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Article ; Online: Editorial (Thematic Issue: Drug Reprofiling: An Alternative Path to Drug Discovery).

Ramaa, C S

2016 Volume 16, Issue 19, Page(s) 2067–2068

MeSH term(s)	Drug Discovery ; Drug Repositioning
Language	English
Publishing date	2016-06-06
Publishing country	United Arab Emirates
Document type	Editorial ; Introductory Journal Article
ZDB-ID	2064823-6
ISSN	1873-4294 ; 1568-0266
ISSN (online)	1873-4294
ISSN	1568-0266
DOI	10.2174/156802661619160530204415
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Article: Hypoglycemic and Hypolipidemic Swords: Synthesis and

Patil, Vijay / Upadhyay, Neha / Tilekar, Kalpana / Joshi, Hardik / Ramaa, C S

Iranian journal of pharmaceutical research : IJPR

2022 Volume 20, Issue 4, Page(s) 188–201

Abstract: Thiazolidinedione (TZD), being a privileged scaffold, has been known as a significant structural moiety of antidiabetic drugs. TZD has been known to improve glycaemic control in type 2 diabetes mellitus (T2DM) by increasing insulin sensitivity in the ... ...

Abstract	Thiazolidinedione (TZD), being a privileged scaffold, has been known as a significant structural moiety of antidiabetic drugs. TZD has been known to improve glycaemic control in type 2 diabetes mellitus (T2DM) by increasing insulin sensitivity in the body. A novel series of 5-benzylidene 2,4-thiazolidinedione derivatives were designed, synthesized (V1-V28), and structurally confirmed by different spectroscopic techniques such as FTIR,
Language	English
Publishing date	2022-02-10
Publishing country	Iran
Document type	Journal Article
ZDB-ID	2578271-X
ISSN	1735-0328 ; 1726-6890
ISSN	1735-0328 ; 1726-6890
DOI	10.22037/ijpr.2021.114969.15131
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Article: Development of 1,2,4-Triazole-5-Thione Derivatives as Potential Inhibitors of Enoyl Acyl Carrier Protein Reductase (InhA) in Tuberculosis.

Vora, Dhagash / Upadhyay, Neha / Tilekar, Kalpana / Jain, Viral / Ramaa, C S

Iranian journal of pharmaceutical research : IJPR

2020 Volume 18, Issue 4, Page(s) 1742–1758

Abstract: Tuberculosis (TB) ranks second, next to AIDS making it most formidable disease in the present age. One of the crucial enzymes involved in cell wall synthesis ... ...

Abstract	Tuberculosis (TB) ranks second, next to AIDS making it most formidable disease in the present age. One of the crucial enzymes involved in cell wall synthesis of
Language	English
Publishing date	2020-02-25
Publishing country	Iran
Document type	Journal Article
ZDB-ID	2578271-X
ISSN	1726-6890 ; 1735-0328 ; 1735-0328
ISSN (online)	1726-6890 ; 1735-0328
ISSN	1735-0328
DOI	10.22037/ijpr.2019.112039.13495
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Article ; Online: Power of two: combination of therapeutic approaches involving glucose transporter (GLUT) inhibitors to combat cancer.

Tilekar, Kalpana / Upadhyay, Neha / Iancu, Cristina V / Pokrovsky, Vadim / Choe, Jun-Yong / Ramaa, C S

Biochimica et biophysica acta. Reviews on cancer

2020 Volume 1874, Issue 2, Page(s) 188457

Abstract: Cancer research of the Warburg effect, a hallmark metabolic alteration in tumors, focused attention on glucose metabolism whose targeting uncovered several agents with promising anticancer effects at the preclinical level. These agents' monotherapy ... ...

