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Article ; Online: Noncoding RNAs as regulators of STAT3 pathway in gastrointestinal cancers: Roles in cancer progression and therapeutic response.

Ashrafizadeh, Milad / Mohan, Chakrabhavi D / Rangappa, Shobith / Zarrabi, Ali / Hushmandi, Kiavash / Kumar, Alan Prem / Sethi, Gautam / Rangappa, Kanchugarakoppal S

Medicinal research reviews

2023 Volume 43, Issue 5, Page(s) 1263–1321

Abstract: Gastrointestinal (GI) tumors (cancers of the esophagus, gastric, liver, pancreas, colon, and rectum) contribute to a large number of deaths worldwide. STAT3 is an oncogenic transcription factor that promotes the transcription of genes associated with ... ...

Abstract	Gastrointestinal (GI) tumors (cancers of the esophagus, gastric, liver, pancreas, colon, and rectum) contribute to a large number of deaths worldwide. STAT3 is an oncogenic transcription factor that promotes the transcription of genes associated with proliferation, antiapoptosis, survival, and metastasis. STAT3 is overactivated in many human malignancies including GI tumors which accelerates tumor progression, metastasis, and drug resistance. Research in recent years demonstrated that noncoding RNAs (ncRNAs) play a major role in the regulation of many signaling pathways including the STAT3 pathway. The major types of endogenous ncRNAs that are being extensively studied in oncology are microRNAs, long noncoding RNAs, and circular RNAs. These ncRNAs can either be tumor-promoters or tumor-suppressors and each one of them imparts their activity via different mechanisms. The STAT3 pathway is also tightly modulated by ncRNAs. In this article, we have elaborated on the tumor-promoting role of STAT3 signaling in GI tumors. Subsequently, we have comprehensively discussed the oncogenic as well as tumor suppressor functions and mechanism of action of ncRNAs that are known to modulate STAT3 signaling in GI cancers.
MeSH term(s)	Humans ; MicroRNAs/genetics ; RNA, Long Noncoding/genetics ; Gastrointestinal Neoplasms/genetics ; Signal Transduction ; STAT3 Transcription Factor/genetics ; STAT3 Transcription Factor/metabolism
Chemical Substances	MicroRNAs ; RNA, Long Noncoding ; STAT3 protein, human ; STAT3 Transcription Factor
Language	English
Publishing date	2023-03-23
Publishing country	United States
Document type	Journal Article ; Review ; Research Support, Non-U.S. Gov't
ZDB-ID	603210-2
ISSN	1098-1128 ; 0198-6325
ISSN (online)	1098-1128
ISSN	0198-6325
DOI	10.1002/med.21950
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Zs.A 1764: Show issues

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Article ; Online: A new triazolyl-indolo-quinoxaline induces apoptosis in gastric cancer cells by abrogating the STAT3/5 pathway through upregulation of PTPεC.

Suresh, Rajaghatta N / Jung, Young Y / Mohan, Chakrabhavi D / Gowda, Shalini V / Harsha, Kachigere B / Mantelingu, Kempegowda / Sethi, Gautam / Ahn, Kwang S / Rangappa, Kanchugarakoppal S

Drug development research

2023 Volume 84, Issue 8, Page(s) 1724–1738

Abstract: Signal transducer and activator of transcription 3 (STAT3) and STAT5 are the transcription factors that have been studied extensively in relevance to the development of cancers in humans. Suppression of either STAT3 or STAT5-mediated signaling events has ...

