Review
Medicine, Research & Experimental
Jian Zhang, Hai Zhao, Gang Yao, Penghai Qiao, Longfei Li, Shuguang Wu
Summary: Iron is an essential trace element for living organisms, but iron overload can lead to osteoporosis. Iron chelators have therapeutic effects on iron overload-induced osteoporosis and may also be used for treating bone loss caused by other factors. Iron chelators have different effects on bone cells, stimulating osteogenic differentiation in osteoblast lineage cells and inhibiting osteoclast differentiation. Antioxidant capability and fibroblast growth factor 23 are also involved in the osteoprotective effects of iron chelators.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Article
Biochemistry & Molecular Biology
Hao Yang, Fang-Ting Wang, Min Wu, Wenjie Wang, Keli Agama, Yves Pommier, Lin -Kun An
Summary: In this study, 11-aminoalkoxy substituted benzophenanthridine derivatives were synthesized as selective TDP1 inhibitors. Six compounds showed high TDP1 inhibition potency, and the most potent inhibitor 14 induced cellular TDP1cc formation and exhibited synergistic effect with topotecan in various cancer cell lines.
BIOORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
O. Yu. Selyutina, P. A. Kononova, V. E. Koshman, E. A. Shelepova, M. Gholam Azad, R. Afroz, M. Dharmasivam, Paul V. Bernhardt, N. E. Polyakov, D. R. Richardson
Summary: Ascorbate-driven redox cycling enhances the anti-proliferative activity of Dp44mT and Emodin.
BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS
(2022)
Article
Chemistry, Medicinal
Zhenlei Zhang, Juzheng Zhang, Tongfu Yang, Shanhe Li, Gang Xu, Hong Liang, Feng Yang
Summary: To develop a next-generation Pt drug with high activity and low toxicity, researchers optimized a Pt(II) thiosemicarbazone compound (C4) with remarkable cytotoxicity to SK N-MC cells and constructed a human serum albumin-C4 (HSA-C4) complex delivery system. In vivo experiments showed that both C4 and the HSA-C4 complex had excellent therapeutic efficiency and minimal toxicity, inducing apoptosis and inhibiting tumor angiogenesis. This system has the potential to become a practical Pt drug, paving the way for the development of next-generation dual-targeted Pt drugs for cancer targeting therapy.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Aarajana Shrestha, Soo-Yeon Hwang, Surendra Kunwar, Tara Man Kadayat, Seojeong Park, Yi Liu, Hyunji Jo, Naeun Sheen, Minjung Seo, Eung-Seok Lee, Youngjoo Kwon
Summary: Topoisomerases are important enzymes for altering DNA topology and have been considered as attractive targets for chemotherapeutic agents. In this study, we presented new di-indenopyridine compounds with inhibitory activity against topoisomerase I/II and alpha. Compound 17 showed 100% inhibition of topoisomerase II and alpha at 20 μM concentration, as well as comparable antiproliferative activity against tested cell lines. These findings highlight the significance of specific groups at the 4-position of the indane ring in designing potent catalytic topoisomerase II and alpha inhibitors with anticancer effects.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
George J. Kontoghiorghes, Annita Kolnagou, Theodora Demetriou, Marina Neocleous, Christina N. Kontoghiorghe
Summary: Trimaltol iron complex is a stable and safe iron supplement used for treating iron deficiency anaemia, showing increased iron absorption capabilities. Compared to other iron formulations, it has a better therapeutic index.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Infectious Diseases
Victor Vinuesa, Raquel Cruces, Francesca Nonnoi, Michael J. McConnell
Summary: Novel synergy between LpxC inhibitors and iron chelators or gallium nitrate has been identified against A. baumannii strains, leading to a significant reduction in bacterial growth.