Abstract	Cancer research of the Warburg effect, a hallmark metabolic alteration in tumors, focused attention on glucose metabolism whose targeting uncovered several agents with promising anticancer effects at the preclinical level. These agents' monotherapy points to their potential as adjuvant combination therapy to existing standard chemotherapy in human trials. Accordingly, several studies on combining glucose transporter (GLUT) inhibitors with chemotherapeutic agents, such as doxorubicin, paclitaxel, and cytarabine, showed synergistic or additive anticancer effects, reduced chemo-, radio-, and immuno-resistance, and reduced toxicity due to lowering the therapeutic doses required for desired chemotherapeutic effects, as compared with monotherapy. The combinations have been specifically effective in treating cancer glycolytic phenotypes, such as pancreatic and breast cancers. Even combining GLUT inhibitors with other glycolytic inhibitors and energy restriction mimetics seems worthwhile. Though combination clinical trials are in the early phase, initial results are intriguing. The various types of GLUTs, their role in cancer progression, GLUT inhibitors, and their anticancer mechanism of action have been reviewed several times. However, utilizing GLUT inhibitors as combination therapeutics has received little attention. We consider GLUT inhibitors agents that directly affect glucose transporters by binding to them or indirectly alter glucose transport by changing the transporters' expression level. This review mainly focuses on summarizing the effects of various combinations of GLUT inhibitors with other anticancer agents and providing a perspective on the current status.
MeSH term(s)	Animals ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Clinical Trials as Topic ; Drug Synergism ; Glucose Transport Proteins, Facilitative/antagonists & inhibitors ; Glycolysis/drug effects ; Humans ; Molecular Structure ; Neoplasms/drug therapy ; Neoplasms/metabolism
Chemical Substances	Antineoplastic Agents ; Glucose Transport Proteins, Facilitative
Language	English
Publishing date	2020-10-21
Publishing country	Netherlands
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	2918802-7
ISSN	1879-2561 ; 0304-419X
ISSN (online)	1879-2561
ISSN	0304-419X
DOI	10.1016/j.bbcan.2020.188457
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Article ; Online: Benzylidene thiazolidinediones: Synthesis, in vitro investigations of antiproliferative mechanisms and in vivo efficacy determination in combination with Imatinib.

Joshi, Hardik / Patil, Vijay / Tilekar, Kalpana / Upadhyay, Neha / Gota, Vikram / Ramaa, C S

Bioorganic & medicinal chemistry letters

2020 Volume 30, Issue 23, Page(s) 127561

Abstract: Thiazolidinedione (TZD) has been an interesting scaffold due to its proven antidiabetic activity and encouraging findings in anticancer drug discovery. We synthesised benzylidene thiazolidinedione derivatives which exhibited excellent antiproliferative ... ...

Abstract	Thiazolidinedione (TZD) has been an interesting scaffold due to its proven antidiabetic activity and encouraging findings in anticancer drug discovery. We synthesised benzylidene thiazolidinedione derivatives which exhibited excellent antiproliferative effects in chronic myeloid leukemic cells K562 and the most active compounds 3t and 3x had GI
MeSH term(s)	Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/therapeutic use ; Antineoplastic Agents/toxicity ; Antineoplastic Combined Chemotherapy Protocols ; Apoptosis/drug effects ; Benzylidene Compounds/chemical synthesis ; Benzylidene Compounds/therapeutic use ; Benzylidene Compounds/toxicity ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Female ; G1 Phase Cell Cycle Checkpoints/drug effects ; Humans ; Imatinib Mesylate/therapeutic use ; Male ; Mice, Nude ; Molecular Structure ; Neoplasms/drug therapy ; Structure-Activity Relationship ; Thiazolidinediones/chemical synthesis ; Thiazolidinediones/therapeutic use ; Thiazolidinediones/toxicity ; Xenograft Model Antitumor Assays
Chemical Substances	Antineoplastic Agents ; Benzylidene Compounds ; Thiazolidinediones ; Imatinib Mesylate (8A1O1M485B)
Language	English
Publishing date	2020-09-19
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2020.127561
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Article ; Online: Assorted Applications of N-substituted-2,4-thiazolidinediones in Various Pathological Conditions.

Gupta, Rakesh / Joshi, Hardik / Ramaa, C S

Mini reviews in medicinal chemistry

2017 Volume 19, Issue 4, Page(s) 346–360

Abstract: Thiazolidine-2,4-dione (TZD) is one of the most frequently encountered heterocyclic rings which has been implicated in design and synthesis of entities for various pathogenic conditions including cancer. Since its discovery various substitutions at 5th ... ...