Abstract	Signal transducer and activator of transcription 3 (STAT3) and STAT5 are the transcription factors that have been studied extensively in relevance to the development of cancers in humans. Suppression of either STAT3 or STAT5-mediated signaling events has been demonstrated to be effective in inducing cytotoxicity in cancer cells. Herein, new hybrids of triazolyl-indolo-quinoxaline are synthesized and examined for their effect on the activation of STAT3 and STAT5 pathways in gastric cancer (GC) cells. Among the newly synthesized compounds, 2,3-difluoro-6-((1-(3-fluorophenyl)-1H-1,2,3-triazol-5-yl)methyl)-6H-indolo[2,3-b]quinoxaline (DTI) displayed selective cytotoxicity against GC cells over their normal counterpart. Flow cytometric analysis, annexin-V-fluorescein isothiocyanate staining, terminal deoxynucleotidyl transferase dUTP nick end labeling assay, live and dead assay, and caspase activation experiments suggested DTI as a potent inducer of apoptosis. The mechanistic approach revealed that DTI imparts cytotoxicity via downregulating the phosphorylation of STAT3
MeSH term(s)	Humans ; Signal Transduction ; STAT5 Transcription Factor/metabolism ; STAT5 Transcription Factor/pharmacology ; STAT3 Transcription Factor/metabolism ; DNA-Binding Proteins/metabolism ; Trans-Activators ; Stomach Neoplasms ; Up-Regulation ; Quinoxalines/pharmacology ; Janus Kinases/metabolism ; Janus Kinases/pharmacology ; STAT Transcription Factors/metabolism ; STAT Transcription Factors/pharmacology ; Phosphorylation ; Apoptosis
Chemical Substances	STAT5 Transcription Factor ; STAT3 Transcription Factor ; DNA-Binding Proteins ; Trans-Activators ; Quinoxalines ; Janus Kinases (EC 2.7.10.2) ; STAT Transcription Factors ; STAT3 protein, human
Language	English
Publishing date	2023-09-27
Publishing country	United States
Document type	Journal Article
ZDB-ID	604587-x
ISSN	1098-2299 ; 0272-4391
ISSN (online)	1098-2299
ISSN	0272-4391
DOI	10.1002/ddr.22117
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: Synthesis, Cytotoxic and Heparanase Inhibition Studies of 5-oxo-1-arylpyrrolidine-3- carboxamides of Hydrazides and 4-amino-5-aryl-4H-1,2,4-triazole-3-thiol.

Hari, Swetha / Swaroop, Toreshettahally R / Preetham, Habbanakuppe D / Mohan, Chakrabhavi D / Muddegowda, Umashakara / Basappa, Salundi / Vlodavsky, Israel / Sethi, Gautam / Rangappa, Kanchugarakoppal S

Current organic synthesis

2019 Volume 17, Issue 3, Page(s) 243–250

Abstract: Design of chemically novel, biologically potent small heterocyclic molecules with anticancer activities, which targets the enzyme heparanase has gained prominent clinical interest. We have synthesized a novel class of carboxamide derivatives by coupling ... ...

Abstract	Design of chemically novel, biologically potent small heterocyclic molecules with anticancer activities, which targets the enzyme heparanase has gained prominent clinical interest. We have synthesized a novel class of carboxamide derivatives by coupling various substituted aromatic acid hydrazides and triazoleamine with pyrrolidine carboxylic acid by using coupling agents. The synthesized compounds are characterized by spectroscopic techniques such as FT-IR, HRMS and NMR. These compounds are investigated for cytotoxicity on different cancer cell lines and heparanase inhibitory activity. Most of them showed moderate heparanase inhibitory activity and good cytotoxicity.
MeSH term(s)	Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/pharmacology ; Cell Line, Tumor ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/pharmacology ; Glucuronidase/antagonists & inhibitors ; Humans ; Hydrazines/chemical synthesis ; Hydrazines/pharmacology ; Mice ; Pyrrolidinones/chemical synthesis ; Pyrrolidinones/pharmacology ; Triazoles/chemical synthesis ; Triazoles/pharmacology
Chemical Substances	Antineoplastic Agents ; Enzyme Inhibitors ; Hydrazines ; Pyrrolidinones ; Triazoles ; heparanase (EC 3.2.1.-) ; Glucuronidase (EC 3.2.1.31)
Language	English
Publishing date	2019-05-06
Publishing country	United Arab Emirates
Document type	Letter ; Research Support, Non-U.S. Gov't
ISSN	1570-1794
ISSN	1570-1794
DOI	10.2174/1570179417666200225123329
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Metabolite Profiling of

Siddaiah, Chandranayaka / Kumar Bm, Anil / Deepak, Saligrama Adavigowda / Lateef, Syed Salman / Nagpal, Saurabh / Rangappa, Kanchugarakoppal S / Mohan, Chakrabhavi D / Rangappa, Shobith / Kumar S, Madan / Sharma, Minaxi / Gupta, Vijai Kumar

Cells

2020 Volume 10, Issue 1

Abstract: There is an urge for traditional herbal remedies as an alternative to modern medicine in treating several ailments. ...

