Article
Biochemical Research Methods
Amiya Kumar Patel, Rajesh Kumar Meher, Praveen Kumar Reddy, Ravi Kumar Pedapati, Pratyush Pragyandipta, Srinivas Kantevari, Manas Ranjan Naik, Pradeep Kumar Naik
Summary: A new class of 1,3-diynyl-noscapinoids derivatives showed anticancer activity against breast cancer cells, with improved binding affinity to tubulin compared to the lead molecule. These derivatives effectively inhibited cellular proliferation, arrested cell cycle in the G2/M phase, and induced apoptosis, demonstrating great potential as a novel therapeutic agent for breast cancers.
JOURNAL OF MOLECULAR GRAPHICS & MODELLING
(2021)
Article
Biochemistry & Molecular Biology
Rajesh Kumar Meher, Pratyush Pragyandipta, Praveen Kumar Reddy, Ravikumar Pedaparti, Srinivas Kantevari, Pradeep K. Naik
Summary: Novel 1,3-diynyl derivatives of noscapine were developed using in silico combinatorial approach, showing promising antitumor activities by targeting tubulin. These derivatives demonstrated cytotoxicity against cancer cells while sparing normal cells, suggesting their potential as a new therapeutic agent for breast cancers.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Biochemistry & Molecular Biology
Rajesh Kumar Meher, Praveen Kumar Reddy Nagireddy, Pratyush Pragyandipta, Srinivas Kantevari, Satyandra Kumar Singh, Vijay Kumar, Pradeep K. Naik
Summary: A series of 9-arylimino derivatives of noscapine were synthesized and shown to display anticancer activity against a panel of breast cancer cells by binding to tubulin. These derivatives effectively inhibited cellular proliferation, arrested the cell cycle in the G2/M-phase, and induced apoptosis in cancer cells.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Chemistry, Multidisciplinary
Pratyush Pragyandipta, Rajesh K. Meher, Manas R. Naik, Praveen K. R. Nagireddy, Ravi K. Pedapati, Srinivas Kantevari, Pradeep K. Naik
Summary: A series of 1,3-diynyl-noscapine derivatives were designed to enhance the anticancer activity, exhibiting strong cytotoxic effects on human breast cancer cells and potential as a novel therapeutic agent.
Article
Biochemistry & Molecular Biology
Faezeh Nemati, Iris Bischoff-Kont, Peyman Salehi, Samad Nejad-Ebrahimi, Maryam Mohebbi, Morteza Bararjanian, Nasim Hadian, Zahra Hassanpour, Yvonne Jung, Sofie Schaerlaekens, Daniel Lucena-Agell, Maria A. Oliva, Robert Fuerst, Hamid R. Nasiri
Summary: A library of novel noscapine derivatives was synthesized, with two of them identified as potent inhibitors of MDA-MB-231 breast cancer cells. These derivatives have improved antiproliferative properties compared to the lead compound noscapine.
BIOORGANIC CHEMISTRY
(2021)
Article
Biology
Shruti Gamya Dash, Srinivas Kantevari, Santosh Kumar Guru, Pradeep Kumar Naik
Summary: The novel compound 9-Br-Trimethoxybenzyl noscapine (BTN) was designed to bind with tubulin with rigorous affinity, showing significant effects on tubulin binding, cell cycle progression, and induction of breast cancer cell death when used in combination with docetaxel (DOX).
COMPUTERS IN BIOLOGY AND MEDICINE
(2021)
Article
Biochemistry & Molecular Biology
Jun Morishita, Paul Nurse
Summary: Researchers identified novel small molecules that inhibit microtubule organization through sequential phenotypic screening of fission yeast and human cells. In vitro assays showed that these compounds directly bind tubulin and destabilize the structures of tubulin dimers. One compound in particular, L1, demonstrated preferential potency against human breast cancer cell lines and synergistic effects when combined with the Plk1 inhibitor BI2536, suggesting it as a candidate for cancer chemotherapy.
