Design, synthesis, and evaluation of novel 4-thiazolylimidazoles as inhibitors of transforming growth factor-β type I receptor kinase

Amada, Hideaki; Sekiguchi, Yoshinori; Ono, Naoya; Matsunaga, Yuko; Koami, Takeshi; Asanuma, Hajime; Shiozawa, Fumiyasu; Endo, Mayumi; Ikeda, Akiko; Aoki, Mari; Fujimoto, Natsuko; Wada, Reiko; Sato, Masakazu

doi:10.1016/j.bmcl.2012.01.066

Cited by 13 publications

(2 citation statements)

References 16 publications

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“…Docking studies indicated that benzothiazole ring could bind by hydrogen bonds with NH of His‐283 in the ATP‐binding site of ALK5, while the thiazolyl group could form water‐mediated networks of hydrogen bonds with the carboxy oxygen of Glu‐245, the hydroxyl hydrogen of Tyr‐249, and the backbone NH of Asp‐351. This was in concordance with the typical hydrogen bond acceptor …”

Section: Imidazoles As Anticancer Agentssupporting

confidence: 88%

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

et al. 2013

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Imidazole ring is an important five-membered aromatic heterocycle widely present in natural products and synthetic molecules. The unique structural feature of imidazole ring with desirable electron-rich characteristic is beneficial for imidazole derivatives to readily bind with a variety of enzymes and receptors in biological systems through diverse weak interactions, thereby exhibiting broad bioactivities. The related research and developments of imidazole-based medicinal chemistry have become a rapidly developing and increasingly active topic. Particularly, numerous imidazole-based compounds as clinical drugs have been extensively used in the clinic to treat various types of diseases with high therapeutic potency, which have shown the enormous development value. This work systematically gives a comprehensive review in current developments of imidazole-based compounds in the whole range of medicinal chemistry as anticancer, antifungal, antibacterial, antitubercular, anti-inflammatory, antineuropathic, antihypertensive, antihistaminic, antiparasitic, antiobesity, antiviral, and other medicinal agents, together with their potential applications in diagnostics and pathology. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic imidazole-based medicinal drugs, as well as more effective diagnostic agents and pathologic probes.

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Section: Imidazoles As Anticancer Agentssupporting

confidence: 88%

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

et al. 2013

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“…As a case study, we report herein a result which demonstrates a novel, efficient, and yet extremely simple application of elemental sulfur in the synthesis of benzothiazoles. This targeted heterocyclic structure is one of the privileged scaffolds widely found in pharmaceutically important compounds as well as functional materials . Different strategies have been developed to achieve efficiently the synthesis of this motif, in which prefunctionalized substrates, such as ortho -thiol or -halo anilines/anilides or thioanilides, were used.…”

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confidence: 99%