Abstract	There is an urge for traditional herbal remedies as an alternative to modern medicine in treating several ailments.
MeSH term(s)	Alangiaceae/chemistry ; Alangiaceae/metabolism ; Chromatography, High Pressure Liquid/methods ; Metabolome ; Plant Bark/chemistry ; Plant Bark/metabolism ; Plant Extracts/chemistry ; Tandem Mass Spectrometry/methods
Chemical Substances	Plant Extracts
Language	English
Publishing date	2020-12-22
Publishing country	Switzerland
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2661518-6
ISSN	2073-4409 ; 2073-4409
ISSN (online)	2073-4409
ISSN	2073-4409
DOI	10.3390/cells10010001
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Article: Endophytic Fungi-Alternative Sources of Cytotoxic Compounds: A Review.

Uzma, Fazilath / Mohan, Chakrabhavi D / Hashem, Abeer / Konappa, Narasimha M / Rangappa, Shobith / Kamath, Praveen V / Singh, Bhim P / Mudili, Venkataramana / Gupta, Vijai K / Siddaiah, Chandra N / Chowdappa, Srinivas / Alqarawi, Abdulaziz A / Abd Allah, Elsayed F

Frontiers in pharmacology

2018 Volume 9, Page(s) 309

Abstract: Cancer is a major cause of death worldwide, with an increasing number of cases being reported annually. The elevated rate of mortality necessitates a global challenge to explore newer sources of anticancer drugs. Recent advancements in cancer treatment ... ...

Abstract	Cancer is a major cause of death worldwide, with an increasing number of cases being reported annually. The elevated rate of mortality necessitates a global challenge to explore newer sources of anticancer drugs. Recent advancements in cancer treatment involve the discovery and development of new and improved chemotherapeutics derived from natural or synthetic sources. Natural sources offer the potential of finding new structural classes with unique bioactivities for cancer therapy. Endophytic fungi represent a rich source of bioactive metabolites that can be manipulated to produce desirable novel analogs for chemotherapy. This review offers a current and integrative account of clinically used anticancer drugs such as taxol, podophyllotoxin, camptothecin, and vinca alkaloids in terms of their mechanism of action, isolation from endophytic fungi and their characterization, yield obtained, and fungal strain improvement strategies. It also covers recent literature on endophytic fungal metabolites from terrestrial, mangrove, and marine sources as potential anticancer agents and emphasizes the findings for cytotoxic bioactive compounds tested against specific cancer cell lines.
Language	English
Publishing date	2018-04-26
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2587355-6
ISSN	1663-9812
ISSN	1663-9812
DOI	10.3389/fphar.2018.00309
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Article ; Online: A new ibuprofen derivative inhibits platelet aggregation and ROS mediated platelet apoptosis.

Rakesh, Kodagahalli S / Jagadish, Swamy / Vinayaka, Ajjampura C / Hemshekhar, Mahadevappa / Paul, Manoj / Thushara, Ram M / Sundaram, Mahalingam S / Swaroop, Toreshettahally R / Mohan, Chakrabhavi D / Basappa / Sadashiva, Marilinganadoddi P / Kemparaju, Kempaiah / Girish, Kesturu S / Rangappa, Kanchugarakoppal S

PloS one

2014 Volume 9, Issue 9, Page(s) e107182

Abstract: Thrombocytopenia is a serious issue connected with the pathogenesis of several human diseases including chronic inflammation, arthritis, Alzheimer's disease, cardiovascular diseases (CVDs) and other oxidative stress-associated pathologies. The ... ...