Article
Biochemistry & Molecular Biology
Magdalena Peruzynska, Aleksandra Borzyszkowska-Ledwig, Jacek G. Sosnicki, Lukasz Struk, Tomasz J. Idzik, Gabriela Maciejewska, Lukasz Skalski, Katarzyna Piotrowska, Pawel Lukasik, Marek Drozdzik, Mateusz Kurzawski
Summary: This study successfully obtained a mitotic-specific inhibitor with high antiproliferative activity and selectivity through structural modifications. By inhibiting tubulin polymerization in a dose-dependent manner, aberrant mitotic spindle formation was induced, leading to cell cycle arrest and apoptosis.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Pratyush Pragyandipta, Ravi Kumar Pedapati, Praveen Kumar Reddy, Arnab Nayek, Rajesh Kumar Meher, Santosh Kumar Guru, Srinivas Kantevari, Pradeep K. Naik
Summary: We have developed a new class of noscapine derivatives, N-imidazopyridine-noscapinoids, that bind to tubulin and show antiproliferative activity against breast cancer cells. These compounds have higher tubulin binding affinity than noscapine and selectively target breast cancer cells without affecting normal cells. One particular compound, N-5-Bromoimidazopyridine-noscapine, exhibited promising antiproliferative activity, induced apoptosis, and successfully regressed implanted tumors in mice. We conclude that N-imidazopyridine-noscapinoids have excellent potential as a treatment for breast cancer.
CHEMICO-BIOLOGICAL INTERACTIONS
(2023)
Article
Biotechnology & Applied Microbiology
Pratyush Pragyandipta, Manas Ranjan Naik, Banajit Bastia, Pradeep Kumar Naik
Summary: Researchers have developed 9-N-arylmethylamino derivatives of noscapine that can kill cancer cells without affecting normal cells. These derivatives induce apoptosis by arresting cells at G2/M phase and binding to tubulin, showing potential as a novel therapeutic agent for breast cancer treatment.
Article
Chemistry, Medicinal
Kun Wang, Hui Zhong, Na Li, Nairong Yu, Yujin Wang, Li Chen, Jianbo Sun
Summary: Compound 12, a novel dual-receptor inhibitor targeting both tubulin and AhR, showed strong anti-breast-cancer activity with potent inhibition of tumor growth in cell lines and xenograft models, as well as inducing apoptosis in breast cancer cells. Its ability to synergistically antagonize tubulin and AhR makes it a promising candidate for further development as an effective and safe anti-breast-cancer drug.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
A. K. Patel, R. K. Meher, P. K. Nagireddy, P. Pragyandipta, R. K. Pedapati, S. Kantevari, P. K. Naik
Summary: A library of 9-arylimino derivatives of noscapine was developed through Schiff base coupling, with compounds 12-14 showing high binding affinity to tubulin. Molecular dynamics simulation combined with MM-PBSA demonstrated strong binding free energies for these compounds, which exhibited significant anticancer activity in breast cancer cell lines by inhibiting cell proliferation and inducing apoptosis.
SAR AND QSAR IN ENVIRONMENTAL RESEARCH
(2021)
Article
Chemistry, Inorganic & Nuclear
Celisnolia M. Leite, Joao Honorato, Ana Carolina B. M. Martin, Rafael G. Silveira, Felippe M. Colombari, Jessica C. Amaral, Analu R. Costa, Marcia R. Cominetti, Ana M. Plutin, Debora de Aguiar, Boniek G. Vaz, Alzir A. Batista
Summary: The study synthesized and characterized six copper(I) complexes, which exhibited cytotoxicity towards three tumor cell lines, with one complex showing significant effects on the cytoskeleton and induction of apoptosis in TNBC cells.
INORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Shruti Gamya Dash, Charu Suri, Praveen Kumar Reddy Nagireddy, Srinivas Kantevari, Pradeep Kumar Naik
Summary: Docetaxel and noscapine are two compounds with potential anti-cancer properties, with noscapine showing promise due to its lack of side effects. A novel derivative, 9-vinyl phenyl noscapine (VPN), has been designed to enhance the anticancer activity of noscapine. The combination of VPN and Docetaxel shows improved cytotoxicity and apoptotic cell death in breast cancer treatment.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Biochemistry & Molecular Biology
Yichang Ren, Yong Ruan, Binbin Cheng, Ling Li, Jin Liu, Yuyu Fang, Jianjun Chen
Summary: Compound 3b, designed as a tubulin inhibitor targeting the colchicine binding site, showed high antiproliferative activity against HepG-2 cells, with the ability to suppress microtubule polymerization, disrupt dynamics, inhibit cancer cell migration, induce cell cycle arrest and apoptosis. Docking studies indicated its potential as a novel tubulin inhibitor deserving further investigation.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Rajesh Kumar Meher, Praveen Kumar Reddy Nagireddy, Pratyush Pragyandipta, Srinivas Kantevari, Satyandra Kumar Singh, Vijay Kumar, Pradeep K. Naik
Summary: A series of 9-arylimino derivatives of noscapine were synthesized and shown to display anticancer activity against a panel of breast cancer cells by binding to tubulin. These derivatives effectively inhibited cellular proliferation, arrested the cell cycle in the G2/M-phase, and induced apoptosis in cancer cells.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Chemistry, Multidisciplinary
A. K. Patel, R. K. Meher, P. K. Nagireddy, P. Pragyandipta, R. K. Pedapati, S. Kantevari, P. K. Naik
Summary: A library of 9-arylimino derivatives of noscapine was developed through Schiff base coupling, with compounds 12-14 showing high binding affinity to tubulin. Molecular dynamics simulation combined with MM-PBSA demonstrated strong binding free energies for these compounds, which exhibited significant anticancer activity in breast cancer cell lines by inhibiting cell proliferation and inducing apoptosis.
SAR AND QSAR IN ENVIRONMENTAL RESEARCH
(2021)
Article
Chemistry, Multidisciplinary
Pratyush Pragyandipta, Rajesh K. Meher, Manas R. Naik, Praveen K. R. Nagireddy, Ravi K. Pedapati, Srinivas Kantevari, Pradeep K. Naik
Summary: A series of 1,3-diynyl-noscapine derivatives were designed to enhance the anticancer activity, exhibiting strong cytotoxic effects on human breast cancer cells and potential as a novel therapeutic agent.
Article
Chemistry, Medicinal
Praveen Kumar Reddy Nagireddy, Dinesh Kumar, Vamsi Krishna Kommalapati, Ravi Kumar Pedapati, Venkateswarlu Kojja, Anjana Devi Tangutur, Srinivas Kantevari
Summary: Noscapine is a phthalide isoquinoline alkaloid with potent antitumor activity, and novel analogs of noscapine have been synthesized with one compound (9-ethynyl noscapine) showing significant anticancer activity against cervical cancer cells (HeLa) by disrupting tubulin polymerization, cell cycle progression, and inducing apoptosis.
DRUG DEVELOPMENT RESEARCH
(2022)
Article
Chemistry, Medicinal
Habeebunnisa Begum, Nagaraju Chirra, Dinesh Kumar, Periyasamy Murugesan, Srinivas Kantevari, Anjana Devi Tangutur
Summary: The study demonstrates that the quinoline derivative 6MN-4-AQ can inhibit the growth and invasion of pancreatic cancer cells by inducing autophagy and apoptosis. The therapeutic effect of 6MN-4-AQ is achieved through the suppression of the Akt/mTOR pathway, induction of ER stress, and inhibition of epithelial-mesenchymal transition.
DRUG DEVELOPMENT RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Rajesh Kumar Meher, Pratyush Pragyandipta, Praveen Kumar Reddy, Ravikumar Pedaparti, Srinivas Kantevari, Pradeep K. Naik
Summary: Novel 1,3-diynyl derivatives of noscapine were developed using in silico combinatorial approach, showing promising antitumor activities by targeting tubulin. These derivatives demonstrated cytotoxicity against cancer cells while sparing normal cells, suggesting their potential as a new therapeutic agent for breast cancers.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Biochemistry & Molecular Biology
Ravi Kumar Pedapati, Pratyush Pragyandipta, Naga Pranathi Abburi, Nagaraju Chirra, Srinivas Kantevari, Pradeep K. Naik
Summary: In this study, a series of new amido-thiadiazol coupled noscapinoids were synthesized and their cytotoxicity was tested in vitro. All of the newly synthesized compounds showed potent cytotoxic potential, with IC50 values ranging from 2.1 to 61.2 μM, higher than noscapine, and without affecting normal cells. Molecular docking studies revealed that these compounds had better binding affinity with tubulin compared to noscapine. One of the most promising synthetic derivatives, 6aa, exhibited the highest binding affinity with tubulin and induced apoptosis in cancer cells more effectively.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Chemistry, Multidisciplinary
Ravi Kumar Pedapati, Nagaraju Chirra, Naga Pranathi Abburi, Rakesh Bollikonda, Danaboiena Alekhya, Balasubramanian Sridhar, Pradeep K. Naik, Srinivas Kantevari
Summary: A series of new noscapinoids were designed, synthesized, and assessed for their cytotoxicity improvements. The newly synthesized derivatives exhibited strong cytotoxic potential against cancer cells in vitro without harming normal cells.
