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  1. Article ; Online: Gallic Acid Derived 1, 2-Diarylindole as a Potential Antifungal Agent against Candida Strain.

    Kurmi, Alka / Singh, Akash Pratap / Gautam, Yashveer / Singh, Nandan / Tripathi, Alok / Negi, Arvind Singh / Gautam, Hemant K / Pal, Anirban / Saikia, Dharmendra

    Current topics in medicinal chemistry

    2024  

    Abstract: Background: In recent decades, Candida albicans has become a serious issue for public health. The worldwide rapid rise in drug resistance to conventional therapies is the main contributing reason. Moreover, because of their potent activity at low ... ...

    Abstract Background: In recent decades, Candida albicans has become a serious issue for public health. The worldwide rapid rise in drug resistance to conventional therapies is the main contributing reason. Moreover, because of their potent activity at low concentrations and apparent lack of toxicity, compounds originating from plants are used in therapeutic treatments because of their potent activity at low concentrations and apparent lack of toxicity. Particularly in immunocompromised people, Candida species can result in a wide range of ailments.
    Objectives: Present manuscript describes antifungal activity of an indole derivative 1-(4-((5- methoxy-2-(3,4,5-trimethoxyphenyl)-1H-indol-1-yl) methyl) phenoxy)-N,N-dimethylethan-1- amine (7, 100DL-6) by using an in-silico and in-vitro anti-candidal activity against two Candida strains; Candida kefyr-DS-02 (ATCC-204093) and Candida albicans (AI-clinical isolate, AIIMS- Delhi).
    Methods: The synthetic strategy for the preparation of indole derivatives was modified through Fischer indole reaction. Antifungal activity of an indole derivative 1-(4-((5-methoxy-2-(3,4,5- trimethoxyphenyl)-1H-indol-1-yl) methyl) phenoxy)-N,N-dimethylethan-1-amine (7, 100DL-6) was done by using an in-silico and in-vitro anti-candidal activity against two Candida strains; Candida kefyr-DS-02 (ATCC-204093) and Candida albicans (AI-clinical isolate, AIIMS-Delhi). Compound 100DL-6 efficacy was determined by Combination synergy study, ergosterol binding assay, MTT toxicity study and Mutagenicity.
    Results: Compound 100DL-6 was obtained in 65% yield on desired motifs. Docking scores found were 100DL-6 (-8.7 kcal/mol) and Fluconazole (-7.6 kcal/mol). Further, RMSD were shown for 100DL6 (0.26 ± 0.23 nm) and fluconazole (1.2 ± 0.62 nm). Indole derivative 100DL-6 was active against the tested fungal pathogens and the total zone of inhibition was measured between 13-14 mm in diameter and MIC values between 31.25 μg/mL to 250 μg/mL and MFC values between 62.5 μg/mL to 500 μg/mL. In checkerboard assay synergistic mode of interaction of 100DL-6 with known antifungal drugs was observed. In the presence of ergosterol 100DL-6 and standard drug (s) increased their MIC values, demonstrating a considerable affinity for ergosterol. Compound 100DL-6 was considered to be less-cytotoxic to the cells as determined by MTT assay. Lead compound 100DL-6 was found to be non-mutagenic.
    Conclusion: In the present study, 100DL6 (indole derivatives) significantly abrupted the ergosterol biosynthetic pathway and showed moderate anti-candidal effects. These studies suggest that 100DL6 significantly enhances antifungal effect of clinical drug fluconazole synergistically and may be considered as in clinical trial prior to some extensive in-vivo validations.
    Language English
    Publishing date 2024-02-15
    Publishing country United Arab Emirates
    Document type Journal Article
    ZDB-ID 2064823-6
    ISSN 1873-4294 ; 1568-0266
    ISSN (online) 1873-4294
    ISSN 1568-0266
    DOI 10.2174/0115680266278892240102045630
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 5572: Show issues Location:
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  2. Article ; Online: Design, synthesis and broad spectrum antibreast cancer activity of diarylindoles via induction of apoptosis in aggressive breast cancer cells.

    Gautam, Yashveer / Das, Sharmistha / Khan, Hamidullah / Pathak, Nandini / Iqbal, Hina / Yadav, Pankaj / Sirohi, Vijay Kumar / Khan, Sana / Raghuvanshi, Dushyant Singh / Dwivedi, Anila / Chanda, Debabrata / Shanker, Karuna / Khan, Feroz / Konwar, Rituraj / Negi, Arvind S

    Bioorganic & medicinal chemistry

    2021  Volume 42, Page(s) 116252

    Abstract: Breast cancer is the second leading cause of cancer deaths in women with significant morbidity and mortality. Present study describes design, synthesis and detailed pharmacology of indole derivatives exhibiting remarkable broad spectrum antiproliferative ...