Abstract	Thrombocytopenia is a serious issue connected with the pathogenesis of several human diseases including chronic inflammation, arthritis, Alzheimer's disease, cardiovascular diseases (CVDs) and other oxidative stress-associated pathologies. The indiscriminate use of antibiotics and other biological drugs are reported to result in thrombocytopenia, which is often neglected during the treatment regime. In addition, augmented oxidative stress induced by drugs and pathological conditions has also been shown to induce thrombocytopenia, which seems to be the most obvious consequence of elevated rate of platelet apoptosis. Thus, blocking oxidative stress-induced platelet apoptosis would be of prime importance in order to negotiate thrombocytopenia and associated human pathologies. The current study presents the synthesis and platelet protective nature of novel ibuprofen derivatives. The potent anti-oxidant ibuprofen derivative 4f was selected for the study and the platelet protective efficacy and platelet aggregation inhibitory property has been demonstrated. The compound 4f dose dependently mitigates the oxidative stress-induced platelet apoptosis in both platelet rich plasma and washed platelets. The platelet protective nature of compound 4f was determined by assessing various apoptotic markers such as ROS generation, cytosolic Ca2+ levels, PS externalization, cytochrome C translocation, Caspase activation, mitochondrial membrane depolarization, cytotoxicity, LDH leakage and tyrosine phosphorylation of cytosolic proteins. Furthermore, compound 4f dose dependently ameliorated agonist induced platelet aggregation. Therefore, compound 4f can be estimated as a potential candidate in the treatment regime of pathological disorders associated with platelet activation and apoptosis. In addition, compound 4f can be used as an auxiliary therapeutic agent in pathologies associated with thrombocytopenia.
MeSH term(s)	Apoptosis/drug effects ; Blood Platelets/cytology ; Blood Platelets/drug effects ; Blood Platelets/metabolism ; Dose-Response Relationship, Drug ; Humans ; Ibuprofen/analogs & derivatives ; Ibuprofen/chemistry ; Ibuprofen/pharmacology ; Oxidative Stress/drug effects ; Platelet Aggregation/drug effects ; Reactive Oxygen Species/metabolism
Chemical Substances	Reactive Oxygen Species ; Ibuprofen (WK2XYI10QM)
Language	English
Publishing date	2014-09-19
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1932-6203
ISSN (online)	1932-6203
DOI	10.1371/journal.pone.0107182
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Synthesis and characterization of novel 2-amino-chromene-nitriles that target Bcl-2 in acute myeloid leukemia cell lines.

Keerthy, Hosadurga K / Garg, Manoj / Mohan, Chakrabhavi D / Madan, Vikas / Kanojia, Deepika / Shobith, Rangappa / Nanjundaswamy, Shivananju / Mason, Daniel J / Bender, Andreas / Basappa / Rangappa, Kanchugarakoppal S / Koeffler, H Phillip

PloS one

2014 Volume 9, Issue 9, Page(s) e107118

Abstract: The anti-apoptotic protein Bcl-2 is a well-known and attractive therapeutic target for cancer. In the present study the solution-phase T3P-DMSO mediated efficient synthesis of 2-amino-chromene-3-carbonitriles from alcohols, malanonitrile and phenols is ... ...

Abstract	The anti-apoptotic protein Bcl-2 is a well-known and attractive therapeutic target for cancer. In the present study the solution-phase T3P-DMSO mediated efficient synthesis of 2-amino-chromene-3-carbonitriles from alcohols, malanonitrile and phenols is reported. These novel 2-amino-chromene-3-carbonitriles showed cytotoxicity in human acute myeloid leukemia (AML) cell lines. Compound 4 g was found to be the most bioactive, decreasing growth and increasing apoptosis of AML cells. Moreover, compound 4 g (at a concentration of 5 µM) increased the G2/M and sub-G1 (apoptosis) phases of AML cells. The AML cells treated with compound 4 g exhibited decreased levels of Bcl-2 and increased levels of caspase-9. In silico molecular interaction analysis showed that compound 4 g shared a similar global binding motif with navitoclax (another small molecule that binds Bcl-2), however compound 4 g occupies a smaller volume within the P2 hot spot of Bcl-2. The intermolecular π-stacking interaction, direct electrostatic interactions, and docking energy predicted for 4 g in complex with Bcl-2 suggest a strong affinity of the complex, rendering 4 g as a promising Bcl-2 inhibitor for evaluation as a new anticancer agent.
MeSH term(s)	Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/pharmacology ; Benzopyrans/chemical synthesis ; Benzopyrans/pharmacology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Drug Screening Assays, Antitumor ; Humans ; Inhibitory Concentration 50 ; Leukemia, Myeloid, Acute/drug therapy ; Molecular Docking Simulation ; Molecular Targeted Therapy ; Nitriles/chemical synthesis ; Nitriles/pharmacology ; Proto-Oncogene Proteins c-bcl-2/antagonists & inhibitors ; Proto-Oncogene Proteins c-bcl-2/chemistry
Chemical Substances	Antineoplastic Agents ; BCL2 protein, human ; Benzopyrans ; Nitriles ; Proto-Oncogene Proteins c-bcl-2
Language	English
Publishing date	2014-09-30
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1932-6203
ISSN (online)	1932-6203
DOI	10.1371/journal.pone.0107118
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Anti-Cancer Activity of 2,4-Disubstituted Thiophene Derivatives: Dual Inhibitors of Lipoxygenase and Cyclooxygenase.