Article
Chemistry, Medicinal
Mostafa M. Elbadawi, Wagdy M. Eldehna, Wenjie Wang, Keli K. Agama, Yves Pommier, Manabu Abe
Summary: Two novel series of 4-alkoxy-2-arylquinolines were designed and synthesized for potential anticancer agents targeting Topoisomerase I, showing potent anticancer activity at sub-micromolar level against diverse cancer cell lines. Compound 14m exhibited the most potent activity, particularly against colon cancer, leukemia, and melanoma cell lines. This compound was also found to stabilize TOP1-DNA cleavage complexes, indicating its potential as a lead compound for the development of more potent anticancer agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Lini Huo, Xiaochen Liu, Yogini Jaiswal, Hao Xu, Rui Chen, Rumei Lu, Yaqin Nong, Leonard Williams, Yan Liang, Zhiruo Jia
Summary: We designed and synthesized a series of novel acridine-triazole and acridine-thiadiazole derivatives. These compounds showed high levels of antitumor activity against gastric cancer cells and bladder cancer cells, while exhibiting low toxicity to normal liver cells. Moreover, their pharmacological mechanisms and effects on cell cycle and apoptosis were evaluated. Furthermore, these compounds demonstrated low cytotoxicity to zebrafish but strong inhibition of the formation of zebrafish sub-intestinal veins, suggesting potential clinical applications.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Medicine, Research & Experimental
Michela Asperti, Luca Cantamessa, Magdalena Gryzik, Mattia Bugatti, Silvia Codenotti, Andrea Denardo, William Vermi, Alessandro Fanzani, Maura Poli
Summary: Rhabdomyosarcoma (RMS) is an aggressive rare neoplasm that requires new therapies. This study investigated the effect of iron modulation on RMS and found that both iron supplementation and iron chelation significantly inhibited tumor growth.
CLINICAL AND EXPERIMENTAL MEDICINE
(2023)
Article
Chemistry, Multidisciplinary
Jiri Kos, Tomas Strharsky, Sarka Stepankova, Katarina Svrckova, Michal Oravec, Jan Hosek, Ales Imramovsky, Josef Jampilek
Summary: A series of nature-inspired 3,4,5-trimethoxycinnamates were synthesized and characterized, with some compounds showing inhibitory activity against AChE and BChE, indicating potential pharmaceutical value.
APPLIED SCIENCES-BASEL
(2021)
Article
Chemistry, Multidisciplinary
Thi-Kim-Chi Huynh, Kim-Khanh-Huy Ngo, Hoang-Phuc Nguyen, Hoai-Khanh Dang, Van-Trung Phung, Khac-Minh Thai, Thi-Kim-Dung Hoang
Summary: A highly efficient and sustainable method for synthesizing 3-aminoalkylated indoles via a Mannich-type reaction without a catalyst, using methanol and ethylene glycol, was investigated. The synthesized indole derivatives were studied for their anticancer activity and showed significant potential against various cancer cell lines, with compounds 5e and 5f exhibiting multitargeted anticancer properties. Molecular docking studies revealed the binding interactions of the most potent compounds at the TopI-DNA binding site, indicating similarities to camptothecin binding.
NEW JOURNAL OF CHEMISTRY
(2021)
Article
Environmental Sciences
Boon Chong Ong, Hong Kit Lim, Chor Yong Tay, Teik-Thye Lim, ZhiLi Dong
Summary: Introducing cobalt-based polyoxometalates (CoV-POMs) into peroxymonosulphate (PMS) greatly enhances the catalytic activation for a complete degradation of organic dyes. The CoV-POMs exhibit non-toxic behavior towards normal cells and also showcase anticancer properties against lung and breast adenocarcinoma cells, indicating their potential for large-scale wastewater treatment and cancer therapy.
Article
Biochemistry & Molecular Biology
Umesh Prasad Yadav, Arshad J. Ansari, Sahil Arora, Gaurav Joshi, Tashvinder Singh, Harsimrat Kaur, Nilambra Dogra, Raj Kumar, Santosh Kumar, Devesh M. Sawant, Sandeep Singh
Summary: A series of imido-heterocycle compounds were synthesized and evaluated for their anticancer potential. Compound 4h showed the best anticancer activity, inhibiting cell cycle and inducing apoptosis in multiple cancer cell lines. The inhibitory effect on MDA-MB-231 mammosphere formation was also observed.
BIOORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Doaa M. Khaled, Mohamed E. Elshakre, Mahmoud A. Noamaan, Haider Butt, Marwa M. Abdel Fattah, Dalia A. Gaber
Summary: Computational chemistry, molecular docking, and drug design approaches were used in this study to evaluate the antitumor activity of thiouracil-based dihydroindeno pyrido pyrimidine derivatives against topoisomerase I and II. The IC50 values of various cell lines were determined using biochemical methods. The computed reactivity descriptors and physicochemical parameters showed good agreement with drug criteria. Molecular docking analysis provided information on binding sites, binding energies, and deactivation constants. QSAR models were developed to correlate IC50 values of colorectal cell line HCT with physicochemical and quantum chemical descriptors, showing good predictive power.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Oncology
Thomas G. Biel, V. Ashutosh Rao
Article
Multidisciplinary Sciences
Baikuntha Aryal, V. Ashutosh Rao
Article
Endocrinology & Metabolism
Kaytee L. Pokrzywinski, Thomas G. Biel, Elliot T. Rosen, Julia L. Bonanno, Baikuntha Aryal, Francesca Mascia, Delaram Moshkelani, Steven Mog, V. Ashutosh Rao
BIOLOGY OF SEX DIFFERENCES
(2018)
Meeting Abstract
Oncology
Baikuntha P. Aryal, Jean-Pierre Gillet, V. Ashutosh Rao
Meeting Abstract
Oncology
Elliot T. Rosen, Dmitry Kryndushkin, Baikuntha Aryal, Yanira Gonzalez, Leena Chehab, Jennifer Dickey, Steven Mog, V. Ashutosh Rao
Article
Chemistry, Multidisciplinary
Geoffrey A. Heinzl, Lo Lai, V. Ashutosh Rao
PHARMACEUTICAL RESEARCH
(2019)
Article
Chemistry, Analytical
Kui Yang, Asha Hewarathna, Ilan Geerlof-Vidaysky, V. Ashutosh Rao, Connie Gryniewicz-Ruzicka, David Keire
ANALYTICAL CHEMISTRY
(2019)
Editorial Material
Oncology
V. Ashutosh Rao
Article
Multidisciplinary Sciences
Elliot Rosen, Dmitry Kryndushkin, Baikuntha Aryal, Yanira Gonzalez, Leena Chehab, Jennifer Dickey, V. Ashutosh Rao
Article
Cell Biology
Thomas G. Biel, Baikuntha Aryal, Michael H. Gerber, Jose G. Trevino, Naoko Mizuno, V. Ashutosh Rao
CELL DEATH & DISEASE
(2020)
Meeting Abstract
Oncology
Yong Zhang, Svetlana Petrovskaya, Emma C. Scott, Luis Santana-Quintero, Tigran Ghazanchyan, Amy Rosenburg, V. Ashutosh Rao, Gideon M. Blumenthal, Marc Theoret, Richard Pazdur, Julia A. Beaver, Dickran Kazandjian
Meeting Abstract
Oncology
Elliot T. Rosen, Dmitry Kryndushkin, Baikuntha Aryal, Yanira Gonzalez, Leena Chehab, Jennifer Dickey, Steven Mog, V. Ashutosh Rao
Meeting Abstract
Oncology
Emma C. Scott, Dickran Kazandjian, Luis Santana-Quintero, Tigran Ghazanchyan, Svetlana Petrovskaya, Yong Zhang, Amy Rosenberg, V. Ashutosh Rao, Jennifer L. Marte, Gideon M. Blumenthal, Marc R. Theoret, Richard Pazdur, James L. Gulley, Julia A. Beaver
Meeting Abstract
Oncology
Baikuntha P. Aryal, Jean-Pierre Gillet, V. Ashutosh Rao
Article
Clinical Neurology
Annemieke Aartsma-Rus, Jennifer Morgan, Pallavi Lonkar, Hendrik Neubert, Jane Owens, Michael Binks, Marisol Montolio, Rahul Phadke, Nicole Datson, Judith Van Deutekom, Glenn E. Morris, V. Ashutosh Rao, Eric P. Hoffman, Francesco Muntoni, Virginia Arechavala-Gomeza
JOURNAL OF NEUROMUSCULAR DISEASES
(2019)