CHEMISTRY-AN ASIAN JOURNAL
(2023)
Article
Biotechnology & Applied Microbiology
Pratyush Pragyandipta, Manas Ranjan Naik, Banajit Bastia, Pradeep Kumar Naik
Summary: Researchers have developed 9-N-arylmethylamino derivatives of noscapine that can kill cancer cells without affecting normal cells. These derivatives induce apoptosis by arresting cells at G2/M phase and binding to tubulin, showing potential as a novel therapeutic agent for breast cancer treatment.
Article
Immunology
Priya Cheruvanachari, Subhaswaraj Pattnaik, Monika Mishra, Pratyush Pragyandipta, Animesh Pattnaik, Pradeep Kumar Naik
Summary: In this study, 2-Phenyl Ethyl Methyl Ether (PEME) extracted from Kewda essential oil showed potential antimicrobial and anti-biofilm properties against ESKAPE pathogenic bacterial strains. It effectively reduced biofilm formation and exopolysaccharides production. Silico studies and gene expression analysis further supported its candidacy as a promising anti-biofilm agent.
MICROBIAL PATHOGENESIS
(2023)
Article
Biochemistry & Molecular Biology
Pratyush Pragyandipta, Ravi Kumar Pedapati, Praveen Kumar Reddy, Arnab Nayek, Rajesh Kumar Meher, Santosh Kumar Guru, Srinivas Kantevari, Pradeep K. Naik
Summary: We have developed a new class of noscapine derivatives, N-imidazopyridine-noscapinoids, that bind to tubulin and show antiproliferative activity against breast cancer cells. These compounds have higher tubulin binding affinity than noscapine and selectively target breast cancer cells without affecting normal cells. One particular compound, N-5-Bromoimidazopyridine-noscapine, exhibited promising antiproliferative activity, induced apoptosis, and successfully regressed implanted tumors in mice. We conclude that N-imidazopyridine-noscapinoids have excellent potential as a treatment for breast cancer.
CHEMICO-BIOLOGICAL INTERACTIONS
(2023)
Article
Chemistry, Medicinal
Rakesh K. Bollikanda, Devendra Nagineni, Abburi Naga Pranathi, Nagaraju Chirra, Sunil Misra, Srinivas Kantevari
Summary: This study synthesized a series of novel compounds by coupling partly saturated benzothiazoles with substituted piperazines, and evaluated their antimicrobial activity. Two compounds showed the best antifungal activity, while four compounds demonstrated strong antibacterial action. This scaffold has potential for the development of antimicrobial drugs.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Analytical
Pratyush Pragyandipta, Rajesh Kumar Meher, Praveen Kumar Reddy, Ravikumar Pedaparti, Srinivas Kantevari, Pradeep K. Naik
Summary: This study designed a novel class of 9-arylimino noscapinoids and demonstrated their high affinity for binding with tumor-related proteins in vitro. These molecules exhibited the ability to inhibit proliferation and induce apoptosis in breast cancer cells, indicating their potential as chemotherapeutic agents for breast cancer treatment.
ANALYTICAL CHEMISTRY LETTERS
(2022)
Article
Biochemistry & Molecular Biology
Ali Mehri, Karim Mahnam, Hajar Sirous, Mahmoud Aghaei, Leila Rafiei, Mahboubeh Rostami
Summary: One potential approach for tumor therapy is inhibiting the binding between MDM2 and p53 to reactivate p53 in tumor cells. In this study, Monastrol derivatives were designed as MDM2 inhibitors and evaluated for their cytotoxicity on cancer cells. Compound 5d showed the best inhibitory results in silico and in vitro experiments. These findings suggest that Monastrol derivatives have the potential to be candidates for MDM2 inhibition.
CHEMICAL BIOLOGY & DRUG DESIGN
(2024)