43036-14-2Relevant academic research and scientific papers
Synthesis and structure-activity relationships of gadolinium complexes of DO3A-benzothiazole conjugates as potential theranostic agents
Jung, Ki-Hye,Kang, Sun-Hee,Kang, Min-Kyoung,Kim, Soyeon,Kim, Hee-Kyung,Kim, Yeoun-Hee,Ho Lee, Gang,Shim, Gyu-Bo,Jung, Jae-Chang,Chang, Yongmin,Kim, Tae-Jeong
, p. 599 - 604 (2015)
The synthesis of two bifunctional chelates, 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid (DO3A) conjugates of benzothiazoles (H3L3a and H3L3b), and the corresponding gadolinium complexes (GdL3a
TARGETED ABERRANT ALPHA-SYNUCLEIN SPECIES AND INDUCED UBIQUITINATION AND PROTEOSOMAL CLEARANCE VIA CO-RECRUITMENT OF AN E3-LIGASE SYSTEM
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, (2022/02/06)
Disclosed are bispecific compounds (degraders) that target α-synuclein protein for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat neurodegenerative diseases.
Metal-chelating benzothiazole multifunctional compounds for the modulation and 64Cu PET imaging of Aβ aggregation
Bandara, Nilantha,Cho, Hong-Jun,Huang, Yiran,Mirica, Liviu M.,Rogers, Buck E.,Sun, Liang,Tran, Diana
, p. 7789 - 7799 (2020/08/19)
While Alzheimer's Disease (AD) is the most common neurodegenerative disease, there is still a dearth of efficient therapeutic and diagnostic agents for this disorder. Reported herein are a series of new multifunctional compounds (MFCs) with appreciable affinity for amyloid aggregates that can be potentially used for both the modulation of Aβ aggregation and its toxicity, as well as positron emission tomography (PET) imaging of Aβ aggregates. Firstly, among the six compounds tested HYR-16 is shown to be capable to reroute the toxic Cu-mediated Aβ oligomerization into the formation of less toxic amyloid fibrils. In addition, HYR-16 can also alleviate the formation of reactive oxygen species (ROS) caused by Cu2+ ions through Fenton-like reactions. Secondly, these MFCs can be easily converted to PET imaging agents by pre-chelation with the 64Cu radioisotope, and the Cu complexes of HYR-4 and HYR-17 exhibit good fluorescent staining and radiolabeling of amyloid plaques both in vitro and ex vivo. Importantly, the 64Cu-labeled HYR-17 is shown to have a significant brain uptake of up to 0.99 ± 0.04 percentID per g. Overall, by evaluating the various properties of these MFCs valuable structure-activity relationships were obtained that should aid the design of improved therapeutic and diagnostic agents for AD. This journal is
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers
Subba Rao,Swapna, Konderu,Shaik, Siddiq Pasha,Lakshma Nayak,Srinivasa Reddy,Sunkari, Satish,Shaik, Thokhir Basha,Bagul, Chandrakant,Kamal, Ahmed
, p. 977 - 999 (2017/02/05)
A series of colchicine site binding tubulin inhibitors were synthesized by the modification of the combretastatin pharmacophore. The ring B was replaced by the pharmacologically relevant benzothiazole scaffolds, and the cis configuration of the olefinic b
2-Arylaminobenzothiazole-arylpropenone conjugates as tubulin polymerization inhibitors
Subba Rao,Rao, Bala Bhaskara,Sunkari, Satish,Shaik, Siddiq Pasha,Shaik, Bajee,Kamal, Ahmed
, p. 924 - 941 (2017/07/12)
A new series of 2-arylaminobenzothiazole-arylpropenone conjugates 5-6(a-r) was designed, synthesized and investigated for their cytotoxic potency against the various human cancer cell lines. Most of these conjugates exhibited cytotoxic activity and inhibi
Design, synthesis and antimetastatic evaluation of 1-benzothiazolylphenylbenzotriazoles for photodynamic therapy in oral cancer cells