    Abstract Breast cancer is the second leading cause of cancer deaths in women with significant morbidity and mortality. Present study describes design, synthesis and detailed pharmacology of indole derivatives exhibiting remarkable broad spectrum antiproliferative activity against breast cancer cells. Detailed mechanistic evaluations confirmed induction of G0/G1 arrest, apoptosis induction, loss of mitochondrial integrity, enhanced ROS generation, autophagy, estrogen receptor β-transactivation and increased tubulin polymerization. In in-vivo efficacy studies in rodent model, these indole derivatives induced significant regression in mice mammary tumour on 21 days daily oral dose. Moreover, compounds 19 and 23 were safe in Swiss albino mice in safety studies. These diarylindoles may further be optimized for better efficacy.
    MeSH term(s) Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Apoptosis/drug effects ; Breast Neoplasms/drug therapy ; Breast Neoplasms/metabolism ; Breast Neoplasms/pathology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Design ; Drug Screening Assays, Antitumor ; Female ; Humans ; Indoles/chemical synthesis ; Indoles/chemistry ; Indoles/pharmacology ; Mammary Neoplasms, Experimental/drug therapy ; Mammary Neoplasms, Experimental/metabolism ; Mammary Neoplasms, Experimental/pathology ; Mice ; Mice, Inbred BALB C ; Molecular Structure ; Polymerization/drug effects ; Structure-Activity Relationship ; Tubulin/metabolism ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry ; Tubulin Modulators/pharmacology
    Chemical Substances Antineoplastic Agents ; Indoles ; Tubulin ; Tubulin Modulators
    Language English
    Publishing date 2021-06-05
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1161284-8
    ISSN 1464-3391 ; 0968-0896
    ISSN (online) 1464-3391
    ISSN 0968-0896
    DOI 10.1016/j.bmc.2021.116252
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    Zs.A 3815: Show issues Location:
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  3. Article ; Online: Indenes and tetralenes analogues attenuates lipopolysaccharide-induced inflammation: An in-vitro and in-vivo study.

    Mohanty, Shilpa / Gautam, Yashveer / Maurya, Anil Kumar / Negi, Arvind S / Prakash, Om / Khan, Feroz / Bawankule, Dnyaneshwar Umrao

    Chemico-biological interactions

    2016  Volume 245, Page(s) 12–19

    Abstract: In an effort to evaluate novel pharmacological activity of 1-chloro-2-formyl indene and tetralene analogues possessing potential antitubercular and antistaphylococcal agents, we explored its anti-inflammatory potential against lipopolysaccharide(LPS)- ... ...

    Abstract In an effort to evaluate novel pharmacological activity of 1-chloro-2-formyl indene and tetralene analogues possessing potential antitubercular and antistaphylococcal agents, we explored its anti-inflammatory potential against lipopolysaccharide(LPS)-induced inflammation using in-vitro and in-vivo bioassay. Synthesized analogues significantly inhibited the production and expression of pro-inflammatory cytokines against LPS-induced inflammation in macrophages isolated from mice. Among all the analogues, TAF-5 (1-Chloro-2-formyl-1-tetralene) exhibited most potent anti-inflammatory activity without any cytotoxic effect. We have further evaluated the therapeutic efficacy and safety of TAF-5 in in-vivo system using LPS-induced sepsis, a systemic inflammation model and acute oral toxicity respectively in mice. Oral administration of TAF-5 inhibited the pro-inflammatory cytokines in serum, attenuated the organs injuries and improved host survival in dose dependent manner. Acute oral toxicity study showed TAF-5 is non-toxic at higher dose in mice. These results suggest the suitability of indene and tetralene analogues as new chemical entities for further investigation towards the management of inflammation related diseases.
    MeSH term(s) Administration, Oral ; Animals ; Anti-Inflammatory Agents/administration & dosage ; Anti-Inflammatory Agents/chemistry ; Anti-Inflammatory Agents/therapeutic use ; Cell Survival/drug effects ; Cytokines/blood ; Cytokines/genetics ; Cytokines/immunology ; Female ; Gene Expression Regulation/drug effects ; Indenes/administration & dosage ; Indenes/chemistry ; Indenes/therapeutic use ; Inflammation/blood ; Inflammation/drug therapy ; Inflammation/genetics ; Inflammation/immunology ; Lipopolysaccharides/immunology ; Macrophages/drug effects ; Macrophages/immunology ; Macrophages/pathology ; Mice ; Mice, Inbred BALB C ; Molecular Docking Simulation ; Sepsis/blood ; Sepsis/drug therapy ; Sepsis/genetics ; Sepsis/immunology
    Chemical Substances Anti-Inflammatory Agents ; Cytokines ; Indenes ; Lipopolysaccharides
    Language English
    Publishing date 2016-02-05
    Publishing country Ireland
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 218799-1
    ISSN 1872-7786 ; 0009-2797
    ISSN (online) 1872-7786
    ISSN 0009-2797
    DOI 10.1016/j.cbi.2015.12.005
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    Zs.A 686: Show issues Location:
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  4. Article: 2-(3′,4′-Dimethoxybenzylidene)tetralone induces anti-breast cancer activity through microtubule stabilization and activation of reactive oxygen species

