, 1-b][1, 3, 4] thiadiazoles: synthesis, cytotoxic activity and mechanism of action S Kumar, M Hegde, V Gopalakrishnan, VK Renuka, SA Ramareddy, ... European journal of medicinal chemistry 84, 687-697 , 2014 2014 Citations: 46
Synthesis, anticancer and cytostatic activity of some 6H-indolo [2, 3-b] quinoxalines S Karki, R Hazare, S Kumar, V Bhadauria, J Balzarini, E De Clercq Acta Pharmaceutica 59 (4), 431-440 , 2009 2009 Citations: 41
ST09, a novel curcumin derivative, blocks cell migration by inhibiting matrix metalloproteases in breast cancer cells and inhibits tumor progression in EAC mouse tumor models S Nirgude, R Mahadeva, J Koroth, S Kumar, KSS Kumar, ... Molecules 25 (19), 4499 , 2020 2020 Citations: 39
Synthesis and evaluation of the biological activity of N'-[2-oxo-1,2 dihydro-3H-indol-3-ylidene] benzohydrazides as potential anticancer agent. SSK Arpit Katiyar,Mahesh Hegde, Sujeet Kumar, Vidya Gopalakrishnan, Khyati D ... RSC Advances 5, 45492-501 , 2015 2015 Citations: 28
Microwave-assisted synthesis and antimicrobial activity of some imidazo [2, 1-b][1, 3, 4] thiadiazole derivatives S Dhepe, S Kumar, R Vinayakumar, SA Ramareddy, SS Karki Medicinal Chemistry Research 21 (8), 1550-1556 , 2012 2012 Citations: 28
Identification and characterization of novel ligase I inhibitors M Pandey, S Kumar, G Goldsmith, M Srivastava, S Elango, M Shameem, ... Molecular carcinogenesis 56 (2), 550-566 , 2017 2017 Citations: 25
1-Arylmethyl-2, 3-dioxo-2, 3-dihydroindole thiosemicarbazones as leads for developing cytotoxins and anticonvulsants SS Karki, VS Bahaduria, V Rana, S Kumar, PG Subbaro, U Das, ... Journal of enzyme inhibition and medicinal chemistry 24 (2), 537-544 , 2009 2009 Citations: 23
Discovery of new pyrazole-4-carboxamide analogues as potential anticancer agents targeting dual Aurora kinase A and B Digambar Yevale, Nishith Teraiya, Twinkle Lalwani, Mayur Dalasaniya, Saumya ... European Journal of Medicinal Chemistry, 116917 , 2024 2024 Citations: 17
Synthesis, molecular docking, and preliminary cytotoxicity study of some novel 2-(naphthalen-1-yl)-methylimidazo [2, 1-b][1, 3, 4] thiadiazoles B Choodamani, S Kumar, AK Gupta, D Schols, H Tahtaci, T Karakurt, ... Journal of Molecular Structure 1234, 130174 , 2021 2021 Citations: 14
Synthesis and antimicrobial activity of some 3-substituted-2-oxindole derivatives SS Karki, R Hazare, S Kumar, A Saxena, A Katiyar Turkish Journal of Pharmaceutical Sciences 8, 169-178 , 2011 2011 Citations: 14
Synthesis, characterization, and biological evaluation of some 4-((thiophen-2- yl -methylene)amino)benzenesulfonamide metal complexes EV Sekhar, SS Karki, J Rangaswamy, M Bhat, S Kumar Beni-Suef University Journal of Basic and Applied Sciences 10 (1), 28 , 2021 2021 Citations: 13
Synthesis, Molecular Docking and Preliminary Antileukemic Activity of 4‐Methoxybenzyl Derivatives Bearing Imidazo[2,1‐ b ][1,3,4]thiadiazole B Choodamani, KG Cano Hernandez, S Kumar, AM Tony, ... Chemistry & biodiversity 18 (2), e2000800 , 2021 2021 Citations: 13
GRANT DETAILS
UGC sponsored project (Diary KABA023/UGCSWRO, dated 28-3-2014 (₹ 1,85,000.00).
AICTE sponsored Research Promotion Scheme, F. No. 8023/BOR/RID/RP S-103/ 2009-10 dated 2211-2010 (₹ 14,30,000.00).
RESEARCH OUTPUTS (PATENTS, SOFTWARE, PUBLICATIONS, PRODUCTS)
Indian Patent filed (as co-inventor), Title: Novel inhibitors of anti-apoptotic BCL-2 Proteins.
US Patent filed (as co-inventor), Title: Pyrazole derivatives with anticancer activity.