Rakesh, Kodagahalli S / Jagadish, Swamy / Swaroop, Toreshettahally R / Mohan, Chakrabhavi D / Ashwini, Nanjundaswamy / Harsha, Kachigere B / Zameer, Farhan / Girish, Kesturu S / Rangappa, Kanchugarakoppal S

Medicinal chemistry (Shariqah (United Arab Emirates))

2014 Volume 11, Issue 5, Page(s) 462–472

Abstract: 2,4-Disubstituted thiophene derivatives were synthesized and assessed for antiinflammatory and anti-cancer activities by targeting two important enzymes of the arachidonic acid metabolism. Both lipoxygenase and cyclooxygenase enzymes play vital role in ... ...

Abstract	2,4-Disubstituted thiophene derivatives were synthesized and assessed for antiinflammatory and anti-cancer activities by targeting two important enzymes of the arachidonic acid metabolism. Both lipoxygenase and cyclooxygenase enzymes play vital role in chronic inflammation and carcinogenesis. Previous studies have proved that COX-2 and 5-LOX are highly activated in various types of cancers; hence inhibition of these clinically important enzymes constitutes the essential criterion for the suppression of tumor progression and metastasis. Among the tested derivatives, 2d and 2g compounds emerged as potent inhibitors of lipoxygenase and cyclooxygenase enzymes. The potent inhibitor of cyclooxygenase was further tested for in vitro cytotoxicity on cervical cancer (HeLa) cells and in vivo tumor model studies using EAT bearing mice where 2-(3,4,5- trimethoxyphenyl)-4-(N-methylindol-3-yl) thiophene (2g) showed eloquent activity. Further, in silico modeling results confirmed the active catalytic ligand binding pockets, which is evident from higher atomic contact energy values of 2d and 2g than compared to standard drug. Thus, 2g may find better application in management of inflammation and in proapoptotic therapeutic engineering.
MeSH term(s)	Animals ; Anti-Inflammatory Agents/chemical synthesis ; Anti-Inflammatory Agents/chemistry ; Anti-Inflammatory Agents/pharmacology ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Apoptosis/drug effects ; Cell Survival/drug effects ; Cyclooxygenase Inhibitors/chemical synthesis ; Cyclooxygenase Inhibitors/chemistry ; Cyclooxygenase Inhibitors/pharmacology ; Drug Screening Assays, Antitumor ; Enzyme Activation/drug effects ; HeLa Cells ; Humans ; Inhibitory Concentration 50 ; Lipoxygenase Inhibitors/chemical synthesis ; Lipoxygenase Inhibitors/chemistry ; Lipoxygenase Inhibitors/pharmacology ; Mice ; Models, Molecular ; Molecular Docking Simulation ; Thiophenes/chemical synthesis ; Thiophenes/chemistry ; Thiophenes/pharmacology
Chemical Substances	Anti-Inflammatory Agents ; Antineoplastic Agents ; Cyclooxygenase Inhibitors ; Lipoxygenase Inhibitors ; Thiophenes
Language	English
Publishing date	2014-05-01
Publishing country	Netherlands
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1875-6638
ISSN (online)	1875-6638
DOI	10.2174/1573406411666141210141918
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Noncoding RNAs as regulators of STAT3 pathway in gastrointestinal cancers: Roles in cancer progression and therapeutic response.

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Article ; Online: A new triazolyl-indolo-quinoxaline induces apoptosis in gastric cancer cells by abrogating the STAT3/5 pathway through upregulation of PTPεC.

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Article: Synthesis, Cytotoxic and Heparanase Inhibition Studies of 5-oxo-1-arylpyrrolidine-3- carboxamides of Hydrazides and 4-amino-5-aryl-4H-1,2,4-triazole-3-thiol.

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Article ; Online: Metabolite Profiling of

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Article: Endophytic Fungi-Alternative Sources of Cytotoxic Compounds: A Review.

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Article ; Online: A new ibuprofen derivative inhibits platelet aggregation and ROS mediated platelet apoptosis.

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Article ; Online: Synthesis and characterization of novel 2-amino-chromene-nitriles that target Bcl-2 in acute myeloid leukemia cell lines.

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Article ; Online: Anti-Cancer Activity of 2,4-Disubstituted Thiophene Derivatives: Dual Inhibitors of Lipoxygenase and Cyclooxygenase.

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