    Gautam, Yashveer / Dwivedi, Sonam / Srivastava, Ankita / Hamidullah / Singh, Arjun / Chanda, D / Singh, Jyotsna / Rai, Smita / Konwar, Rituraj / Negi, Arvind S

    RSC advances. 2016 Apr. 05, v. 6, no. 40

    2016  

    Abstract: Breast cancer is a leading cause of women mortality worldwide. Diverse analogues of 2-benzylidene tetralone have been synthesized and evaluated for anti-cancer activity against a panel of cancer cell lines. Among these, compounds 13, 15 and 19 exhibited ... ...

    Abstract Breast cancer is a leading cause of women mortality worldwide. Diverse analogues of 2-benzylidene tetralone have been synthesized and evaluated for anti-cancer activity against a panel of cancer cell lines. Among these, compounds 13, 15 and 19 exhibited potent anti-cancer activity (IC50 = 1–3 μM) against human breast cancer cells, MDA-MB-231 and non-toxic towards non-malignant cell line, HEK-293. Compounds 13, 15 and 19 significantly stabilized tubulin polymerization and arrested cell cycle progression at G0/G1 phase instead of typical mitotic arrest at G2/M phase as observed in case of tubulin polymerization modulators suggesting induction of mitotic slippage followed by cell death. Further, mechanistic studies revealed that compound 13 induced reactive oxygen species generation and apoptosis in breast cancer cells. Inhibition of ROS by N-acetyl-l-cysteine prevented compound 13 induced cytotoxicity. Compound 13 showed potent anti-cancer activity (74–79% tumour reduction) in syngeneic rat mammary tumour model without any adverse side effect. It was well tolerated up to 1000 mg kg−1 dose in acute oral toxicity. The identified lead molecule 13 may further be optimized for better activity.
    Keywords acetylcysteine ; acute oral toxicity ; adverse effects ; antineoplastic activity ; apoptosis ; breast neoplasms ; cell lines ; cytotoxicity ; inhibitory concentration 50 ; interphase ; mammary neoplasms (animal) ; microtubules ; mitosis ; models ; mortality ; neoplasm cells ; polymerization ; rats ; reactive oxygen species ; tubulin ; women
    Language English
    Dates of publication 2016-0405
    Size p. 33369-33379.
    Publishing place The Royal Society of Chemistry
    Document type Article
    ISSN 2046-2069
    DOI 10.1039/c6ra02663j
    Database NAL-Catalogue (AGRICOLA)

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  5. Article ; Online: Natural antitubulin agents: importance of 3,4,5-trimethoxyphenyl fragment.

    Negi, Arvind S / Gautam, Yashveer / Alam, Sarfaraz / Chanda, Debabrata / Luqman, Suaib / Sarkar, Jayanta / Khan, Feroz / Konwar, Rituraj

    Bioorganic & medicinal chemistry

    2015  Volume 23, Issue 3, Page(s) 373–389

    Abstract: Microtubules are polar cytoskeletal filaments assembled from head-to-tail and comprised of lateral associations of α/β-tubulin heterodimers that play key role in various cellular processes. Because of their vital role in mitosis and various other ... ...

    Abstract Microtubules are polar cytoskeletal filaments assembled from head-to-tail and comprised of lateral associations of α/β-tubulin heterodimers that play key role in various cellular processes. Because of their vital role in mitosis and various other cellular processes, microtubules have been attractive targets for several disease conditions and especially for cancer. Antitubulin is the most successful class of antimitotic agents in cancer chemotherapeutics. The target recognition of antimitotic agents as a ligand is not much explored so far. However, 3,4,5-trimethoxyphenyl fragment has been much highlighted and discussed in such type of interactions. In this review, some of the most important naturally occurring antimitotic agents and their interactions with microtubules are discussed with a special emphasis on the role of 3,4,5-trimethoxyphenyl unit. At last, some emerging naturally occurring antimitotic agents have also been tabulated.
    MeSH term(s) Animals ; Anisoles/chemistry ; Anisoles/pharmacology ; Antimitotic Agents/chemistry ; Antimitotic Agents/pharmacology ; Humans ; Microtubules/drug effects ; Molecular Structure ; Structure-Activity Relationship ; Tubulin/chemistry ; Tubulin/metabolism ; Tubulin Modulators/chemistry ; Tubulin Modulators/pharmacology
    Chemical Substances Anisoles ; Antimitotic Agents ; Tubulin ; Tubulin Modulators
    Language English
    Publishing date 2015-02-01
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 1161284-8
    ISSN 1464-3391 ; 0968-0896
    ISSN (online) 1464-3391
    ISSN 0968-0896
    DOI 10.1016/j.bmc.2014.12.027
    Database MEDical Literature Analysis and Retrieval System OnLINE

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