Senadi, Gopal Chandru,Liao, Chieh-Ming,Kuo, Kung-Kai,Lin, Jian-Cheng,Chang, Long-Sen,Wang, Jeh Jeng,Hu, Wan-Ping
, p. 1151 - 1158 (2016/07/06)
We have designed and synthesized a new series of 1-benzothiazolylphenylbenzotriazoles 9a-p and studied their antimetastatic mechanism involved in photosensitive effects induced by UVA in oral cancer cell Ca9-22. Our results revealed that the compounds plus UVA significantly suppressed migration and invasion, as detected by wound healing assay and Boyden chamber assay. Quantitative RT-PCR assay indicated that compound 9i plus UVA induced an antimetastatic effect through up-regulation of syndecan-1 and TIMP-3 and down-regulation of heparanase, MMP-2 and MMP-9 mRNA expressions. Western blot analysis showed that Ca9-22 treated with 9i plus UVA resulted in decreased levels of p-EGFR and p-ERK, MMP-2 and MMP-9, and an increased level of TIMP-3. These results are the first to report the function of UVA-activated 1-benzothiazolylphenylbenzotriazoles in tumor metastasis and their underlying molecular mechanism, and thus suggest that compound 9i plus PDT may serve as a potential ancillary modality for the treatment of oral cancer.
The flocculated acryloyldimethyltauric molecule ligand
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Paragraph 0437; 0438, (2016/10/08)
Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.
Gd3+ complexes conjugated to Pittsburgh compound B: Potential MRI markers of β-amyloid plaques Topical Issue on Metal-Based MRI Contrast Agents. Guest editor: Valerie C. Pierre
Martins, André F.,Morfin, Jean-Fran?ois,Geraldes, Carlos F. G. C.,Tóth, éva
, p. 281 - 295 (2014/03/21)
In an effort towards the visualization of β-amyloid (Aβ) plaques by T 1-weighted magnetic resonance imaging for detection of Alzheimer's disease, we report the synthesis and characterization of stable, noncharged Gd3+ complexes of th
Design, synthesis and structure-activity relationship of rhenium 2-arylbenzothiazoles as β-amyloid plaque binding agents
Pan, Jinhe,Mason, Neale S.,Debnath, Manik L.,Mathis, Chester A.,Klunk, William E.,Lin, Kuo-Shyan
, p. 1720 - 1726 (2013/04/10)
To continue our efforts toward the development of 99mTc PiB analogs, we have synthesized 24 neutral and lipophilic Re (as a surrogate of 99mTc) 2-arylbenzothiazoles, and explored their structure-activity relationship for binding to Aβ1-40 fibrils. These Re complexes were designed and synthesized via the integrated approach, so their 99mTc analogs would have a greater chance of crossing the blood-brain barrier. While the lipophilicities (log PC18 = 1.59-3.53) of these Re 2-arylbenzothiazoles were all within suitable range, their binding affinities (Ki = 30-617 nM) to Aβ1-40 fibrils varied widely depending on the selection and integration of the tetradentate chelator into the 2-phenylbenzothiazole pharmacophore. For potential clinical applications, further refinement to obtain Re 2-arylbenzothiazoles with better binding affinities (99mTc analogs for more widespread application via the use of SPECT scanners.
PiB-conjugated, metal-based imaging probes: Multimodal approaches for the visualization of β-amyloid plaques
Martins, Andre F.,Morfin, Jean-Francois,Kubickova, Anna,Kubicek, Vojtech,Buron, Frederic,Suzenet, Franck,Salerno, Milena,Lazar, Adina N.,Duyckaerts, Charles,Arlicot, Nicolas,Guilloteau, Denis,Geraldes, Carlos F. G. C.,Toth, Eva
, p. 436 - 440 (2013/07/11)
In an effort toward the visualization of β-amyloid plaques by in vivo imaging techniques, we have conjugated an optimized derivative of the Pittsburgh compound B (PiB), a well-established marker of Aβ plaques, to DO3A-monoamide that is capable of forming