Abstract	Thiazolidine-2,4-dione (TZD) is one of the most frequently encountered heterocyclic rings which has been implicated in design and synthesis of entities for various pathogenic conditions including cancer. Since its discovery various substitutions at 5th position have been carried out and reviewed. Various substitutions at 5th position have led to generation of glitazones, whose target peroxisome proliferating activated receptor γ (PPARγ) was found decade after their discovery. Acidic hydrogen (-NH) of TZD is a prime pharmacophoric requirement for the activation of PPARγ. However, advanced in-silico techniques have helped to design compounds bearing substitutions at both methylene and -NH group of TZD, targeting range of enzymes involved in various pathological conditions viz., diabetes, hyperlipidemia, infectious disease, inflammation and cancer. The promising activities shown by methylene and N-substituted TZDs in above mentioned therapeutic areas, prompted us to collate the information which would help researchers to alter the structure of existing ligands and to design new TZD derivatives with better safety and efficacy profiles.
MeSH term(s)	Animals ; Disease ; Drug Discovery/methods ; Humans ; Nitrogen/chemistry ; Safety ; Structure-Activity Relationship ; Thiazolidinediones/adverse effects ; Thiazolidinediones/chemistry ; Thiazolidinediones/pharmacology
Chemical Substances	Thiazolidinediones ; 2,4-thiazolidinedione (AA68LXK93C) ; Nitrogen (N762921K75)
Language	English
Publishing date	2017-11-30
Publishing country	Netherlands
Document type	Journal Article ; Review
ZDB-ID	2104081-3
ISSN	1875-5607 ; 1389-5575
ISSN (online)	1875-5607
ISSN	1389-5575
DOI	10.2174/1389557518666171129163426
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Article ; Online: Novel Anthraquinone Derivatives as Dual Inhibitors of Topoisomerase 2 and Casein Kinase 2: In Silico Studies, Synthesis and Biological Evaluation on Leukemic Cell Lines.

Kabir, Abbas / Tilekar, Kalpana / Upadhyay, Neha / Ramaa, C S

Anti-cancer agents in medicinal chemistry

2018 Volume 18, Issue 11, Page(s) 1551–1562

Abstract: Background: Cancer being a complex disease, single targeting agents remain unsuccessful. This calls for "multiple targeting", wherein a single drug is so designed that it will modulate the activity of multiple protein targets. Topoisomerase 2 (Top2) ... ...

Abstract	Background: Cancer being a complex disease, single targeting agents remain unsuccessful. This calls for "multiple targeting", wherein a single drug is so designed that it will modulate the activity of multiple protein targets. Topoisomerase 2 (Top2) helps in removing DNA tangles and super-coiling during cellular replication, Casein Kinase 2 (CK2) is involved in the phosphorylation of a multitude of protein targets. Thus, in the present work, we have tried to develop dual inhibitors of Top2 and CK2. Objective: With this view, in the present work, 2 human proteins, Top2 and CK2 have been targeted to achieve the anti-proliferative effects. Methods: Novel 1-acetylamidoanthraquinone (3a-3y) derivatives were designed, synthesized and their structures were elucidated by analytical and spectral characterization techniques (FTIR, 1H NMR, 13C NMR and Mass Spectroscopy). The synthesized compounds were then subjected to evaluation of cytotoxic potential by the Sulforhodamine B (SRB) protein assay, using HL60 and K562 cell lines. Ten compounds were analyzed for Top2, CK2 enzyme inhibitory potential. Further, top three compounds were subjected to cell cycle analysis. Results: The compounds 3a to 3c, 3e, 3f, 3i to 3p, 3t and 3x showed excellent cytotoxic activity to HL-60 cell line indicating their high anti-proliferative potential in AML. The compounds 3a to 3c, 3e, 3f, 3i to 3p and 3y have shown good to moderate activity on K-562 cell line. Compounds 3e, 3f, 3i, 3x and 3y were found more cytotoxic than standard doxorubicin. In cell cycle analysis, the cells (79-85%) were found to arrest in the G0/G1 phase. Conclusion: We have successfully designed, synthesized, purified and structurally characterized 1- acetylamidoanthraquinone derivatives. Even though our compounds need design optimization to further increase enzyme inhibition, their overall anti-proliferative effects were found to be encouraging.
MeSH term(s)	Anthraquinones/chemical synthesis ; Anthraquinones/chemistry ; Anthraquinones/pharmacology ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Casein Kinase II/antagonists & inhibitors ; Casein Kinase II/metabolism ; Cell Proliferation/drug effects ; Computer Simulation ; DNA Topoisomerases, Type II/metabolism ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; HL-60 Cells ; Humans ; K562 Cells ; Molecular Docking Simulation ; Molecular Structure ; Structure-Activity Relationship
Chemical Substances	Anthraquinones ; Antineoplastic Agents ; Enzyme Inhibitors ; Casein Kinase II (EC 2.7.11.1) ; DNA Topoisomerases, Type II (EC 5.99.1.3)
Language	English
Publishing date	2018-04-12
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	2217610-X
ISSN	1875-5992 ; 1871-5206
ISSN (online)	1875-5992
ISSN	1871-5206
DOI	10.2174/1871520618666180423111309
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Article ; Online: Double-edged Swords: Diaryl pyrazoline thiazolidinediones synchronously targeting cancer epigenetics and angiogenesis.

