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Farnesyltransferase Inhibitors: Current and Prospective Development for Hematologic Malignancies
Published in Gertjan J. L. Kaspers, Bertrand Coiffier, Michael C. Heinrich, Elihu Estey, Innovative Leukemia and Lymphoma Therapy, 2019
In the clinical arena, Goemans et al. (87) examined drug sensitivity profiles of pediatric leukemias, using a methyl-thiazole-tetrazolium (MTT) assay to compare tipifarnib responsiveness with traditional cytotoxic agents. T-cell ALLs and acute monoblastic AMLs exhibited the greatest tipifarnib sensitivity without correlation between Ras mutational status or in vitro drug responsiveness but with correlation in AML samples between resistance to tipifarnib and resistance to anthracyclines or etoposide. These studies may be a useful template for understanding shared mechanisms of drug resistance among structurally diverse compounds and, in turn, providing insights into strategies by which to overcome such resistance factors.
Hits and Lead Discovery in the Identification of New Drugs against the Trypanosomatidic Infections
Published in Venkatesan Jayaprakash, Daniele Castagnolo, Yusuf Özkay, Medicinal Chemistry of Neglected and Tropical Diseases, 2019
Theodora Calogeropoulou, George E. Magoulas, Ina Pöhner, Joanna Panecka-Hofman, Pasquale Linciano, Stefania Ferrari, Nuno Santarem, Ma Dolores Jiménez-Antón, Ana Isabel Olías-Molero, José María Alunda, Anabela Cordeiro da Silva, Rebecca C. Wade, Maria Paola Costi
Many thiazole derivatives were synthesized and evaluated for their antiparasitic activity during the last year by several research groups. Compound 99 (Filho et al. 2017) showed activity against the trypomastigote form of T. cruzi (IC50 = 0.37 μM), compound 100 (Thompson et al. 2017) with IC50 = 0.055 μM against T. cruzi, and compounds 101 and 102 (Silva et al. 2017b) with IC50 values 1.2 and 1.6 μM, respectively against the trypomastigote form of T. cruzi (Figure 36). Structures of potential hits 99–102.
Drug Targeting to the Lung: Chemical and Biochemical Considerations
Published in Anthony J. Hickey, Sandro R.P. da Rocha, Pharmaceutical Inhalation Aerosol Technology, 2019
Peter A. Crooks, Narsimha R. Penthala, Abeer M. Al-Ghananeem
A-69,412 (39) was reported to be a potent and selective inhibitor of 5-lipoxygenase with a long duration of action, and 1C1-211,965 (40) emerged from a structure-activity relationship study of a (methoxyalkyl)thiazole series designed to inhibit 5-lipoxygenase (Bird et al. 1991). A review of recent advances in 5-lipoxygenase inhibition and the design of newer molecules of this class for the treatment of asthma has been published (Bruno et al. 2018).
Current trends of benzothiazoles in drug discovery: a patent review (2015–2020)
Published in Expert Opinion on Therapeutic Patents, 2022
Christine Shing Wei Law, Keng Yoon Yeong
Thiazole is a five-membered heterocyclic ring comprising sulfur (S) and nitrogen (N) atoms at 1-position and 3-position, respectively. The fusion of thiazole and benzene rings forms 1,3-benzothiazole (BZT), a planar, bicyclic ring system (Figure 1) [1]. BZT was and still is an important pharmacological moiety. Compounds bearing BZT scaffold have been reported to exert anticancer, antiviral, antimicrobial, anticonvulsant, antidepressant, anti-inflammatory and antidiabetic properties, among other therapeutic benefits [1,2]. Some of the BZT-based drugs are as shown in Figure 1. For example, riluzole is a BZT commonly used to treat amyotrophic lateral sclerosis (ALS) and has potential antidepressant and anxiolytic activities [1]. Additionally, various BZT derivatives are in different phases of clinical trials for treatment of various diseases. The successes of existing BZT-based drugs and the advancement of other BZT-based therapeutic agents into clinical trials have amplified the interest in utilizing BZT as a pharmacological scaffold for a myriad of therapeutic applications.
Study of acute oral toxicity of the thiazole derivative N-(1-methyl-2-methyl-pyridine)-N-(p-bromophenylthiazol-2-yl)-hydrazine in a Syrian hamster
Published in Toxicology Mechanisms and Methods, 2021
Vinícius Vasconcelos Gomes de Oliveira, Mary Angela Aranda de Souza, Rafaela Ramos Mororó Cavalcanti, Marcos Veríssimo de Oliveira Cardoso, Ana Cristina Lima Leite, Regina Célia Bressan Queiroz de Figueiredo, Sebastião Rogério de Freitas Silva, Leucio Câmara Alves, Valdemiro Amaro da Silva Junior
Although this is a pioneer study to evaluate the acute oral toxicity of thiazole compounds to Syrian hamster, some studies using ruthenium-arene-thiazole complexes in rats also reported a low acute toxicity of this compound’s class (Grozav et al. 2016). It was observed that this compound was very well tolerated orally, with a LD50 > 2000 mg/kg. Both results demonstrate that thiazole complexes have low toxicity in animals, even though TAP-04 does not have a metal complex in its structure. The comparison with nonmetallic thiazole complexes was not possible because there is no information about this specific structure in the literature. Moreover, the use of hamsters in this study was necessary since these animals are considered the most appropriate model for experimental infection of the VL (Moreira et al. 2016) and TAP-04 will be tested for its potential leishmanicide in this species.
Design, synthesis and biological evaluation of novel thiazole-naphthalene derivatives as potential anticancer agents and tubulin polymerisation inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Guangcheng Wang, Wenjing Liu, Meiyan Fan, Min He, Yongjun Li, Zhiyun Peng
Thiazole is an important heterocyclic scaffold widely found in a range of synthetic bioactive molecules, which has attracted considerable attention in drug discovery over the past decade. Thiazole derivatives displayed a wide range of pharmacological activities, such as anticancer, anti-inflammatory, antioxidant, antimicrobial, anti-HIV, and antibacterial activities12–14. Several thiazole-containing drugs have been approved for clinical use, such as sulphathiazole, ravuconazole, ritonavir, and meloxicam. It's important to note that thiazole could be used as a promising scaffold for the development of anticancer agents15–17. Over the last few years, numerous thiazole derivatives have been reported to show potent anticancer activity by inhibiting tubulin polymerisation (Figure 1, I–IV)18–21.