This study involved the administration of amonafide intravenously 300 mg/m2 daily times five days every three weeks to 16 refractory and relapsed myeloma patients. Doses were escalated to toxicity. These doses caused severe thrombocytopenia and granulocytopenia in seven patients. No responses were seen in this heavily pretreated group of patients.
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Design, docking optimization, and evaluation of biotin-PEG4-1,8-naphthalimide as a potent and safe antitumor agent with dual targeting of ferroptosis and DNA.
RSC Med Chem
May 2024
Guangxi Key Laboratory of Drug Discovery and Optimization, School of Pharmacy, Guilin Medical University Guilin 541004 China
Article Synopsis
- A set of biotin-PEG-naphthalimide derivatives were designed to target ferroptosis and DNA as potential antitumor agents, with biotin-PEG4-piperazine-1,8-naphthalimide (4d) identified as the top candidate through docking simulations.
- In vitro and in vivo tests showed that 4d demonstrated significant antitumor efficacy and safety, outperforming known treatments like amonafide and temozolomide.
- The compound was found to induce DNA damage, inhibit DNA synthesis, cause cell cycle arrest, and promote lipid peroxidation, effectively triggering ferroptosis in cancer cells via a dual-targeting approach.
Discovery of 4-(N-dithiobenzyl piperazine)-1,8-naphthalimide as a potent multi-target antitumor agent with good efficacy, limited toxicity, and low resistance.
Eur J Med Chem
January 2024
Guangxi Key Laboratory of Drug Discovery and Optimization, Guangxi Engineering Research Center for Pharmaceutical Molecular Screening and Druggability Evaluation, Key Laboratory of Medical Biotechnology and Translational Medicine, School of Pharmacy, Guilin Medical University, Guilin, 541004, China. Electronic address:
A series of 4-(N-dithiobenzyl piperazine)-1,8-naphthalimide derivatives 4-6 were designed, synthesized, and evaluated as novel multi-target antitumor agents. 3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) results showed that compounds 5j, 5k, and 6j exhibited superior in vitro antiproliferative activity in MGC-803, HepG-2, SKOV-3, and T24 cancer cell lines and the cisplatin-resistant cell line A549/DDP. HepG-2, SKOV-3, and T24 xenograft assay results revealed that compounds 5j, 5k, and 6j exhibited good antitumor effects compared with amonafide.
View Article and Find Full Text PDFDesign, synthesis, and antitumor evaluation of morpholine substituted bisnaphthalimides as DNA targeting agents.
Bioorg Med Chem Lett
April 2023
Guangxi Key Laboratory for Pharmaceutical Molecular Discovery and Druggability Optimization, School of Pharmacy, Guilin Medical University, Guilin 541199, China; Guangxi Engineering Research Center for Pharmaceutical Molecular Screening and Druggability Evaluation, School of Pharmacy, Guilin Medical University, Guilin 5411199, China. Electronic address:
A series of mono- and bisnaphthalimides derivatives containing 3-nitro and 4-morpholine moieties were designed, synthesized, and evaluated for their in vitro anticancer activities against four cancer cell lines. Some compounds exhibited relatively good antiproliferative activity on the cell lines tested, in comparison with mitonafide and amonafide. It is noteworthy that bisnaphthalimide A6 was identified as the most potent compound in anti-proliferation against MGC-803 cells, with an IC lowered to 0.
View Article and Find Full Text PDFA naphthalimide-polyamine conjugate preferentially accumulates in hepatic carcinoma metastases as a lysosome-targeted antimetastatic agent.
Eur J Med Chem
October 2021
School of Pharmacy, Institute for Innovative Drug Design and Evaluation, Henan University, N. Jinming Ave, 475004, Kaifeng, China. Electronic address:
Disseminated tumors lead to approximately 90% of cancer-associated deaths especially for hepatocellular carcinoma (HCC), indicating the imperative need of antimetastatic drugs and the ineffectiveness of current therapies. Recently polyamine derivatives have been identified as a promising prospect in dealing with metastatic tumors. Herein, a novel class of naphthalimide-polyamine conjugates 8a-8d, 13a-13c, 17 and 21 were synthesized and the mechanism was further determined.
View Article and Find Full Text PDFSynthesis, electrochemistry, DNA binding and in vitro cytotoxic activity of tripodal ferrocenyl bis-naphthalimide derivatives.
J Inorg Biochem
June 2021
Key Laboratory of Hui Ethnic Medicine Modernization, Ministry of Education, Ningxia Engineering and Technology Research Center of Characteristic Chinese Medicine Modernization, College of Pharmacy, Ningxia Medical University, Yinchuan 750004, PR China. Electronic address:
A series of tripodal ferrocenyl bis-naphthalimide derivatives were synthesized and characterized. All of the bis-naphthalimide derivatives exhibited good DNA binding ability which was confirmed by ethidium bromide (EB) displacement experiment and ultraviolet (UV)-visible absorption titration. And the binding mode of these compounds was proved to be a hybrid binding mode by experiments.
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