Upadhyay, Neha / Tilekar, Kalpana / Safuan, Sabreena / Kumar, Alan P / Schweipert, Markus / Meyer-Almes, Franz-Josef / Ramaa, C S

Bioorganic chemistry

2021 Volume 116, Page(s) 105350

Abstract: In the present study, two novel series of compounds incorporating naphthyl and pyridyl linker were synthesized and biological assays revealed 5-((6-(2-(5-(2-chlorophenyl)-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethoxy) naphthalene-2-yl) ... ...

Abstract	In the present study, two novel series of compounds incorporating naphthyl and pyridyl linker were synthesized and biological assays revealed 5-((6-(2-(5-(2-chlorophenyl)-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethoxy) naphthalene-2-yl)methylene)thiazolidine-2,4-dione (14b) as the most potent dual inhibitors of vascular endothelial growth factors receptor-2 (VEGFR-2) and histone deacetylase 4 (HDAC4). Compounds 13b, 14b, 17f, and 21f were found to stabilize HDAC4; where, pyridyl linker swords were endowed with higher stabilization effects than naphthyl linker. Also, 13b and 14b showed best inhibitory activity on VEGFR-2 as compared to others. Compound 14b was most potent as evident by in-vitro and in-vivo biological assessments. It displayed anti-angiogenic potential by inhibiting endothelial cell proliferation, migration, tube formation and also suppressed new capillary formation in the growing chick chorioallantoic membranes (CAMs). It showed selectivity and potency towards HDAC4 as compared to other HDAC isoforms. Compound 14b (25 mg/kg, i.p.) also indicated exceptional antitumor efficacy on in-vivo animal xenograft model of human colorectal adenocarcinoma (HT-29). The mechanism of action of 14b was also confirmed by western blot.
MeSH term(s)	Angiogenesis Inhibitors/chemical synthesis ; Angiogenesis Inhibitors/chemistry ; Angiogenesis Inhibitors/pharmacology ; Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Cell Line, Tumor ; Cell Movement/drug effects ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Histone Deacetylase Inhibitors/chemical synthesis ; Histone Deacetylase Inhibitors/chemistry ; Histone Deacetylase Inhibitors/pharmacology ; Histone Deacetylases/metabolism ; Humans ; Mice ; Molecular Structure ; Neoplasms, Experimental/drug therapy ; Neoplasms, Experimental/metabolism ; Neoplasms, Experimental/pathology ; Neovascularization, Pathologic/drug therapy ; Protein Kinase Inhibitors/chemical synthesis ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/pharmacology ; Pyrazoles/chemical synthesis ; Pyrazoles/chemistry ; Pyrazoles/pharmacology ; Repressor Proteins/antagonists & inhibitors ; Repressor Proteins/metabolism ; Structure-Activity Relationship ; Thiazolidinediones/chemical synthesis ; Thiazolidinediones/chemistry ; Thiazolidinediones/pharmacology ; Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors ; Vascular Endothelial Growth Factor Receptor-2/metabolism
Chemical Substances	Angiogenesis Inhibitors ; Antineoplastic Agents ; Histone Deacetylase Inhibitors ; Protein Kinase Inhibitors ; Pyrazoles ; Repressor Proteins ; Thiazolidinediones ; KDR protein, human (EC 2.7.10.1) ; Vascular Endothelial Growth Factor Receptor-2 (EC 2.7.10.1) ; HDAC4 protein, human (EC 3.5.1.98) ; Histone Deacetylases (EC 3.5.1.98)
Language	English
Publishing date	2021-09-11
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	120080-x
ISSN	1090-2120 ; 0045-2068
ISSN (online)	1090-2120
ISSN	0045-2068
DOI	10.1016/j.bioorg.2021.105350
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Article ; Online: Development and investigation of thiazolidinedione and pyrazoline compounds as antiangiogenic weapons targeting VEGFR-2.

Upadhyay, Neha / Tilekar, Kalpana / Safuan, Sabreena / Kumar, Alan P / Schweipert, Markus / Meyer-Almes, Franz-Josef / Ramaa, C S

Future medicinal chemistry

2021 Volume 13, Issue 22, Page(s) 1963–1986

Abstract: Background: ...

Abstract	Background:
MeSH term(s)	Angiogenesis Inhibitors/chemical synthesis ; Angiogenesis Inhibitors/chemistry ; Angiogenesis Inhibitors/pharmacology ; Drug Development ; Humans ; Neovascularization, Physiologic/drug effects ; Protein Kinase Inhibitors/chemical synthesis ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/pharmacology ; Pyrazoles/chemical synthesis ; Pyrazoles/chemistry ; Pyrazoles/pharmacology ; Thiazolidinediones/chemical synthesis ; Thiazolidinediones/chemistry ; Thiazolidinediones/pharmacology ; Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors ; Vascular Endothelial Growth Factor Receptor-2/metabolism
Chemical Substances	Angiogenesis Inhibitors ; Protein Kinase Inhibitors ; Pyrazoles ; Thiazolidinediones ; KDR protein, human (EC 2.7.10.1) ; Vascular Endothelial Growth Factor Receptor-2 (EC 2.7.10.1)
Language	English
Publishing date	2021-09-28
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1756-8927
ISSN (online)	1756-8927
DOI	10.4155/fmc-2021-0139
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Article ; Online: Hydroxy Cinnamic Acid Derivatives as Partial PPARγ Agonists: In silico Studies, Synthesis and Biological Characterization Against Chronic Myeloid Leukemia Cell Line (K562).

Joshi, Hardik / Marulkar, Kavita / Gota, Vikram / Ramaa, C S

Anti-cancer agents in medicinal chemistry

2017 Volume 17, Issue 4, Page(s) 524–541

Abstract: Background: Peroxisome proliferator-activated receptor gamma (PPARγ) is a nuclear receptor that regulates the expression of many genes relevant to carcinogenesis. By analogy to selective estrogen receptor modulator for treatment of cancer, selective or ... ...

Abstract	Background: Peroxisome proliferator-activated receptor gamma (PPARγ) is a nuclear receptor that regulates the expression of many genes relevant to carcinogenesis. By analogy to selective estrogen receptor modulator for treatment of cancer, selective or partial PPARγ agonists are considered clinically important for chemotherapy of cancer. Objective: In this study we have rationally modified the structure of existing p-coumaric acid and ferulic acid, which would selectively activate PPARγ and exert their anti-proliferative effect at lower dose as compared to natural phytoconstituents. Method: A series of p-coumaric (3a-3y) and ferulic acid (4a-4y) derivatives were designed as docked and virtually studied for their molecular properties using suitable software. Synthesized derivatives were assessed to check their effect on non-transformed hepatocytes using MTT assay. The final products, 3a-3y and 4a-4y, substituted 4- hydroxycinnamic acid derivatives and ferulic acid derivatives respectively were synthesized by stirring compound 1a or 1b with compounds 2a-2y (molar ratio- 1:2) for 24 hours, in presence of K2CO3, using dimethyl formamide (DMF) as the solvent. Synthesized molecules were characterized by 1HNMR, 13C NMR, Mass and elemental analysis. Synthesized molecules were studied for their antiproliferative activity by SRB assay. Compounds were screened further evaluated for PPARγ activating assay, cell cycle analysis (propidium iodide) and westernblot analysis. Results: Molecules 3c, 3m, 4c and 4m were found to have GI50 value less than 50μM. These molecules were found to block G0/G1 phase of cell cycle in dose dependent manner. Western blot analysis revealed that these molecules inhibit proliferating cell nuclear antigen (PCNA) and cyclin D1 expression. Conclusion: Collectively, these results suggest that these molecules could play a role as a novel therapeutic strategy for chronic myeloid leukemia.
MeSH term(s)	Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Cell Cycle/drug effects ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Computer Simulation ; Coumaric Acids/chemical synthesis ; Coumaric Acids/chemistry ; Coumaric Acids/pharmacology ; Dose-Response Relationship, Drug ; Drug Partial Agonism ; Drug Screening Assays, Antitumor ; Humans ; K562 Cells ; Leukemia, Myelogenous, Chronic, BCR-ABL Positive/drug therapy ; Leukemia, Myelogenous, Chronic, BCR-ABL Positive/pathology ; Molecular Structure ; PPAR alpha/agonists ; Structure-Activity Relationship
Chemical Substances	Antineoplastic Agents ; Coumaric Acids ; PPAR alpha ; ferulic acid (AVM951ZWST)
Language	English
Publishing date	2017
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	2217610-X
ISSN	1875-5992 ; 1871-5206
ISSN (online)	1875-5992
ISSN	1871-5206
DOI	10.2174/1871520616666160607010156
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